Any feedback?
Information on EC 3.4.22.38 - cathepsin K
for references in articles please use BRENDA:EC3.4.22.38Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
EC Tree
3.4.22.38 cathepsin KSpecify your search results
Word Map
- 3.4.22.38
- resorption
- osteoporosis
-
osteoclastogenesis
- rankl
-
tartrate-resistant
- osteoblast
- collagen
- nfatc1
-
rankl-induced
-
multinucleated
- mmp-9
- c-fos
-
fracture
-
trabecular
- pi
- calcitonin
- osteocalcin
- osteoprotegerin
-
osteolytic
-
resorb
- m-csf
-
collagenolytic
- bisphosphonates
-
osteoclast-mediated
-
trap-positive
-
osteoclast-specific
- odanacatib
- oscar
-
antiresorptive
- tracp
- lacuna
-
ovariectomy-induced
-
rankl-mediated
-
dc-stamp
-
bone-resorbing
-
sclerostin
-
osteoclast-related
-
telopeptide
-
osteoclast-like
-
osteoclastogenic
-
denosumab
-
preosteoclasts
-
teriparatide
- pharmacology
-
anti-osteoclastogenic
- osteosclerosis
-
anti-osteoporotic
- atp6v0d2
- medicine
-
ranelate
- drug development
-
deoxypyridinoline
-
rankl-stimulated
- diagnostics
The enzyme appears in viruses and cellular organisms
Synonyms
cathepsin k, cathepsin-k, cat k, cath k, cat-k, cathepsin o2, oc-2 protein, 
more
topPlease wait a moment until the data is sorted. This message will disappear when the data is sorted.
SYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
Cat K
cath K
cathepsin K
Cathepsin O2
catK
CTSK
OC-2 protein
-
-
-
-
rhCK
-
-
-
-
additional information
Cat K
-
-
cathepsin K
-
-
Cathepsin O2
-
-
-
-
catK
-
-
additional information
-
cathepsin K is a member of the papain family of cysteine proteases
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
Broad proteolytic activity. With small-molecule substrates and inhibitors, the major determinant of specificity is P2, which is preferably Leu, Met > Phe, and not Arg
endopeptidase
-
-
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of peptide bond
hydrolysis of peptide bond
-
-
-
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
CAS REGISTRY NUMBER
COMMENTARY
94716-09-3
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
Abz-His-Pro-Gly-Gly-Pro-Gln-EDDnp + H2O
?
-
cathepsin k is unusual among the cysteine cathepsins since it can cleave substrates with Pro in the P2 position. A specific peptide substrate for cathepsin K is developed (kcat/Km: 426000/Msec) that is resistant to proteolysis by cathepsin B, L, S, F, H,V and the serine proteases (cathepsin G, chymotrypsin and leukocyte elastase)
-
-
?
Ac-Lys-His-Pro-Lys-7-amido-3-carbamoylmethyl-4-methylcoumarin + H2O
Ac-Lys-His-Pro-Lys + 7-amino-3-carbamoylmethyl-4-methylcoumarin
-
assay at pH 5.5, 37°C
-
-
?
Acetyl-Phe-Arg 4-methylcoumarin 7-amide + H2O
Acetyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Ala-Ala-Phe-7-amido-4-methylcoumarin + H2O
Ala-Ala-Phe + 7-amino-4-methylcoumarin
31.29% activity compared to benzyloxycarbonyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin
-
-
?
Benzoyl-Arg 4-methylcoumarin 7-amide + H2O
Benzoyl-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Benzoyl-Phe-Val-Arg 4-methylcoumarin 7-amide + H2O
Benzoyl-Phe-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Benzyloxycarbonyl-Arg-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Arg-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Arg-Arg + 7-amino-4-methylcoumarin
47.92% activity compared to benzyloxycarbonyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin
-
-
?
Benzyloxycarbonyl-Glu-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Glu-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Gly-Gly-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Gly-Gly-Arg + 7-amino-4-methylcoumarin
89.78% activity compared to benzyloxycarbonyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin
-
-
?
benzyloxycarbonyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Gly-L-Pro-L-Arg + 7-amino-4-methylcoumarin
Benzyloxycarbonyl-Gly-Pro-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Gly-Pro-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Gly-Pro-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Gly-Pro-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Benzyloxycarbonyl-Leu-Arg 4-methoxy-2-naphthylamide + H2O
Benzyloxycarbonyl-Leu-Arg + 4-methoxy-2-naphthylamine
Benzyloxycarbonyl-Leu-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Leu-Arg + 7-amino-4-methylcoumarin
benzyloxycarbonyl-Leu-Arg-4-methylcoumarin 7-amide + H2O
benzyloxycarbonyl-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Benzyloxycarbonyl-Leu-Leu-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Leu-Leu-Arg + 7-amino-4-methylcoumarin
benzyloxycarbonyl-Leu-Leu-Glu-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Leu-Leu-Glu + 7-amino-4-methylcoumarin
23.91% activity compared to benzyloxycarbonyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin
-
-
?
Benzyloxycarbonyl-Phe-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
?
-
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
Benzyloxycarbonyl-Phe-Pro-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Phe-Pro-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Benzyloxycarbonyl-Val-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Benzyloxycarbonyl-Val-Val-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
carbobenzoxy-Gly-Pro-Arg-7-amido-4-methylcoumarin + H2O
carbobenzoxy-Gly-Pro-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
carbobenzoxy-Phe-Arg-7-amido-4-methylcoumarin + H2O
carbobenzoxy-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
?
carbobenzyloxy-Gly-Pro-Arg-4-methylcoumaryl-7-amide + H2O
carbobenzyloxy-Gly-Pro-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
carbobenzyloxy-Leu-Arg-4-methoxy-2-naphthylamide + H2O
carbobenzyloxy-Leu-Arg + 4-methoxy-2-naphthylamine
-
-
-
-
?
carbobenzyloxy-Leu-Arg-4-methylcoumaryl-7-amide + H2O
carbobenzyloxy-Leu-Arg + 7-amino-4-methylcoumarin
carbobenzyloxy-Phe-Arg-4-methylcoumaryl-7-amide + H2O
carbobenzyloxy-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Cbz-Phe-Arg-7-amido-4-methylcoumarin + H2O
Cbz-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
chemo-attractant stromal-derived factor-1alpha + H2O
?
the enzyme cleaves chemo-attractant stromal-derived factor-1alpha (SDF-1alpha) at 3 sites in the N-terminus, which is the region of SDF-1alpha that binds to its receptors
-
-
?
Collagen type II + H2O
Fragments of collagen type II
-
-
cleavage near the N-terminal region within the helical domain, Pro in P2- position
?
D-Ala-Leu-Lys-7-amido-4-methylcoumarin + H2O
D-Ala-Leu-Lys + 7-amino-4-methylcoumarin
-
-
-
-
?
D-Phe-Phe-Arg 4-methylcoumarin 7-amide + H2O
D-Phe-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Lys-Gln-Lys-Leu-Arg-4-methylcoumarin-7-amide + H2O
Lys-Gln-Lys-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
N-succinyl-Ala-Ala-Pro-Phe-7-amido-4-methylcoumarin + H2O
N-succinyl-Ala-Ala-Pro-Phe + 7-amino-4-methylcoumarin
24.13% activity compared to benzyloxycarbonyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin
-
-
?
N-succinyl-Ile-Ala-7-amido-4-methylcoumarin + H2O
N-succinyl-Ile-Ala + 7-amino-4-methylcoumarin
17.34% activity compared to benzyloxycarbonyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin
-
-
?
N-succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin + H2O
N-succinyl-Leu-Leu-Val-Tyr + 7-amino-4-methylcoumarin
25.03% activity compared to benzyloxycarbonyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin
-
-
?
N-succinyl-Leu-Tyr-7-amido-4-methylcoumarin + H2O
N-succinyl-Leu-Tyr + 7-amino-4-methylcoumarin
31.57% activity compared to benzyloxycarbonyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin
-
-
?
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-alaninamide + H2O
?
-
-
-
-
?
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-methioninamide + H2O
?
-
-
-
-
?
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucylglycinamide + H2O
?
-
-
-
-
?
Osteonectin + H2O
Fragments of osteonectin
-
-
the cleavage products are of MW 34000 and 14000. The 34000 Da protein represents the amino-terminus of osteonectin minus three amino acids Ala-Pro-Gln. Cleavage of the Arg-Val bond in the sequence Gln-Lys-Leu-Arg-Val-Lys-Ole-His of the 14000 Da fragment. The presence of Lsu-Arg at position P2-P1 is favorable
?
Succinyl-Leu-Tyr 4-methylcoumarin 7-amide + H2O
Succinyl-Leu-Tyr + 7-amino-4-methylcoumarin
-
-
-
-
?
tert-Butyloxycarbonyl-Ala-Gly-Pro-Arg 4-methylcoumarin 7-amide + H2O
tert-Butyloxycarbonyl-Ala-Gly-Pro-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
tert-Butyloxycarbonyl-Phe-Val-Arg 4-methylcoumarin 7-amide + H2O
tert-Butyloxycarbonyl-Phe-Val-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
tert-Butyloxycarbonyl-Val-Leu-Lys 4-methylcoumarin 7-amide + H2O
tert-Butyloxycarbonyl-Val-Leu-Lys + 7-amino-4-methylcoumarin
-
-
-
-
?
tert-Butyloxycarbonyl-Val-Pro-Arg 4-methylcoumarin 7-amide + H2O
tert-Butyloxycarbonyl-Val-Pro-Arg + 7-amino-4-methylcoumarin
Tosyl-Gly-Pro-Arg 4-methylcoumarin 7-amide + H2O
Tosyl-Gly-Pro-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
type II collagen + H2O
?
-
cathepsin K cleaves the triple helix of type II collagen
-
-
?
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin + H2O
Z-Gly-Pro-Arg + 7-amino-4-methylcoumarin
-
-
-
?
benzyloxycarbonyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Gly-L-Pro-L-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Gly-L-Pro-L-Arg + 7-amino-4-methylcoumarin
100% activity
-
-
?
Benzyloxycarbonyl-Leu-Arg 4-methoxy-2-naphthylamide + H2O
Benzyloxycarbonyl-Leu-Arg + 4-methoxy-2-naphthylamine
-
-
-
-
?
Benzyloxycarbonyl-Leu-Arg 4-methoxy-2-naphthylamide + H2O
Benzyloxycarbonyl-Leu-Arg + 4-methoxy-2-naphthylamine
-
-
-
-
?
Benzyloxycarbonyl-Leu-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Benzyloxycarbonyl-Leu-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Benzyloxycarbonyl-Leu-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Benzyloxycarbonyl-Leu-Leu-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Leu-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Benzyloxycarbonyl-Leu-Leu-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Leu-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Benzyloxycarbonyl-Phe-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Benzyloxycarbonyl-Phe-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
71.17% activity compared to benzyloxycarbonyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin
-
-
?
carbobenzyloxy-Leu-Arg-4-methylcoumaryl-7-amide + H2O
carbobenzyloxy-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
?
carbobenzyloxy-Leu-Arg-4-methylcoumaryl-7-amide + H2O
carbobenzyloxy-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
?
CBZ-Phe-Arg-4-methylcoumarin 7-amide + H2O
CBZ-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
CBZ-Phe-Arg-4-methylcoumarin 7-amide + H2O
CBZ-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
?
CBZ-Phe-Arg-4-methylcoumarin 7-amide + H2O
CBZ-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Collagen + H2O
?
-
cathepsin K cleaves within the telo as well as triple helical domains of collagens
-
-
?
collagen I + H2O
?
-
Cat K can degrade several bone matrix proteins including type I collagen during osteoclastic bone resorption
-
-
?
collagen I + H2O
?
-
cathepsin K is responsible for the degradation of type I collagen in osteoclast-mediated bone resorption. Cathepsin K interaction with type I collagen is required for 1. the release of cryptic Arg-Gly-Asp motifs during the initial attachment of osteoclasts and 2. termination of resorption via the creation of autocrine signals originating from type I collagen degradation, overview
-
-
?
collagen I + H2O
?
-
cathepsin K is the only cathepsin that can degrade native type-I collagen in a triple-helix structure
-
-
?
collagen I + H2O
?
-
osteoclasts degrade bone matrix by demineralization followed by degradation of type I collagen through secretion of the cysteine protease, cathepsin K
-
-
?
collagen I + H2O
?
-
the lysosomal cysteine protease cathepsin K plays a key role in the degradation of the bone matrix, Cat K deficiency leads to an increase in bone mineral density
-
-
?
collagen I + H2O
?
-
cathepsin K inhibition by cathepsin K inhibitor significantly increases the bone mineral density and the bone volume of the primary and secondary spongiosa, with a reduction of the urinary C-telopeptide of type I collagen that is increased by ovariectomized surgery compared to sham surgery, respectively, overview
-
-
?
collagen I + H2O
?
-
cathepsin K is responsible for the degradation of type I collagen in osteoclast-mediated bone resorption. Cathepsin K interaction with type I collagen is required for 1. the release of cryptic Arg-Gly-Asp motifs during the initial attachment of osteoclasts and 2. termination of resorption via the creation of autocrine signals originating from type I collagen degradation, overview
-
-
?
collagen I + H2O
?
-
cathepsin K regulates adipocyte differentiation, possible involvement of type I collagen degradation and regulation of collagen type I expression, molecular mechanism, overview
-
-
?
collagen I + H2O
?
-
CatK is a cysteine protease expressed predominantly in osteoclastsosteoclasts, that plays a prominent role in degrading type I collagen. Growing CatK null mice have osteopetrosis associated with a reduced ability to degrade bone matrix
-
-
?
collagen I + H2O
?
-
inhibition of cathepsin K reduces bone erosion, cartilage degradation and inflammation evoked by collagen-induced arthritis in mice, overview
-
-
?
collagen I + H2O
?
-
osteoclasts degrade bone matrix by demineralization followed by degradation of type I collagen through secretion of the cysteine protease, cathepsin K
-
-
?
collagen I + H2O
?
-
cathepsin K is responsible for the degradation of type I collagen in osteoclast-mediated bone resorption. Cathepsin K interaction with type I collagen is required for 1. the release of cryptic Arg-Gly-Asp motifs during the initial attachment of osteoclasts and 2. termination of resorption via the creation of autocrine signals originating from type I collagen degradation, overview
-
-
?
collagen I + H2O
?
-
inhibition of cathepsin K reduces bone erosion, cartilage degradation and inflammation evoked by collagen-induced arthritis in mice, overview
-
-
?
collagen I + H2O
?
-
cathepsin K is the only cathepsin that can degrade native type-I collagen in a triple-helix structure
-
-
?
collagen II + H2O
?
-
cathepsin K is a cysteine protease which can also cleave the triple helix of type II collagen
-
-
?
collagen II + H2O
?
-
cathepsin K is a cysteine protease of the papain family that cleaves triple-helical type II collagen, the major structural component of the extracellular matrix of articular cartilage
-
-
?
Collagen type I + H2O
Fragemnts of collagen type I
-
-
cleavage in telopeptide region
?
Collagen type I + H2O
Fragemnts of collagen type I
-
-
cleavage near the N-terminal region within the helical domain, Pro in P2- position
?
Elastin + H2O
?
-
the elastinolytic activity of cathepsin K at pH 7.4 is 60% of that observed at pH 6.2
-
-
?
Gelatin + H2O
?
-
cathepsin K maintains activity on gelatin at pH 7.0 and 8.0
-
-
?
Gelatin + H2O
?
distinct cathepsin K/chondroitin 4-sulfate interactions are necessary for the collagenolytic activity of the enzyme
-
-
?
kinin + H2O
?
-
the potency of cathepsin K to modulate bradikinin-dependent contraction of smooth muscles, cathepsin K may act as a kininase
-
-
?
matrix-metalloproteinase-9 + H2O
?
cathepsin K is responsible for the activation of pro-MMP-9. Knocking down cathepsin K in MDA-MB-231 cells also diminishes MMP-9 activity compared to wild type control
-
-
?
Pro-Phe-Arg 4-methylcoumarin 7-amide + H2O
Pro-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Pro-Phe-Arg 4-methylcoumarin 7-amide + H2O
Pro-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Protein + H2O
?
-
remodeling of extracellular bone matrix, together with other collagenolytic and gelatinolytic enzymes
-
-
?
Protein + H2O
?
-
involved in bone resorption, hydrolysis of proteinaceous bone matrix in the process of remodeling of the human skeleton
-
-
?
tartrate-resistant acid phosphatase + H2O
?
-
cathepsin K, colocalizes with tartrate-resistant acid phosphatase in osteoclast-resorptive compartments, supporting a role for cathepsin K in the extracellular processing of monomeric tartrate-resistant acid phosphatase in the resorption lacuna
-
-
?
tartrate-resistant acid phosphatase + H2O
?
-
processing by cathepsin K occurs sequentially by an initial excision of the loop peptide Gly143Gly160 followed by the removal of a Val161Ala162 dipeptide at the N-terminus of the C-terminal 16-kDa subunit of tartrate-resistant acid phosphatase
-
-
?
tert-Butyloxycarbonyl-Val-Pro-Arg 4-methylcoumarin 7-amide + H2O
tert-Butyloxycarbonyl-Val-Pro-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
tert-Butyloxycarbonyl-Val-Pro-Arg 4-methylcoumarin 7-amide + H2O
tert-Butyloxycarbonyl-Val-Pro-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Type I collagen + H2O
?
-
cleavage sites in type I collagen are telopeptides and multiple sites in triple helix
-
-
?
Z-Leu-Arg-4-methylcoumarin 7-amide + H2O
Z-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Z-Leu-Arg-4-methylcoumarin 7-amide + H2O
Z-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Z-Leu-Arg-7-amido-4-methylcoumarin + H2O
Z-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Z-Leu-Arg-7-amido-4-methylcoumarin + H2O
Z-Leu-Arg + 7-amino-4-methylcoumarin
-
-
-
?
Z-Phe-Arg-4-methylcoumarin 7-amide + H2O
Z-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Z-Phe-Arg-4-methylcoumarin 7-amide + H2O
Z-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Z-Phe-Arg-7-amido-4-methylcoumarin + H2O
Z-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Z-Phe-Arg-7-amido-4-methylcoumarin + H2O
Z-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
?
Z-Phe-Arg-7-amido-4-methylcoumarin + H2O
Z-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
additional information
?
-
-
cathepsin K degrades several bone and cartilage matrix components, it is playing a role in osteoarthritis, enzyme inhibition reduces the degradation process, overview
-
-
?
additional information
?
-
-
cathepsin K degrades articular cartilage in naturally occurring equine osteoarthritis, it plays a role in both lesional and peri-lesional regions, overview
-
-
?
additional information
?
-
-
cathepsin K degrades articular cartilage in naturally occurring equine osteoarthritis
-
-
?
additional information
?
-
-
bone mineral density values show no statistically significant association with any of the individual cathepsin K polymorphisms or cathepsin K haplotypes (in a large cohort of perimenopausal women from Scotland)
-
-
?
additional information
?
-
-
cathepsin K could be one of the determinants of adipocyte differentiation and may be involved in the pathogenesis of obesity by promoting adipocyte differentiation
-
-
?
additional information
?
-
-
cathepsin K plays a critical role in the degradation of bone and appears to be a limiting step in osteoclastic bone resorption
-
-
?
additional information
?
-
-
cathepsin K plays a pivotal role in lung matrix homeostasis under physiological and pathological conditions
-
-
?
additional information
?
-
-
the NIRF imaging agent consists of the CatK peptide substrate GHPGGPQGKC-NH2 linked to an activatable fluorogenic polymer. In vitro, CatK produces a 2- to 14fold activation of the agent
-
-
?
additional information
?
-
-
CAT K plays a significant role in numerous important physiological and pathological processes, such as bone resorption, cancer progression and atherosclerosis
-
-
?
additional information
?
-
-
cathepsin K is a lysosomal cysteine protease that is highly and selectively expressed in osteoclasts, the cells which degrade bone during the continuous cycle of bone degradation and formation
-
-
?
additional information
?
-
-
cathepsin K is involved in bone resorption, resorption of bone is performed by osteoclasts, the function of which is controlled by receptor activator of NF-kappaB ligand, overview
-
-
?
additional information
?
-
-
cathepsin K is the key regulator in the osteoclast-mediated bone resorption
-
-
?
additional information
?
-
-
cathepsin K is the major collagenolytic enzyme produced by bone-resorbing osteoclasts
-
-
?
additional information
?
-
-
cathepsin K plays a role in osteoclast mediated bone resorption, it is responsible for the degradation of the collagen matrix of the bone after the removal of its mineral components. Deficiency of cathepsin K causes pycnodysostosis, a rare skeletal dysplasia presenting with bone abnormalities such as short stature, osteosclerosis, acro-osteolysis of distal phalanges, and skull deformities
-
-
?
additional information
?
-
-
deficiency and inhibition of cathepsin K reduce preadipocyte adipogenesis, body weight gain, and increase glucose metabolism in mice, selective inhibition of the enzyme in adipose tissue blocks the lipid accumulation in preadipocytes, overview
-
-
?
additional information
?
-
-
expression of cathepsin K indicates persistent osteodestructive activity in longstanding ankylosing spondylitis, a frequent largely genetically determined rheumatic disease that is characterised by spinal inflammation and new bone formation
-
-
?
additional information
?
-
-
generation of a C-terminal neoepitope, C2K, in triple-helical type II collagen by the proteolytic action of cathepsin K, the optimal concentration of cathepsin K for generation of C2K neoepitope is 0.01 mM, effects of its presence in normal adult and osteoarthritic femoral condylar articular cartilage, overview
-
-
?
additional information
?
-
-
important role of cathepsin K in osteoclast function, overview. The human disorder pycnodysostosis is a rare, autosomal, recessive, skeletal disorder caused by mutations in cathepsin K, the enzyme might be also involved in the pathological mechanism of osteolysis causing aseptic loosening of total hip replacement implants. In diseases such as arthritis and osteoporosis, the release of cathepsin K likely causes tissue injury. Regulation of cathepsin K expression, overview
-
-
?
additional information
?
-
-
media from cells on plastic show higher CatK activation than cells on dentin, consistent with cellular expression of cathepsin K mRNA, 2fold upregulation of cathepsin K mRNA from cells cultured on plastic correlates with increased cathepsin K activation, overview
-
-
?
additional information
?
-
-
the enzyme may play a role in tumor progression, coculture of CTSK+ fibroblasts enhances the invasion of CTSK-breast tumor epithelial cells, whichis blocked by CTSK inhibitors, overview
-
-
?
additional information
?
-
human cathepsin K preferentially hydrolyses the substrates with Pro at the P2 position, substrate specificity compared to the rat enzyme, overview
-
-
?
additional information
?
-
-
human cathepsin K preferentially hydrolyses the substrates with Pro at the P2 position, substrate specificity compared to the rat enzyme, overview
-
-
?
additional information
?
-
-
cathepsin K plays a role in collagen degradation
-
-
?
additional information
?
-
-
2-aminobenzoyl-RP-PGFSPFR-(3-nitrotyrosine) is not cleaved by the mutant enzyme Y67L/L205A
-
-
?
additional information
?
-
-
absence of leucocyte CatK results in dramatically decreased collagen and increased macrophage content of the atherosclerotic lesions while lesion size is not affected
-
-
?
additional information
?
-
-
Cat K plays a key role in matrix degradation during bone resorption
-
-
?
additional information
?
-
-
cathepsin K plays a role in bone tissue development as well as skeletal remodeling, overview
-
-
?
additional information
?
-
-
deficiency and inhibition of cathepsin K reduce body weight gain and increase glucose metabolism, reducing serum glucose and insulin levels, in mice, selective inhibition of the enzyme in adipose tissue blocks the lipid accumulation in preadipocytes, overview
-
-
?
additional information
?
-
-
media from cells on plastic show higher CatK activation than cells on dentin, consistent with cellular expression of cathepsin K mRNA, 2fold upregulation of cathepsin K mRNA from cells cultured on plastic correlates with increased cathepsin K activation, overview
-
-
?
additional information
?
-
-
cathepsin K plays a role in bone tissue development as well as skeletal remodeling, overview
-
-
?
additional information
?
-
cathepsin K is not able to hydrolyze protein substrates such as azocasein, fibrinogen, and bovine serum albumin
-
-
?
additional information
?
-
-
cathepsin K is not able to hydrolyze protein substrates such as azocasein, fibrinogen, and bovine serum albumin
-
-
?
additional information
?
-
rat cathepsin K preferentially hydrolyses the substrates at the P2 Hyp position, substrate specificity compared to the human enzyme, overview
-
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
chemo-attractant stromal-derived factor-1alpha + H2O
?
the enzyme cleaves chemo-attractant stromal-derived factor-1alpha (SDF-1alpha) at 3 sites in the N-terminus, which is the region of SDF-1alpha that binds to its receptors
-
-
?
Collagen + H2O
?
-
cathepsin K cleaves within the telo as well as triple helical domains of collagens
-
-
?
matrix-metalloproteinase-9 + H2O
?
cathepsin K is responsible for the activation of pro-MMP-9. Knocking down cathepsin K in MDA-MB-231 cells also diminishes MMP-9 activity compared to wild type control
-
-
?
tartrate-resistant acid phosphatase + H2O
?
-
cathepsin K, colocalizes with tartrate-resistant acid phosphatase in osteoclast-resorptive compartments, supporting a role for cathepsin K in the extracellular processing of monomeric tartrate-resistant acid phosphatase in the resorption lacuna
-
-
?
type II collagen + H2O
?
-
cathepsin K cleaves the triple helix of type II collagen
-
-
?
collagen I + H2O
?
-
Cat K can degrade several bone matrix proteins including type I collagen during osteoclastic bone resorption
-
-
?
collagen I + H2O
?
-
cathepsin K is responsible for the degradation of type I collagen in osteoclast-mediated bone resorption. Cathepsin K interaction with type I collagen is required for 1. the release of cryptic Arg-Gly-Asp motifs during the initial attachment of osteoclasts and 2. termination of resorption via the creation of autocrine signals originating from type I collagen degradation, overview
-
-
?
collagen I + H2O
?
-
cathepsin K is the only cathepsin that can degrade native type-I collagen in a triple-helix structure
-
-
?
collagen I + H2O
?
-
osteoclasts degrade bone matrix by demineralization followed by degradation of type I collagen through secretion of the cysteine protease, cathepsin K
-
-
?
collagen I + H2O
?
-
the lysosomal cysteine protease cathepsin K plays a key role in the degradation of the bone matrix, Cat K deficiency leads to an increase in bone mineral density
-
-
?
collagen I + H2O
?
-
cathepsin K inhibition by cathepsin K inhibitor significantly increases the bone mineral density and the bone volume of the primary and secondary spongiosa, with a reduction of the urinary C-telopeptide of type I collagen that is increased by ovariectomized surgery compared to sham surgery, respectively, overview
-
-
?
collagen I + H2O
?
-
cathepsin K is responsible for the degradation of type I collagen in osteoclast-mediated bone resorption. Cathepsin K interaction with type I collagen is required for 1. the release of cryptic Arg-Gly-Asp motifs during the initial attachment of osteoclasts and 2. termination of resorption via the creation of autocrine signals originating from type I collagen degradation, overview
-
-
?
collagen I + H2O
?
-
cathepsin K regulates adipocyte differentiation, possible involvement of type I collagen degradation and regulation of collagen type I expression, molecular mechanism, overview
-
-
?
collagen I + H2O
?
-
CatK is a cysteine protease expressed predominantly in osteoclastsosteoclasts, that plays a prominent role in degrading type I collagen. Growing CatK null mice have osteopetrosis associated with a reduced ability to degrade bone matrix
-
-
?
collagen I + H2O
?
-
inhibition of cathepsin K reduces bone erosion, cartilage degradation and inflammation evoked by collagen-induced arthritis in mice, overview
-
-
?
collagen I + H2O
?
-
osteoclasts degrade bone matrix by demineralization followed by degradation of type I collagen through secretion of the cysteine protease, cathepsin K
-
-
?
collagen I + H2O
?
-
cathepsin K is responsible for the degradation of type I collagen in osteoclast-mediated bone resorption. Cathepsin K interaction with type I collagen is required for 1. the release of cryptic Arg-Gly-Asp motifs during the initial attachment of osteoclasts and 2. termination of resorption via the creation of autocrine signals originating from type I collagen degradation, overview
-
-
?
collagen I + H2O
?
-
inhibition of cathepsin K reduces bone erosion, cartilage degradation and inflammation evoked by collagen-induced arthritis in mice, overview
-
-
?
collagen I + H2O
?
-
cathepsin K is the only cathepsin that can degrade native type-I collagen in a triple-helix structure
-
-
?
collagen II + H2O
?
-
cathepsin K is a cysteine protease which can also cleave the triple helix of type II collagen
-
-
?
collagen II + H2O
?
-
cathepsin K is a cysteine protease of the papain family that cleaves triple-helical type II collagen, the major structural component of the extracellular matrix of articular cartilage
-
-
?
Gelatin + H2O
?
-
cathepsin K maintains activity on gelatin at pH 7.0 and 8.0
-
-
?
Gelatin + H2O
?
distinct cathepsin K/chondroitin 4-sulfate interactions are necessary for the collagenolytic activity of the enzyme
-
-
?
kinin + H2O
?
-
the potency of cathepsin K to modulate bradikinin-dependent contraction of smooth muscles, cathepsin K may act as a kininase
-
-
?
Protein + H2O
?
-
remodeling of extracellular bone matrix, together with other collagenolytic and gelatinolytic enzymes
-
-
?
Protein + H2O
?
-
involved in bone resorption, hydrolysis of proteinaceous bone matrix in the process of remodeling of the human skeleton
-
-
?
Type I collagen + H2O
?
-
cleavage sites in type I collagen are telopeptides and multiple sites in triple helix
-
-
?
additional information
?
-
-
cathepsin K degrades several bone and cartilage matrix components, it is playing a role in osteoarthritis, enzyme inhibition reduces the degradation process, overview
-
-
?
additional information
?
-
-
cathepsin K degrades articular cartilage in naturally occurring equine osteoarthritis, it plays a role in both lesional and peri-lesional regions, overview
-
-
?
additional information
?
-
-
cathepsin K degrades articular cartilage in naturally occurring equine osteoarthritis
-
-
?
additional information
?
-
-
bone mineral density values show no statistically significant association with any of the individual cathepsin K polymorphisms or cathepsin K haplotypes (in a large cohort of perimenopausal women from Scotland)
-
-
?
additional information
?
-
-
cathepsin K could be one of the determinants of adipocyte differentiation and may be involved in the pathogenesis of obesity by promoting adipocyte differentiation
-
-
?
additional information
?
-
-
cathepsin K plays a critical role in the degradation of bone and appears to be a limiting step in osteoclastic bone resorption
-
-
?
additional information
?
-
-
cathepsin K plays a pivotal role in lung matrix homeostasis under physiological and pathological conditions
-
-
?
additional information
?
-
-
CAT K plays a significant role in numerous important physiological and pathological processes, such as bone resorption, cancer progression and atherosclerosis
-
-
?
additional information
?
-
-
cathepsin K is a lysosomal cysteine protease that is highly and selectively expressed in osteoclasts, the cells which degrade bone during the continuous cycle of bone degradation and formation
-
-
?
additional information
?
-
-
cathepsin K is involved in bone resorption, resorption of bone is performed by osteoclasts, the function of which is controlled by receptor activator of NF-kappaB ligand, overview
-
-
?
additional information
?
-
-
cathepsin K is the key regulator in the osteoclast-mediated bone resorption
-
-
?
additional information
?
-
-
cathepsin K is the major collagenolytic enzyme produced by bone-resorbing osteoclasts
-
-
?
additional information
?
-
-
cathepsin K plays a role in osteoclast mediated bone resorption, it is responsible for the degradation of the collagen matrix of the bone after the removal of its mineral components. Deficiency of cathepsin K causes pycnodysostosis, a rare skeletal dysplasia presenting with bone abnormalities such as short stature, osteosclerosis, acro-osteolysis of distal phalanges, and skull deformities
-
-
?
additional information
?
-
-
deficiency and inhibition of cathepsin K reduce preadipocyte adipogenesis, body weight gain, and increase glucose metabolism in mice, selective inhibition of the enzyme in adipose tissue blocks the lipid accumulation in preadipocytes, overview
-
-
?
additional information
?
-
-
expression of cathepsin K indicates persistent osteodestructive activity in longstanding ankylosing spondylitis, a frequent largely genetically determined rheumatic disease that is characterised by spinal inflammation and new bone formation
-
-
?
additional information
?
-
-
generation of a C-terminal neoepitope, C2K, in triple-helical type II collagen by the proteolytic action of cathepsin K, the optimal concentration of cathepsin K for generation of C2K neoepitope is 0.01 mM, effects of its presence in normal adult and osteoarthritic femoral condylar articular cartilage, overview
-
-
?
additional information
?
-
-
important role of cathepsin K in osteoclast function, overview. The human disorder pycnodysostosis is a rare, autosomal, recessive, skeletal disorder caused by mutations in cathepsin K, the enzyme might be also involved in the pathological mechanism of osteolysis causing aseptic loosening of total hip replacement implants. In diseases such as arthritis and osteoporosis, the release of cathepsin K likely causes tissue injury. Regulation of cathepsin K expression, overview
-
-
?
additional information
?
-
-
media from cells on plastic show higher CatK activation than cells on dentin, consistent with cellular expression of cathepsin K mRNA, 2fold upregulation of cathepsin K mRNA from cells cultured on plastic correlates with increased cathepsin K activation, overview
-
-
?
additional information
?
-
-
the enzyme may play a role in tumor progression, coculture of CTSK+ fibroblasts enhances the invasion of CTSK-breast tumor epithelial cells, whichis blocked by CTSK inhibitors, overview
-
-
?
additional information
?
-
-
cathepsin K plays a role in collagen degradation
-
-
?
additional information
?
-
-
absence of leucocyte CatK results in dramatically decreased collagen and increased macrophage content of the atherosclerotic lesions while lesion size is not affected
-
-
?
additional information
?
-
-
Cat K plays a key role in matrix degradation during bone resorption
-
-
?
additional information
?
-
-
cathepsin K plays a role in bone tissue development as well as skeletal remodeling, overview
-
-
?
additional information
?
-
-
deficiency and inhibition of cathepsin K reduce body weight gain and increase glucose metabolism, reducing serum glucose and insulin levels, in mice, selective inhibition of the enzyme in adipose tissue blocks the lipid accumulation in preadipocytes, overview
-
-
?
additional information
?
-
-
media from cells on plastic show higher CatK activation than cells on dentin, consistent with cellular expression of cathepsin K mRNA, 2fold upregulation of cathepsin K mRNA from cells cultured on plastic correlates with increased cathepsin K activation, overview
-
-
?
additional information
?
-
-
cathepsin K plays a role in bone tissue development as well as skeletal remodeling, overview
-
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
((S)-1-[1-[4(R,S)-((S)-2-benzyloxycarbonylamino-4-methylpentanoylamino)-3-oxoazepan-1-yl]methanoyl]-3-methylbutl)carbamic acid benzyl ester
-
the faster eluting diastereomer C34H46N4O7*0.4H2O; the slower eluting diastereomer C34H46N4O7*0.3H2O
((S)-1-[[(3R,S)-((S)-2-benzyloxycarbonylamino-4-methylpentanoylamino)-3-oxopiperidin-1-yl]methanoyl]-3-methylbutyl)carbamic acid benzyl ester
-
-
((S)-1-[[(3R,S)-((S)-2-benzyloxycarbonylamino-4-methylpentanoylamino)-4-oxopyrrolidin-1-yl]methanoyl]-3-methylbutyl)carbamic acid benzyl ester
-
-
((S)-1-[[(3R,S)-((S)-2-benzyloxycarbonylmethylamino-4-methylpentanoylamino)-4-oxopyrrolidin-1-yl]methanoyl]-3-methylbutyl)carbamic acid benzyl ester
-
-
(1'S)-7-(1-aminoethyl)-2-(2-methoxyphenyl)pyrazolo[1,5-a] pyrimidine hydrochloride
-
(1'S)-7-(1-aminoethyl)-2-(3-trifluoromethylphenyl)pyrazolo-[1,5-a]pyrimidine hydrochloride
-
(1'S)-7-(1-aminoethyl)-2-benzyl-3-phenylpyrazolo[1,5-a]pyrimidine hydrochloride
-
(1'S)-7-(1-aminoethyl)pyrazolo[1,5-a]pyrimidine-3-(N-methylcarboxamide) hydrochloride
-
(1'S)-7-(1-aminoethyl)pyrazolo[1,5-a]pyrimidine-3-carboxylate hydrochloride
-
(11R,12R)-14,14-difluoro-34-(methylsulfanyl)-N-(prop-2-yn-1-yl)-11,12,13,14,15,16-hexahydro[11,21:22,31-terphenyl]-12-carboxamide
-
(1R)-1-benzyl-2-methylpropyl [(1S)-1-[(E)-[(morpholin-4-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
(1R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
(1R,2R)-2-[1-benzyl-5-[4-(methylsulfanyl)phenyl]-1H-1,2,3-triazol-4-yl]-N-(cyanomethyl)-5,5-difluorocyclohexanecarboxamide
(1R,2R)-5,5-dichloro-2-[4-[4-(methanesulfonyl)phenyl]-1-(2,2,2-trifluoroethyl)-1H-pyrrol-3-yl]-N-(prop-2-yn-1-yl)cyclohexane-1-carboxamide
-
(1R,2R)-5,5-dichloro-N-(1-cyanocyclopropyl)-2-[4-[4-(methylsulfonyl)phenyl]-1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-yl]cyclohexanecarboxamide
-
i.e. MK-1256, a nonbasic, nitrile-containing cathepsin K inhibitor, that shows high selectivity for Cat K, 1100fold versus Cat B, L, S, C, H, Z, and V, 110fold versus Cat F
(1R,2R)-5,5-difluoro-2-[4-[4-(methanesulfonyl)phenyl]-1-(2,2,2-trifluoroethyl)-1H-pyrrol-3-yl]-N-(prop-2-yn-1-yl)cyclohexane-1-carboxamide
-
(1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carbonyl)cyclohexane-1-carboxamide
-
(1R,2R)-N-(1-cyanocyclopropyl)-5,5-difluoro-2-[4-[4-(methylsulfonyl)phenyl]-1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-2-(4-[4-[(difluoromethyl)sulfanyl]phenyl]pyridin-3-yl)-5,5-difluorocyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[1-methyl-4-[4-(methylsulfanyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[1-methyl-4-[4-(methylsulfonyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-methyl-4-[4-(methylsulfanyl)phenyl]-1,3-thiazol-5-yl]cyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-[4-(methylsulfanyl)phenyl]pyridin-3-yl]cyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-1-oxidopyridin-4-yl]cyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]pyridin-4-yl]cyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4-[4-(methylsulfonyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[5-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
(1R,2S)-N-(cyanomethyl)-2-[2-[4-(methylsulfanyl)phenyl]ethyl]cyclohexanecarboxamide
-
-
(1S)-1-methyl-2-phenylethyl [(1S)-1-[(E)-[(morpholin-4-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
(1S)-1-[(5,6-dichloro-1H-benzimidazol-1-yl)methyl]-2,2-dimethylpropyl [(1S)-1-methyl-2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamate
-
-
(1S)-1-[(5,6-dichloro-1H-benzimidazol-1-yl)methyl]-2,2-dimethylpropyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-([[(6-fluoropyridin-2-yl)carbonyl]amino]acetyl)pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-methyl-2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[oxo(1H-pyrazol-5-ylamino)acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[[(morpholin-4-ylcarbonyl)amino]acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]methyl)propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([4-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-[(3-pyridin-3-yl-1H-pyrazol-1-yl)methyl]propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-[(3-pyridin-4-yl-1H-pyrazol-1-yl)methyl]propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-[[3-(trifluoromethyl)-1H-pyrazol-1-yl]methyl]propyl [(1S)-1-methyl-2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamate
-
-
(1S)-2,2-dimethyl-1-[[3-(trifluoromethyl)-1H-pyrazol-1-yl]methyl]propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
-
-
(2E,4E)-5-(1-hydroxy-2,6,6-trimethyl-4-oxocyclohex-2-en-1-yl)-3-methylpenta-2,4-dienoic acid
-
(2R)-2-[3'-[2-(4-tert-butylpiperazin-1-yl)-1,3-thiazol-4-yl]biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
-
-
(2R)-3,3-dimethyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)butan-2-yl [(3S)-1,2-dioxo-1-[[(1S)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(2R)-3,3-dimethyl-1-[2-oxo-3-[4-(trifluoromethyl)phenyl]imidazolidin-1-yl]butan-2-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamate
-
-
(2R)-3,3-dimethyl-1-[3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]butan-2-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamate
-
-
(2R)-3,3-dimethyl-1-[4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]butan-2-yl [(3S)-1,2-dioxo-1-(1,3-thiazol-2-ylamino)heptan-3-yl]carbamate
-
-
(2R)-3,3-dimethyl-1-[4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]butan-2-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamate
-
-
(2R)-3,3-dimethyl-1-[4-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]butan-2-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamate
-
-
(2R)-4-fluoro-4-methyl-N-(3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl)-2-((R)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2R)-N-(cyanomethyl)-2-[3'-(2-[[3-(dimethylamino)pyrrolidin-1-yl]methyl]-1,3-thiazol-4-yl)biphenyl-3-yl]-4-methylpentanamide
-
-
(2R)-N-(cyanomethyl)-4-methyl-2-[3'-[2-(piperazin-1-ylmethyl)-1,3-thiazol-4-yl]biphenyl-3-yl]pentanamide
-
-
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methylpiperazin-1-yl)biphenyl-3-yl]pentanamide
-
-
(2R)-N-cyano-4-methyl-2-[4'-(piperazin-1-yl)[1,1'-biphenyl]-3-yl]pentanamide
-
(2S)-1-[5-(4-fluorophenyl)-1,3,4-oxadiazol-2-yl]-3,3-dimethylbutan-2-yl [(3S)-1,2-dioxo-1-[(pyridin-3-ylmethyl)amino]heptan-3-yl]carbamate
-
-
(2S)-1-[5-(4-fluorophenyl)-1,3,4-oxadiazol-2-yl]-3,3-dimethylbutan-2-yl [(3S)-1,2-dioxo-1-[[(1S)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(2S)-2-(biphenyl-2-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
-
-
(2S)-2-(biphenyl-3-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
-
-
(2S)-2-(biphenyl-4-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
-
-
(2S)-3,3-dimethyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)butan-2-yl [(3S)-1,2-dioxo-1-[[(1S)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(2S)-3,3-dimethyl-1-[5-[4-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]butan-2-yl [(3S)-1,2-dioxo-1-[(2-oxo-1,3-oxazolidin-3-yl)amino]heptan-3-yl]carbamate
-
-
(2S)-3-methyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)butan-2-yl [(3S)-1,2-dioxo-1-[[(1S)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(2S)-4,4-dichloro-N-(1-cyanocyclopropyl)-2-([(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]amino)butanamide
-
-
(2S)-4-fluoro-4-methyl-N-(1-(2-(methylsulfonyl)phenyl)-3-oxopiperidin-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-4-fluoro-4-methyl-N-(1-(methylsulfonyl)-3-oxoazepan-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-4-fluoro-4-methyl-N-(1-(methylsulfonyl)-4-oxopyrrolidin-3-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-4-fluoro-4-methyl-N-(3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
racemate
(2S)-4-fluoro-4-methyl-N-(3-oxo-1-(pyridin-2-ylsulfonyl)piperidin-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-4-fluoro-4-methyl-N-(3-oxo-1-phenylpiperidin-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-4-fluoro-4-methyl-N-(3-oxoazepan-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-4-fluoro-4-methyl-N-(4-oxo-1-(pyridin-2-ylsulfonyl)pyrrolidin-3-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-4-fluoro-4-methyl-N-(4-oxopyrrolidin-3-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-N-(1-(benzylsulfonyl)-3-oxoazepan-4-yl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-N-(1-acetyl-4-oxopyrrolidin-3-yl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-N-(1-benzoyl-4-oxopyrrolidin-3-yl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-N-(1-cyanocyclopropyl)-4,4,4-trifluoro-2-([(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]amino)butanamide
-
-
(2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-(3-phenoxyphenoxy)pentanamide
-
-
(2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-(4-phenoxyphenoxy)pentanamide
-
-
(2S,3S)-3-([(1S)-3-methyl-1-[(2-methylpropoxy)methyl]butyl]carbamoyl)oxirane-2-carboxylate
-
through screening, a potent orally active cathepsin K inhibitor named NC-2300 is obtained, which suppresses autoimmune inflammation of the joints as well as osteoclastic bone resorption in an adjuvant-induced arthritis animal model in rats. Computer-assisted simulation of the cathepsin K/NC-2300 complex indicates that NC-2300 blocks the active-site cleft where Cys25 and His162 of cathepsin K form the catalytic site. Pharmacological inhibition of cathepsin K results in defective Toll-like receptor 9 signaling in dendritic cells in response to unmethylated CpG DNA, which in turn leads to an attenuated induction of T helper 17 cells, without affecting the antigen-presenting ability of dendritic cells
(3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetic acid
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
(3S)-1-(1H-indol-6-ylcarbonyl)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-(2,2-dimethylpropoxy)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-(benzylcarbamoyl)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-(benzylsulfonyl)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-(biphenyl-4-ylcarbonyl)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-(dicyclopentylmethoxy)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-(heptan-4-yloxy)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-([(2R)-1-[5-(4-fluorophenyl)-1,3,4-oxadiazol-2-yl]-3,3-dimethylbutan-2-yl]oxy)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(3S)-2-oxopiperidin-3-yl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-([(3S)-1-[(3,5-dimethyl-1,2-oxazol-4-yl)carbonyl]-4,4-dimethylpyrrolidin-3-yl]oxy)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-benzyl-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-tert-butoxy-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[(thiophen-2-ylmethyl)amino]heptan-3-yl]carbamate
-
-
(3S)-1-tert-butoxy-4,4-dimethylpyrrolidin-3-yl [(3S)-1-(ethylamino)-1,2-dioxoheptan-3-yl]carbamate
-
-
(3S)-1-[(1-benzylcyclobutyl)methoxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[(2,4-dimethylpentan-3-yl)oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[(3,3-dimethylbutan-2-yl)oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[[(2R)-3,3-dimethyl-1-[5-[4-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]butan-2-yl]oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamate
-
-
(3S)-1-[[(2R)-3,3-dimethyl-1-[5-[4-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]butan-2-yl]oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1S)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[[(3R)-2,2-dimethyl-6-phenylhexan-3-yl]oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[[(3R)-4,4-dimethyl-1-phenylpentan-3-yl]oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[[(3S)-1-(1-benzothiophen-2-ylcarbonyl)-4,4-dimethylpyrrolidin-3-yl]oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[[(3S)-1-benzoyl-4,4-dimethylpyrrolidin-3-yl]oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[[(3S)-4,4-dimethyl-1-phenylpentan-3-yl]oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[[1-(4-fluorobenzyl)cyclobutyl]methoxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamate
-
-
(3S)-2-oxo-N-[(1R)-1-phenylethyl]-3-[([[1-(2-phenylethyl)cyclobutyl]oxy]acetyl)amino]heptanamide
-
-
(3S)-2-oxo-N-[(1R)-1-phenylethyl]-3-[([[1-(3-phenylpropyl)cyclobutyl]oxy]acetyl)amino]heptanamide
-
-
(3S)-3-([[(2-methyl-1-phenylpropan-2-yl)oxy]acetyl]amino)-2-oxo-N-[(1R)-1-phenylethyl]heptanamide
-
-
(3S)-4,4-dimethyl-1-(1,2-oxazol-5-ylcarbonyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-(4-phenylbutanoyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-(naphthalen-2-ylcarbonyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-(pentan-3-yloxy)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-(phenylacetyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-(phenylcarbamoyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-(phenylsulfonyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-(pyridin-3-ylcarbonyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-[(2,2,4,4-tetramethylpentan-3-yl)oxy]pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-[(2-phenylethyl)carbamoyl]pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-[4-(trifluoromethyl)benzoyl]pyrrolidin-3-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-3-ylamino)heptan-3-yl]carbamate
-
-
(4-[[(2S)-2-([1-[([1,1'-biphenyl]-3-yl)amino]cyclohexane-1-carbonyl]amino)butyl]amino]phenoxy)acetic acid
-
(4R)-N-(1-cyanocyclopropyl)-5,5,5-trifluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
(4S)-N-(1-cyanocyclopropyl)-5,5,5-trifluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
(S)-N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(S,S)-piperidine-4-carboxylic acid [1-[1-(benzoxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([2-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-3-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-4-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(thiophen-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[methyl(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(methylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(phenylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[(1-[4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamido]cyclohexane-1-carbonyl)amino]-L-erythro-hex-2-ulose
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-([[4-([[(dimethylamino)methyl]sulfonyl]amino)phenyl]carbonyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([2-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-fluoro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([4-[(ethylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-(methylsulfamoyl)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-([[4-(1-methylethyl)-1,3-thiazol-2-yl]sulfonyl]amino)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-sulfamoylphenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methyl-1H-imidazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methylethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2,2,2-trifluoroethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2-methylphenyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methylpyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(5-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[4-methyl-N-(thiophen-3-ylcarbonyl)-L-leucyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([4-[(benzylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([4-[(butylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([4-[(cyclopropylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-chloropyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(3-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(4-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(cyclohexylmethyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1-(3-chlorophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
-
-
1-(4-chlorophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
-
-
1-(4-cyanophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
-
-
1-(4-cyclohexylphenoxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
-
1-(4-ethylphenoxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
-
1-(biphenyl-2-ylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
-
1-(biphenyl-3-ylamino)-N-[(1R)-2-[(4-methoxyphenyl)amino]-1-methylethyl]cyclohexanecarboxamide
-
-
1-(biphenyl-3-ylamino)-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]butyl]cyclohexanecarboxamide
-
-
1-(biphenyl-3-ylamino)-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]pentyl]cyclohexanecarboxamide
-
-
1-(biphenyl-3-ylamino)-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]propyl]cyclohexanecarboxamide
-
-
1-(biphenyl-3-ylamino)-N-[(1S)-2-[(4-methoxyphenyl)amino]-1-methylethyl]cyclohexanecarboxamide
-
-
1-(biphenyl-3-ylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
-
1-(biphenyl-3-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
-
1-(biphenyl-4-ylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
-
1-(biphenyl-4-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
-
1-(N-benzyloxycarbonyl-leucyl)-5-(N-Boc-phenylalanylleucyl)carbohydrazide
-
cathepsin K inhibitor
1-(phenoxymethyl)cyclobutyl (3aR,6aS)-6-oxohexahydro-1H-furo[3,2-c]pyrazole-1-carboxylate
-
1-(phenoxymethyl)cyclobutyl (3aS,6aR)-3-oxohexahydro-4H-furo[3,2-b]pyrrole-4-carboxylate
-
1-benzylcyclopentyl [(1S)-1-[(E)-[(2,3-dihydro-1H-indol-1-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
1-benzylcyclopentyl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
1-ethyl-2-[(4-methylpiperazin-1-yl)methyl]-6-[3-(trifluoromethyl)phenyl]-2,3-dihydro-1H-indole-4-carbonitrile
-
1-Isopropyl-2-methylpropyl (1S)-1-cyclohexylmethyl-2,3-dioxo-3-[(thien-2-ylmethyl)-amino]propylcarbamate
-
IC50: 14 nM
1-Isopropyl-2-methylpropyl (1S)-1-isoprpyl-2,3-dioxo-3-[(thien-2-ylmethyl)-amino]propylcarbamate
-
IC50: 47 nM
1-Isopropyl-2-methylpropyl (1S)-1-methyl-2,3-dioxo-3-[(thien-2-ylmethyl)-amino]propylcarbamate
-
IC50: 360 nM
1-Isopropyl-2-methylpropyl (1S)-1-[(isoxazol-3-ylamino)(oxo)acetyl]pentylcarbamate
-
IC50: 5.1 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1,3,4-thiadiazol-2-ylamino)acetyl]pentylcarbamate
-
IC50: 83 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1,3-thiazol-2-ylamino)acetyl]pentylcarbamate
-
IC50: 40 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(isoquinolin-2-ylamino)acetyl]pentylcarbamate
-
IC50: 4.8 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(pyrazin-2-ylamino)acetyl]pentylcarbamate
-
IC50: 52 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(pyridin-2-ylamino)acetyl]pentylcarbamate
-
IC50: 32 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(pyridin-3-ylamino)acetyl]pentylcarbamate
-
IC50: 95 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(quinolin-2-ylamino)acetyl]pentylcarbamate
-
IC50: 250 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-2-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-4-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(3-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(4-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(thien-2-ylmethyl)-amino]acetyl]pentylcarbamate
-
IC50: 9.2 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclohexyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclopentyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-ethyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isopropyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-3-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(3-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.71 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-bromo-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.24 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-cyano-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.91 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-fluoro-1H-indazol-3-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.26 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(3,3-dimethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(cyclopropylmethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-2,3-dioxo--1-phenyl-3-[(thien-2-ylmethyl)-amino]propylcarbamate
-
IC50: 27 nM
1-Isopropyl-2-methylpropyl (1S)-3-methyl-1-[oxo[(thien-2-ylmethyl)-amino]acetyl]butylcarbamate
-
IC50: 24 nM
1-Isopropyl-2-methylpropyl (1S,2S)-2-methyl-1-[oxo[(thien-2-ylmethyl)-amino]acetyl]butylcarbamate
-
IC50: 87 nM
1-Isopropyl-2-methylpropyl 2,3-dioxo-3-[(thien-2-ylmethyl)-amino]propylcarbamate
-
IC50: 0.012 mM
1-methylethyl (2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazinecarboxylate
-
-
1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-(3-methylphenyl)urea
-
-
1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-phenylurea
-
-
1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-[3-(trifluoromethyl)phenyl]urea
-
-
13-methyl-2H,10H-[1,3]benzodioxolo[5,6-c][1,3]dioxolo[4,5-i]phenanthridin-13-ium
-
2-(2,4-dihydroxyphenyl)-5,7-dihydroxy-6-[5-methyl-2-(prop-1-en-2-yl)hex-4-en-1-yl]-2,3-dihydro-4H-1-benzopyran-4-one
-
2-(3-methoxyphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-(3-methylphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-(3-tert-butylphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-(4-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-3-oxoazepan-1-ylsulfonyl)pyridine 1-oxide
-
-
2-(biphenyl-3-yl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-(cyclohexylmethyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-cyano-4-(cyclohexylamino)-N-(4-methoxyphenethyl)-pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylamino)-N-[2-(3-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylamino)-N-[2-(4-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylamino)-N-[2-(4-pyrrolidin-1-ylphenyl)ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylamino)-N-[2-[4-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[3-[2-(1H-imidazol-1-yl)ethoxy]-4-methoxyphenyl]ethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[3-[2-(1H-imidazol-1-yl)ethoxy]phenyl]ethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[4-[(1-methylpiperidin-4-yl)oxy]phenyl]ethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]ethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[4-[2-(1H-imidazol-1-yl)ethoxy]phenyl]ethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-(3-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-(4-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-(4-pyrrolidin-1-ylphenyl)ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-[3-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-[4-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-[(cyclohexylmethyl)(methyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-4-[[(4,4-difluorocyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[[(4,4-dimethylcyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-N-(1-methyl-4-phenylpiperidin-4-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-(4,5-dimethoxybiphenyl-2-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-(4-methoxyphenethyl)-4-(neopentylamino)pyrimidine-5-carboxamide
-
-
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-[(1-methyl-4-phenylpiperidin-4-yl)methyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-[(1R)-2-pyridin-2-yl-1-(pyrrolidin-1-ylmethyl)ethyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-[5-[(1-methylpiperidin-4-yl)oxy]biphenyl-2-yl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cycloheptyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-cycloheptyl-3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-cycloheptyl-4-[2-(dimethylamino)ethyl]-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-cycloheptyl-4-[3-(morpholin-4-yl)propyl]-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-cyclohexyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-cyclopentyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-methyl-1-phenylpropan-2-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
2-methylpropyl [(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamate
-
-
2-phenylethyl (4S)-4-[[(4S)-4-([[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamoyl]oxy)-3,3-dimethylpyrrolidin-1-yl]oxy]-3,3-dimethylpyrrolidine-1-carboxylate
-
-
2-phenylpropan-2-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
2-[3-(hydroxymethyl)phenyl]-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-[[2-cyano-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methyl]-N-cyclohexyl-1,3-dioxo-2,8-diazaspiro[4.5]decane-8-carboxamide
-
-
2-[[2-cyano-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methyl]-N-methyl-1,3-dioxo-2,8-diazaspiro[4.5]decane-8-carboxamide
-
-
3,3'-[(3-carboxy-4-oxocyclohexa-2,5-dien-1-ylidene)methylene]bis(6-hydroxybenzoic acid)
-
3,5-dioxo-2-phenyl-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3,5-dioxo-2-[3-(propan-2-yl)phenyl]-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3,5-dioxo-4-(2-phenylethyl)-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3,5-dioxo-4-phenyl-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3,5-dioxo-4-propyl-2-[4-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3,5-dioxo-4-[2-(piperidin-1-yl)ethyl]-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2-[3-(propan-2-yl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-2-oxopropylcarbamate
-
-
3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxo-N-(phenylsulfonyl)pyrrolidine-1-carboxamide
-
-
3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxo-N-phenylpyrrolidine-1-carboxamide
-
-
3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxamide
-
-
3-(4-([4'-((1-[(cyanomethyl)carbamoyl]cyclohexyl)carbamoyl)biphenyl-4-yl]oxy)piperidin-1-yl)propanoic acid
-
-
3-(4-[[(2S)-2-([[1-(biphenyl-3-ylamino)cyclohexyl]carbonyl]amino)butyl]amino]phenoxy)propanoic acid
-
-
3-benzylpentan-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
3-[(6-deoxy-L-mannopyranosyl)oxy]-5-hydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-en-1-yl)-4-oxo-4H-1-benzopyran-7-yl D-glucopyranoside
-
3-[4-([(2S)-2-[(N-biphenyl-3-yl-L-leucyl)amino]butyl]amino)phenoxy]propanoic acid
-
-
3-[[(2S)-2-[([3-acetyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
3-[[(2S)-2-[[(4-[[(4-aminophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
4'-(4-tert-butylpiperazin-1-yl)-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-4-carboxamide
-
-
4'-(4-tert-butylpiperazin-1-yl)-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]biphenyl-4-carboxamide
-
strong inhibition
4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-fluoro-4-methyl-1-oxopentan-2-yl]amino)-2,2,2-trifluoroethyl][1,1'-biphenyl]-4-sulfonic acid
-
4'-[(1S)-1-([(2S)-1-[(cyanomethyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2,2-trifluoroethyl][1,1'-biphenyl]-4-sulfonic acid
-
4'-[4-(tert-butylamino)piperidin-1-yl]-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-4-carboxamide
-
-
4'-[4-(tert-butylamino)piperidin-1-yl]-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]biphenyl-4-carboxamide
-
strong inhibition
4-(2-[(3R)-3-aminopyrrolidin-1-yl]-1,3-thiazol-4-yl)-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
4-(4-acetylpiperazin-1-yl)-5-amino-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
-
-
4-(dimethylamino)-N-[1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]benzamide
-
-
4-(trifluoromethoxy)-N-(1-[[(1S)-1-([5-[3-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]carbonyl)butyl]carbamoyl]cyclohexyl)benzamide
-
-
4-(trifluoromethoxy)-N-(1-[[(1S)-1-([5-[4-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]carbonyl)butyl]carbamoyl]cyclohexyl)benzamide
-
-
4-benzyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-butyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-cyclopentyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-ethyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-fluoro-N-(3-oxoazepan-4-yl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-(4-oxopyrrolidin-3-yl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-(5-oxo-2-phenylpiperidin-4-yl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-prop-2-yn-1-yl-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
4-fluoro-N-[1-(methylsulfonyl)-3-oxoazepan-4-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[1-(methylsulfonyl)-4-oxopyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]benzamide
-
-
4-fluoro-N-[2-[2-(methylsulfonyl)phenyl]-5-oxopiperidin-4-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[3-oxo-1-(pyridin-2-ylsulfonyl)piperidin-4-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[4-oxo-1-(phenylcarbamoyl)pyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[4-oxo-1-(phenylcarbonyl)pyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[4-oxo-1-(pyridin-2-ylsulfonyl)pyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[4-oxo-1-[(phenylsulfonyl)carbamoyl]pyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-methyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-propyl-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
moderate cathepsin K potency
4-[(2,2-dimethylpropyl)amino]-5-(3-[4-[(4-methoxyphenyl)sulfonyl]piperazin-1-yl]prop-1-yn-1-yl)pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)amino]-5-[3-(pyridin-3-yloxy)prop-1-yn-1-yl]pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)amino]-5-[3-[4-(4-methylpiperazin-1-yl)phenyl]prop-1-yn-1-yl]pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)[4-(1H-1,2,4-triazol-1-ylmethyl)benzyl]amino]pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)[4-(3-piperidin-1-ylprop-1-yn-1-yl)benzyl]amino]pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)[4-[3-(1H-1,2,4-triazol-1-yl)prop-1-yn-1-yl]benzyl]amino]pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)[4-[3-(4-methylpiperazin-1-yl)prop-1-yn-1-yl]benzyl]amino]pyrimidine-2-carbonitrile
-
-
4-[2-(1,4'-bipiperidin-1'-yl)-1,3-thiazol-4-yl]-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
4-[2-(1,4'-bipiperidin-1'-yl)-1,3-thiazol-4-yl]-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
strong inhibition
4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
-
4-[2-(4-methylpiperazin-1-yl)-4,5-dihydro-1,3-thiazol-4-yl]-N-(1-[[(3S,4R)-2-oxo-4-phenoxyazetidin-3-yl]carbamoyl]cyclohexyl)benzamide
-
4-[2-(4-tert-butylpiperazin-1-yl)-1,3-thiazol-4-yl]-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
4-[2-(4-tert-butylpiperazin-1-yl)-1,3-thiazol-4-yl]-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
strong inhibition
4-[2-(dimethylamino)ethyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-[2-[(3R)-3-aminopyrrolidin-1-yl]-1,3-thiazol-4-yl]-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
strong inhibition
4-[3-(dimethylamino)propyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-[3-(morpholin-4-yl)propyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-[3-(pentan-3-ylamino)propyl]-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[3-(piperidin-1-yl)propyl]-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[3-(tert-butylamino)propyl]-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzoic acid
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
4-[[4-[3-(1,4'-bipiperidin-1'-yl)prop-1-yn-1-yl]benzyl](2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
-
-
4-[[4-[3-(4-acetylpiperazin-1-yl)prop-1-yn-1-yl]benzyl](2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-(3-[4-[(3-chloropropyl)sulfonyl]piperazin-1-yl]prop-1-yn-1-yl)-4-[(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-amino-4-(3-hydroxyazetidin-1-yl)-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-amino-4-(bicyclo[2.2.1]hept-2-ylamino)-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-morpholin-4-yl-6-(tetrahydrofuran-3-ylamino)pyrimidine-2-carbonitrile
-
-
5-amino-4-[(1,1-dioxidotetrahydrothiophen-3-yl)amino]-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-amino-4-[(2,2-dimethylpropyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-[(2-methoxyethyl)amino]-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-amino-4-[(2-methylpropyl)amino]-6-[(tetrazolidin-5-ylmethyl)amino]pyrimidine-2-carbonitrile
-
-
5-bromo-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
-
5-bromo-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]thiophene-2-carboxamide
-
moderate inhibition
5-[3-(1,3-dihydro-2H-isoindol-2-yl)prop-1-yn-1-yl]-4-[(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-[3-(3,4-dihydroisoquinolin-2(1H)-yl)prop-1-yn-1-yl]-4-[(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-[3-(4,5-dichloro-1H-imidazol-1-yl)prop-1-yn-1-yl]-4-[(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
-
-
6,8-dihydroxy-3-(3,4,5-trihydroxyphenyl)-2,3-dihydro-1,4-benzodioxin-2-yl 3,4,5-trihydroxybenzoate
-
6-(4-chlorobenzyl)-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-piperidin-1-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(3,3,3-trifluoropropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(3,3-dimethylbutyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(4,4,4-trifluorobutyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(4,4-dimethylpentyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-[2-(piperidin-1-yl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(bromomethyl)-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(cyclohexylamino)-9-[(2S,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-9H-purine-2-carbonitrile
-
-
6-(cyclohexylamino)-9-[2-(4-methylpiperazin-1-yl)ethyl]-9H-purine-2-carbonitrile
-
-
6-benzyl-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-cyano-2-(3-trifluoromethyl-phenyl)-3,5-dioxo-1,2,4-triazine
-
poor catK potency
6-[(1'-acetyl-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[(4,5-dichloro-1H-imidazol-1-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[(5,5-dimethyl-2,4-dioxo-1,3-oxazolidin-3-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[(8-acetyl-1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[(8-benzyl-1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[4-[(diethylamino)methyl]benzyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[4-[3-(diethylamino)propoxy]-3-(trifluoromethyl)phenyl]-1-ethyl-2,3-dihydro-1H-indole-4-carbonitrile
-
6-[[4-(1-acetyl-1,2,3,6-tetrahydropyridin-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
6-[[4-(1-acetylpiperidin-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
6-[[4-(4-acetyl-1,4-diazepan-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-[[4-(4-acetylpiperazin-1-yl)-3-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[8-(2,4-dimethoxyphenyl)-1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl]methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethyl-propyl)-6-(1,3-dioxo-2,8-diaza-spiro[4.5]dec-2-ylmethyl)-7H-pyrrolo[2,3-d] pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-(1H-1,2,3-triazol-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-(1H-imidazol-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(1'-methyl-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(1,3-dioxo-2,8-diazaspiro[4.5]decan-2-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-3-propyl-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-8-propyl-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-[(2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(3-methyl-2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-[(5-fluoro-1'-methyl-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(5-fluoro-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-[(5-methoxy-1'-methyl-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(5-methoxy-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-[(pyridin-4-yloxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[4-(4-methylpiperazin-1-yl)benzyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[4-(morpholin-4-yl)benzyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[[2-oxo-1'-(propan-2-yl)spiro[indole-3,4'-piperidin]-1(2H)-yl]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[[4-(4-fluorophenyl)piperazin-1-yl]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[[8-(morpholin-4-ylacetyl)-1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2-cyclohexylethyl)-6-(4-methoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[(pyridin-2-yloxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[(pyridin-2-ylsulfanyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[[methyl(phenyl)amino]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
benzofuran-2-carboxylic acid [(S)-3-methyl-1-[2-oxo-3-(pyridin-2-ylsulfonylamino)propylcarbamoyl]butyl]amide
-
-
benzyl (2S)-2-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)-4-methylpentanoate
-
-
benzyl (2S,3R)-1-(cyanomethylamino)-3-hydroxy-1-oxobutan-2-ylcarbamate
-
weak inhibition
benzyl (2S,3S)-1-(cyanomethylamino)-3-methyl-1-oxopentan-2-ylcarbamate
-
weak inhibition
benzyl [(1S)-1-[(cyanomethyl)carbamoyl]-2,2-dimethylpropyl]carbamate
-
weak inhibition
benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate
benzyl [(5S,13S)-11,15-dimethyl-5-(2-methylpropyl)-3,6,9,12-tetraoxo-1-phenyl-2-oxa-4,7,11-triazahexadecan-13-yl]carbamate
-
biphenyl-4-yl (4S)-4-([[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamoyl]oxy)-3,3-dimethylpyrrolidine-1-carboxylate
-
-
biphenyl-4-ylmethyl (4S)-4-([[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamoyl]oxy)-3,3-dimethylpyrrolidine-1-carboxylate
-
-
Boc-I
-
lysosomotropic, water-soluble polymer selective catK inhibitor. Inhibition of catK greatly reduces melanoma cell invasion through Matrigel basement membrane matrix and increases detection of internalized collagen
cystatin
-
different types, expression analysis in various cell types isolated from normal and neoplastic breast tissue, overview
-
dibenzyl [(2-oxopropane-1,3-diyl)bis[azanediyl[(2S)-4-methyl-1-oxopentane-1,2-diyl]]]biscarbamate
-
dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate
ethyl (4S)-4-[(4-fluoro-N-[2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucyl)amino]-3-oxopiperidine-1-carboxylate
-
ethyl 3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxylate
-
-
ethyl 3-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-4-oxopyrrolidine-1-carboxylate
-
-
ethyl 4-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-3-oxoazepane-1-carboxylate
-
-
ethyl 4-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-3-oxopiperidine-1-carboxylate
-
-
ethyl 4-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-3-oxoazepane-1-carboxylate
-
-
ethyl 4-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-5-oxopiperidine-2-carboxylate
-
-
Ethyl 5-[((3S)-3[[(isopropyl-2-methylpropoxy)carbonyl]amide]-2-oxoheptanoyl)amino]-1H-pyrazole-4-carboxylate
-
IC50: 1.7 nM
ethyl N-[[(2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazino]carbonyl]-b-alaninate
-
-
ethyl N-[[(2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazino]carbonyl]glycinate
-
-
H-kininogen
-
natural inhibitor of cathepsin K, reversible, tight-binding competitive inhibitor
-
kushennol F
shows inhibitory effects on the bone resorption process related to cathepsin K
L-13006235
-
shows no selectivity in cell-based assays over cathepsins B, L, and S
L-kininogen
-
natural inhibitor of cathepsin K, reversible, tight-binding competitive inhibitor
-
methyl (3S)-3-[(4-fluoro-N-[2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucyl)amino]-4-oxopyrrolidine-1-carboxylate
-
methyl 3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxylate
-
-
methyl 3-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-4-oxopyrrolidine-1-carboxylate
-
-
methyl 4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-fluoro-4-methyl-1-oxopentan-2-yl]amino)-2,2-difluoroethyl]biphenyl-4-sulfinate
-
-
methyl 4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2,2-trifluoroethyl]biphenyl-4-sulfinate
-
-
methyl 4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2-difluoroethyl]biphenyl-4-sulfinate
-
-
methyl 4'-[(1S)-1-([(2S)-1-[(cyanomethyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2-difluoroethyl]biphenyl-4-sulfinate
-
-
methyl 5-hydroxy-7,12-dioxo-7,12-dihydrodinaphtho[1,2-b:2',3'-d]furan-6-carboxylate
-
methyl 5-hydroxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
-
furanquinone from Paulownia tomentosa stem
methyl N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-methioninate
-
-
methyl [[(2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazino]carbonyl]carbamate
-
-
mPEG-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
conjugate
N'-cyano-N,N',4-trimethyl-2-([11,21:24,31-terphenyl]-14-yl)pentanehydrazide
-
N-((S)-4-methyl-1-oxo-1-((S)-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-ylamino)pentan-2-yl)benzofuran-2-carboxamide
-
-
N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
N-(1-acetyl-4-oxopyrrolidin-3-yl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-carbamoyl-4-oxopyrrolidin-3-yl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-cyano-1-methylethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-cyano-2-phenylethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-4,4-difluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-norvalinamide
-
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(1-hydroxycyclopropyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(1-hydroxycyclopropyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(2-hydroxypropan-2-yl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(2-hydroxypropan-2-yl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4-(4-methyl-4,5-dihydro-1,3-thiazol-2-yl)phenyl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4-(quinolin-6-yl)phenyl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4-[5-(1-hydroxycyclopropyl)pyridin-2-yl]phenyl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4-[6-(methylsulfonyl)pyridin-3-yl]phenyl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1R)-2,2-difluoro-1-hydroxyethyl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1R)-2,2-difluoro-1-hydroxyethyl][1,1'-biphenyl]-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
-
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1S)-2,2-difluoro-1-hydroxyethyl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1S)-2,2-difluoro-1-hydroxyethyl][1,1'-biphenyl]-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
-
N-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(2,2,2-trifluoro-1-hydroxyethyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-N2-[(1S)-2,2-difluoro-1-[4'-(2,2,2-trifluoro-1-hydroxyethyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-ethynylcyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-2-pyridin-4-yl-1,3-thiazole-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-(4-fluoropiperidin-4-yl)biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-(dimethylamino)biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-(piperazin-1-ylsulfonyl)biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-([(2S)-1-methylpyrrolidin-2-yl]methoxy)biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-([1-(2-hydroxyethyl)piperidin-4-yl]oxy)biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-([4-(2,2,2-trifluoroethyl)piperazin-1-yl]sulfonyl)biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-isoxazol-5-ylbiphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-piperazin-1-ylbiphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-[(1-methylpiperidin-3-yl)oxy]biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-[(1-methylpiperidin-4-yl)oxy]biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-[methyl(1-methylpyrrolidin-3-yl)amino]biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-(4-[(1-methylethyl)amino]piperidin-1-yl)-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-(4-[methyl(1-methylethyl)amino]piperidin-1-yl)-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-morpholin-4-yl-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[(4-methylpiperazin-1-yl)amino]-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[(4-methylpiperazin-1-yl)methyl]-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[3-(dimethylamino)pyrrolidin-1-yl]-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[4-(2-methoxyethyl)piperazin-1-yl]-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[4-(tetrahydro-2H-pyran-4-yl)piperazin-1-yl]-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(4-methylpiperazin-1-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(4-propylpiperazin-1-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[(4-methylpiperazin-1-yl)carbonyl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[(4-methylpiperazin-1-yl)sulfonyl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(1,4-dimethylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(1-methylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(4-morpholin-4-ylpiperidin-1-yl)-1,3-thiazol-4-yl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(morpholin-4-ylmethyl)-1,3-thiazol-4-yl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(piperidin-4-yloxy)-1,3-thiazol-4-yl]benzamide
-
-
N-(1-[[(1S)-1-[[5-(1-methylethyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamoyl]cyclohexyl)-4-(trifluoromethoxy)benzamide
-
-
N-(1-[[(1S)-1-[[5-(3-methoxyphenyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamoyl]cyclohexyl)-4-(trifluoromethoxy)benzamide
-
-
N-(1-[[(1S)-1-[[5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamoyl]cyclohexyl)-4-(trifluoromethoxy)benzamide
-
-
N-(2,3-dichlorophenyl)triazolyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
IC50: 9 nM
N-(2-chlorophenyl)triazolyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
IC50: 6 nM
N-(3-bromoprop-2-yn-1-yl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-(3-[[(3R)-3-([1,1'-biphenyl]-3-yl)-5-methylhex-1-en-2-yl]amino]-2-oxopropyl)-4-phenoxybenzene-1-sulfonamide
-
N-(4-benzyl-1-methylpiperidin-4-yl)-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-(4-chlorophenyl)-2-methylalanyl-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-L-leucinamide
-
IC50 is below 1 nM
N-(4-methyl-1-oxo-1-[[3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]amino]pentan-2-yl)-1-benzofuran-2-carboxamide
-
-
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)propanamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
N-(5-isopropyl)pyridine-2-carboxyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
IC50: less than 3 nM
N-(cyanomethyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-(cyanomethyl)-4-methyl-2-[3'-(2-piperazin-1-yl-1,3-thiazol-4-yl)biphenyl-3-yl]pentanamide
-
-
N-(cyanomethyl)-4-methyl-2-[3'-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]biphenyl-3-yl]pentanamide
-
-
N-(cyanomethyl)-4-methyl-2-[4'-(2-piperazin-1-yl-1,3-thiazol-4-yl)biphenyl-3-yl]pentanamide
-
-
N-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(piperazin-1-yl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-4-benzyloxybenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
IC50: 6 nM
N-4-isopropylbenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
IC50: less than 3 nM
N-4-propylbenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
IC50: less than 3 nM
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)oxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-benzyl-2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-benzyl-3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxamide
-
-
N-but-3-yn-2-yl-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-N2-(piperazin-1-ylcarbonyl)-D-leucinamide
-
i.e. APC3328
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylpropyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[(2-methyl-1H-imidazol-1-yl)acetyl]-L-leucinamide
-
IC50: 190 nM
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[(4-phenylpiperidin-1-yl)acetyl]-L-leucinamide
-
IC50: 84 nM
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[(4-pyridin-4-ylpiperazin-1-yl)acetyl]-L-leucinamide
-
IC50: 9 nM
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[(5-methyl-1H-imidazol-4-yl)acetyl]-L-leucinamide
-
IC50: 24 nM
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[2-(4-chlorophenoxy)-2-methylpropanoyl]-L-leucinamide
-
IC50 is below 1 nM
N-[(1S)-1-((3-hydroxy-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl)carbamoyl)-3-methylbutyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
-
-
N-[(1S)-1-([(1R)-2-(benzyloxy)-1-cyanoethyl]carbamoyl)-3-methylbutyl]-1-methyl-1H-indole-2-carboxamide
-
IC50 is below 1 nM
N-[(1S)-1-([(1R)-2-(benzyloxy)-1-cyanoethyl]carbamoyl)-3-methylbutyl]-1H-indole-2-carboxamide
-
IC50: 430 nM
N-[(1S)-1-([1-(2-hydroxy-2,3-dihydro-1,4-benzodioxin-2-yl)ethenyl]carbamoyl)-3-methylbutyl]-1-benzofuran-2-carboxamide
-
-
N-[(1S)-1-([3-(2-hydroxyphenoxy)-1-methylidene-2-oxopropyl]carbamoyl)-3-methylbutyl]-1-benzofuran-2-carboxamide
-
-
N-[(1S)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-[(1S)-1-carbamoyl-3-(methylsulfonyl)propyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[(1S)-1-carbamoyl-3-phenylpropyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[(1S)-1-cyano-2-phenylethyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[(1S)-1-cyano-3-(methylsulfanyl)propyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[(1S)-1-cyanoethyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
N-[(1S)-1-cyclohexyl-3-[(2Z)-2-[(4R)-3,4-dimethyl-1,3-thiazolidin-2-ylidene]hydrazinyl]-2,3-dioxopropyl]cycloheptanecarboxamide
-
N-[(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]-2-phenylacetamide
-
-
N-[(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]-3-phenylpropanamide
-
-
N-[(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]-N2-(2,2,2-trifluoroethyl)-L-leucinamide
-
-
N-[(1S)-1-[2-(methylsulfanyl)ethyl]-2-oxopropyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-3-(methylsulfonyl)-L-alaninamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-alaninamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-methioninamide
-
excellent selectivity against the cathepsins B, L and S
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-methionine
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-phenylalaninamide
-
excellent selectivity against the cathepsins B, L and S
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N,N-dimethyl-L-methioninamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-(2,2,2-trifluoroethyl)-L-methioninamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-(methylsulfonyl)-L-methioninamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-benzyl-L-methioninamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-methyl-L-methioninamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-S-methyl-L-cysteinamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucylglycinamide
-
-
N-[(1S)-3-methyl-1-(((4R)-3-oxo-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl)carbamoyl)butyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
-
-
N-[(1S)-3-methyl-1-([(1S)-1-methyl-2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamoyl)butyl]-1-benzofuran-2-carboxamide
-
-
N-[(1S)-3-methyl-1-([(4S)-3-oxo-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl]carbamoyl)butyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
N-[(1S)-3-methyl-1-[[3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]carbamoyl]butyl]-1-benzofuran-2-carboxamide
-
-
N-[(2S)-1-[4-(benzyloxy)anilino]butan-2-yl]-N2-(morpholine-4-carbonyl)-L-leucinamide
-
N-[(2S)-1-[4-(morpholin-4-yl)anilino]butan-2-yl]-N2-[(1S)-2,2,2-trifluoro-1-(4-hydroxyphenyl)ethyl]-L-leucinamide
-
N-[(2S)-1-[[(2R,4S)-2,4-dimethyl-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]amino]-4-methyl-1-oxopentan-2-yl]-1-benzofuran-2-carboxamide
-
-
N-[(2S)-1-[[(4S,5S)-4,5-dimethyl-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]amino]-4-methyl-1-oxopentan-2-yl]-1-benzofuran-2-carboxamide
-
-
N-[(2S)-4-methyl-1-([2-[4-(2-methylpropoxy)anilino]ethyl]amino)-1-oxopentan-2-yl]-2,3-dihydro-1-benzofuran-2-carboxamide
-
N-[(2S)-4-methyl-1-oxo-1-[(3aS,6aR)-3-oxohexahydro-4H-furo[3,2-b]pyrrol-4-yl]pentan-2-yl]-4-(4-methylpiperazin-1-yl)benzamide
-
N-[(2S)-4-methyl-1-oxo-1-[(3aS,7aR)-3-oxohexahydrofuro[3,2-b]pyridin-4(2H)-yl]pentan-2-yl]-4-(4-methylpiperazin-1-yl)benzamide
-
N-[(2S)-4-methyl-1-oxo-1-[[(4R)-3-oxo-1-(pyridine-2-sulfonyl)azepan-4-yl]amino]pentan-2-yl]-2,3-dihydro-1-benzofuran-2-carboxamide
-
N-[(2S)-4-methyl-1-[(3aS,6S,6aR)-6-methyl-3-oxohexahydro-4H-furo[3,2-b]pyrrol-4-yl]-1-oxopentan-2-yl]-4-[2-(1-methylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
-
N-[(2S)-4-methyl-1-[[(4S,7R)-7-methyl-3-oxo-1-(pyridine-2-sulfonyl)azepan-4-yl]amino]-1-oxopentan-2-yl]-2,3-dihydro-1-benzofuran-2-carboxamide
-
N-[(4S)-3-oxo-1-(pyridine-2-sulfonyl)azepan-4-yl]-N2-[2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-[1-(benzylcarbamoyl)-4-oxopyrrolidin-3-yl]-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[1-(benzylsulfonyl)-3-oxoazepan-4-yl]-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[1-([(1S)-1-[(5-ethyl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
N-[1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
N-[1-([(1S)-1-[(5-methoxy-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
N-[1-([(1S)-1-[(5-phenyl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
N-[1-([(1S)-1-[(5-tert-butyl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
N-[1-([(1S)-1-[(5-thiophen-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-2-pyridin-4-yl-1,3-thiazole-4-carboxamide
-
moderate inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-(4-fluoropiperidin-4-yl)biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-(dimethylamino)biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-(piperazin-1-ylsulfonyl)biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-isoxazol-5-ylbiphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-piperazin-1-ylbiphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[(1-methylpiperidin-3-yl)oxy]biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[(1-methylpiperidin-4-yl)oxy]biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[methyl(1-methylpyrrolidin-3-yl)amino]biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[[(2S)-1-methylpyrrolidin-2-yl]methoxy]biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[[1-(2-hydroxyethyl)piperidin-4-yl]oxy]biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[[1-(2-methoxyethyl)piperidin-4-yl]oxy]biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[[4-(2,2,2-trifluoroethyl)piperazin-1-yl]sulfonyl]biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(2-morpholin-4-yl-1,3-thiazol-4-yl)benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(2-[4-[(1-methylethyl)amino]piperidin-1-yl]-1,3-thiazol-4-yl)benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(2-[4-[methyl(1-methylethyl)amino]piperidin-1-yl]-1,3-thiazol-4-yl)benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(4-methylpiperazin-1-yl)benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-morpholin-4-ylbenzamide
-
moderate inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[(4-methylpiperazin-1-yl)carbonyl]benzamide
-
moderate inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[(4-methylpiperazin-1-yl)sulfonyl]benzamide
-
moderate inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(1-methylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(4-morpholin-4-ylpiperidin-1-yl)-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(morpholin-4-ylmethyl)-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(piperidin-4-yloxy)-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-[(4-methylpiperazin-1-yl)methyl]-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-[3-(dimethylamino)pyrrolidin-1-yl]-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-[4-(tetrahydro-2H-pyran-4-yl)piperazin-1-yl]-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-[methyl(4-methylpiperazin-1-yl)amino]-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]biphenyl-3-carboxamide
-
moderate inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]biphenyl-4-carboxamide
-
moderate inhibition
N-[2-[(4-methoxyphenyl)amino]ethyl]-1-[4-(1-methylethyl)phenoxy]cyclohexanecarboxamide
-
-
N-[4-methyl-1-oxo-1-([2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]amino)pentan-2-yl]-1-benzofuran-2-carboxamide
-
-
N-[cyano(dicyclobutyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[cyano(dicyclopropyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[cyano(phenyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N2-(morpholin-4-ylcarbonyl)-N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-leucinamide
-
-
N2-biphenyl-3-yl-N-[(1S)-1-[([4-[2-(1H-tetrazol-5-yl)ethoxy]phenyl]amino)methyl]propyl]-L-leucinamide
-
-
N2-biphenyl-3-yl-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]propyl]-L-leucinamide
-
-
N2-biphenyl-3-yl-N-[(1S)-2-[(4-methoxyphenyl)amino]-1-methylethyl]-L-leucinamide
-
-
N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)-2'-fluorobiphenyl-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
-
N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)-2'-fluorobiphenyl-4-yl]-2,2-difluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
-
N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)biphenyl-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
-
N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)[1,1'-biphenyl]-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
N2-[(1S)-1-[4'-(2-amino-2-oxoethyl)[1,1'-biphenyl]-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
N2-[(1S)-1-[4'-[(2S)-1-amino-1-oxopropan-2-yl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
-
N2-[(1S)-1-[4-[5-(1-carbamoylcyclopropyl)pyridin-2-yl]phenyl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
-
N2-[(benzyloxy)carbonyl]-N-((1S)-1-cyano-2-[4-(trifluoromethyl)phenyl]ethyl)-L-leucinamide
-
IC50: 43 nM
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-4-methyl-L-leucinamide
-
moderate inhibition
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-5,5,5-trifluoroleucinamide
-
moderate inhibition
N2-[(benzyloxy)carbonyl]-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-L-leucinamide
-
IC50: 9 nM
N2-[(benzyloxy)carbonyl]-N-[(1R)-2-tert-butoxy-1-cyanoethyl]-L-leucinamide
-
IC50: 240 nM
N2-[(benzyloxy)carbonyl]-N-[(1S)-1-cyano-2-(3-methylphenyl)ethyl]-L-leucinamide
-
IC50: 120 nM
N2-[(benzyloxy)carbonyl]-N-[(1S)-1-cyano-2-(4-methoxyphenyl)ethyl]-L-leucinamide
-
IC50: 63 nM
N2-[(benzyloxy)carbonyl]-N-[(1S)-1-cyano-2-(4-methylphenyl)ethyl]-L-leucinamide
-
IC50: 48 nM
N2-[(benzyloxy)carbonyl]-N-[(1S)-2-(4-tert-butoxyphenyl)-1-cyanoethyl]-L-leucinamide
-
IC50: 398 nM
N2-[(benzyloxy)carbonyl]-N-[2-oxo-3-[(4-phenoxybenzene-1-sulfonyl)amino]propyl]-L-leucinamide
-
Nalpha-3-chlorobenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
less efficient than Nalpha-benzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
Nalpha-3-methoxybenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
less efficient than Nalpha-benzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
Nalpha-3-methylbenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
-
Nalpha-4-chlorobenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
-
Nalpha-4-methoxybenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
IC50: 64 nM
Nalpha-4-methylbenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
-
Nalpha-benzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
IC50: 470 nM
naphthalen-2-yl (4S)-4-([[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamoyl]oxy)-3,3-dimethylpyrrolidine-1-carboxylate
-
-
odanacatib 1
-
i.e. MK-0822, a reversible, non-basic, potent and selective Cat K inhibitor. The nitrile forms a hydrogen bond-stabilized thioimidate intermediate with Cys25. The leucine moiety interacts with the hydrophobic S2 subsite and the biphenyl moiety with the S3 subsite, and the hydrogen bond of the trifluroethylamine amide isostere interact with Gly66. Furthermore, odanacatib does not interact with the prime side of Cat K, binding structure, overview
phenyl (4S)-4-([[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamoyl]oxy)-3,3-dimethylpyrrolidine-1-carboxylate
-
-
PHPMA-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
conjugate
PHPMA-GG-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
conjugate
piperidin-2-yl-[2-(trifluoromethyl)-6-[4-(trifluoromethyl)phenyl]pyridin-4-yl] methanol
-
-
piperidine-4-carboxylic acid [3-methyl-1[1-(1-oxa-3-aza-cyclopenta[a]naphthalene-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
piperidine-4-carboxylic acid [3-methyl-1[1-(naphtho[1,2-d]oxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
quinoline-2-carboxylic acid [(S)-1-((3R,S)-4-oxotetrahydrofuran-3ylcarbamoyl)-3-methylbutyl]amide
-
-
S-(1-methylethyl) (2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazinecarbothioate
-
-
SM934-testosterone
inhibits proliferation and metastasis ability of breast cancer cells via inhibiting the expression of cathepsin K followed by the inhibition of Bcl-xL
sodium (2S,3S)-3-[[(2S)-4-methyl-1-(2-methylpropoxy)pentan-2-yl]amino]oxirane-2-carboxylate
-
sophoraflavanone G
shows inhibitory effects on the bone resorption process related to cathepsin K
Stefin B
-
natural inhibitor of cathepsin K, reversible, tight-binding competitive inhibitor
-
STPHPMA-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
conjugate
tert-butyl ([1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]carbamoyl)carbamate
-
-
tert-butyl 3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxylate
-
-
tert-butyl 3-(4-[[(2S)-2-([[1-(biphenyl-3-ylamino)cyclohexyl]carbonyl]amino)butyl]amino]phenoxy)propanoate
-
-
tert-butyl 3-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-4-oxopyrrolidine-1-carboxylate
-
-
tert-butyl 3-[4-([(2S)-2-[(N-biphenyl-3-yl-L-leucyl)amino]butyl]amino)phenoxy]propanoate
-
-
tert-butyl [(1S)-1-([5-[4-(dimethylamino)phenyl]-1,3,4-oxadiazol-2-yl]carbonyl)butyl]carbamate
-
-
tert-butyl [(1S)-1-[(5-thiophen-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-(4,5-dihydro-1,3-thiazol-2-ylhydrazono)methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(2,3-dihydro-1H-indol-1-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(3,4-dihydroisoquinolin-2(1H)-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(3,4-dihydroquinolin-1(2H)-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(3-methylbutanoyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(diethylcarbamoyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(dimethylcarbamoyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(dimethylsulfamoyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(morpholin-4-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(piperidin-1-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(pyrrolidin-1-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(tert-butylcarbamoyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[methyl[(2-phenylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[methyl[methyl(2-phenylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[[(1-methylethyl)carbamothioyl]hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[[(1-methylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[[(2-phenylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[[(morpholin-4-ylcarbonyl)oxy]imino]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[[methyl(2-phenylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[[5-(1-methylethyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamate
-
-
tert-butyl [(1S)-1-[[5-(2-methoxyphenyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamate
-
-
tert-butyl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
tert-butyl [(3S)-1,2-dioxo-1-[[(1S)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
tert-butyl [1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]carbamate
-
-
VEL-0230
highly selective inhibitor of CatK that significantly decreases bone resorption and increases bone formation biomarkers
[(S)-1-((3R,S)-1-acetyl-4-oxopyrrolidin-3-ylcarbamoyl)-3-methylbutyl]carbamic acid benzyl ester
-
-
[(S)-1-((3R,S)-4-oxotetrahydrofuran-3-ylcarbamoyl)-3-methylbutyl]carbamic acid benzyl ester
-
-
[(S)-1-((4R,S)-3-oxotetrahydropyran-4-ylcarbamoyl)-3-methylbutyl]carbamic acid benzyl ester
-
-
[1-(2-cyano-tetrahydro-pyridazine-1-carbonyl)-2-methyl-propyl]-carbamic acid benzyl ester
-
inhibits the bone resorptive activity of mature osteoclasts, structure and interaction pattern with cathepsin K, overview
(1R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
-
-
(1R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
-
-
(1R,2R)-2-[1-benzyl-5-[4-(methylsulfanyl)phenyl]-1H-1,2,3-triazol-4-yl]-N-(cyanomethyl)-5,5-difluorocyclohexanecarboxamide
-
-
(1R,2R)-2-[1-benzyl-5-[4-(methylsulfanyl)phenyl]-1H-1,2,3-triazol-4-yl]-N-(cyanomethyl)-5,5-difluorocyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-2-(4-[4-[(difluoromethyl)sulfanyl]phenyl]pyridin-3-yl)-5,5-difluorocyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-2-(4-[4-[(difluoromethyl)sulfanyl]phenyl]pyridin-3-yl)-5,5-difluorocyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[1-methyl-4-[4-(methylsulfanyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[1-methyl-4-[4-(methylsulfanyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-methyl-4-[4-(methylsulfanyl)phenyl]-1,3-thiazol-5-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-methyl-4-[4-(methylsulfanyl)phenyl]-1,3-thiazol-5-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-[4-(methylsulfanyl)phenyl]pyridin-3-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-[4-(methylsulfanyl)phenyl]pyridin-3-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-1-oxidopyridin-4-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-1-oxidopyridin-4-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]pyridin-4-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]pyridin-4-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[5-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[5-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
-
-
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)-[1,1'-biphenyl]-3-yl]pentanamide
-
IC 50: 3 nM, reversible inhibition
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)-[1,1'-biphenyl]-3-yl]pentanamide
-
-
(S,S)-piperidine-4-carboxylic acid [1-[1-(benzoxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
-
(S,S)-piperidine-4-carboxylic acid [1-[1-(benzoxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
-
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1H-pyrazol-5-ylamino)acetyl]pentylcarbamate
-
IC50: 0.77 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1H-pyrazol-5-ylamino)acetyl]pentylcarbamate
-
IC50: 13 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
-
IC50: 15 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
-
IC50: 790 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-2-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
-
IC50: 62 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-2-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
-
IC50: 0.0012 mM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-4-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
-
IC50: 25 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-4-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
-
IC50: 470 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(3-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
-
IC50: 0.65 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(3-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
-
IC50: 12 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(4-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
-
IC50: 0.21 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(4-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
-
IC50: 1.8 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 15 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.0011 mM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclohexyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 22 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclohexyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.0012 mM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclopentyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 20 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclopentyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.0011 mM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-ethyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 26 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-ethyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.0015 mM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 39 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.0027 mM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isopropyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 17 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isopropyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.001 mM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-3-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.41 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-3-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 11 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 32 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.0017 mM
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.47 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 5.5 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(3,3-dimethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
-
IC50: 62 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(3,3-dimethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.0016 mM
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(cyclopropylmethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
-
IC50: 27 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(cyclopropylmethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.0017 mM
6-(4-chlorobenzyl)-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(2-cyclooctylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cyclooctylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-[2-(3-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-[2-(3-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethyl-propyl)-6-(1,3-dioxo-2,8-diaza-spiro[4.5]dec-2-ylmethyl)-7H-pyrrolo[2,3-d] pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethyl-propyl)-6-(1,3-dioxo-2,8-diaza-spiro[4.5]dec-2-ylmethyl)-7H-pyrrolo[2,3-d] pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-3-propyl-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-3-propyl-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-8-propyl-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-8-propyl-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(3-methyl-2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(3-methyl-2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(5-fluoro-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(5-fluoro-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(5-methoxy-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(5-methoxy-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
balicatib
-
shows no selectivity in cell-based assays over cathepsins B, L, and S
balicatib
-
potent human cathepsin K inhibitor with a high selectivity against human cathepsins B, L and S (> 4800fold, > 500fold and > 65000fold, respectively)
benzyl [(1S)-2-[(cyanomethyl)amino]-1-(naphthalen-2-ylmethyl)-2-oxoethyl]carbamate
-
-
benzyl [(1S)-2-[(cyanomethyl)amino]-1-(naphthalen-2-ylmethyl)-2-oxoethyl]carbamate
-
weak inhibition
benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate
-
shows any degree of Cat K selectivity (10fold vs. Cat L and F)
benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate
-
-
benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate
-
-
BML-244
-
has moderate selectivity (more than 30fold), but is a relatively weak inhibitor of human Cat K
cystatin C
-
natural inhibitor of cathepsin K, reversible, tight-binding competitive inhibitor
-
dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate
-
-
dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate
-
-
dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate
-
-
E-64
i.e. L-3-carboxy-trans-2,3-epoxypropionylleucylamido-(4-guanidino)butane
E-64
-
i.e. epoxysuccinyl-L-leucylamido-{4-guanidino} butane, nonspecific inhibitor
E64
-
i.e. L-3-carboxy-trans-2,3-epoxypropionyl-leucylamido-(4-guanidino)butane, inhibitor-enzyme complex structure 9in presence of different chondroitin 4-sulfate fractions, overview
L-006235
-
shows no selectivity in cell-based assays over cathepsins B, L, and S
L-006235
-
shows no selectivity in cell-based assays over cathepsins B, L, and S
L-006235
-
shows no selectivity in cell-based assays over cathepsins B, L, and S
L-006235
-
shows no selectivity in cell-based assays over cathepsins B, L, and S
L-006235
-
shows no selectivity in cell-based assays over cathepsins B, L, and S
L-873724
-
highly selective for cathespin K over other cathepsins, metabolization, overview
L-873724
-
high degree of potency and selectivity (more than 100fold) for purified human Cat K
L-873724
-
has a greater than 800fold selectivity over other cysteine cathepsins
L-873724
-
the neutral Cat K inhibitor suppresses biochemical markers of bone resorption in vivo, highly selective for cathespin K over other cathepsins, metabolization, overview
L-873724
-
highly selective for cathespin K over other cathepsins, metabolization, overview
Mu-Leu-Hph-fluoromethylketone
-
highly potent versus Cat K, but is essentially non-selective versus all human cathepsins
N'-cyano-N,N',4-trimethyl-2-(4'-(methylsulfonyl)-[1,1'-biphenyl]-3-yl)pentanehydrazide
racemic
N'-cyano-N,N',4-trimethyl-2-(4'-(methylsulfonyl)-[1,1'-biphenyl]-3-yl)pentanehydrazide
racemic
N'-cyano-N,N',4-trimethyl-2-(4'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)pentanehydrazide
racemic
N'-cyano-N,N',4-trimethyl-2-(4'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)pentanehydrazide
racemic
N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
-
i.e. L-006235 or CRA-013788/L
N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
-
i.e. L-006235 or CRA-013788/L
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1R)-2,2-difluoro-1-hydroxyethyl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1R)-2,2-difluoro-1-hydroxyethyl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
-
MIV-701
N-[(1S)-1-cyanoethyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[(1S)-1-cyanoethyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[(1S)-3-methyl-1-([(4S)-3-oxo-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl]carbamoyl)butyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
-
-
N-[(1S)-3-methyl-1-([(4S)-3-oxo-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl]carbamoyl)butyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
-
-
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(4-propylpiperazin-1-yl)benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(4-propylpiperazin-1-yl)benzamide
-
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
-
NSC13345
i.e. 2-[(2-carbamoylsulfanylacetyl)-amino]benzoic acid, good selectivity for cathepsin K over related enzymes
odanacatib
-
i.e. MK-0822, a selective cathepsin K inhibitor, pharmacokinetics of odanacatib
odanacatib
-
i.e. MK-0822, development of an enantioselective method for synthesis of the potent cathepsin K inhibitor, via triflate displacement of an alpha-trifluoromethylbenzyl triflate, overview. The key step involves the novel stereospecific SN2 triflate displacement of a chiral alpha-trifluoromethylbenzyl triflate with (S)-gamma-fluoroleucine ethyl ester to generate the required alpha-trifluoromethylbenzyl amino stereocenter
odanacatib
-
i.e. MK-0822, a selective cathepsin K inhibitor, pharmacokinetics of odanacatib
odanacatib
-
i.e. MK-0822, a selective cathepsin K inhibitor, pharmacokinetics of odanacatib
piperidine-4-carboxylic acid [3-methyl-1[1-(1-oxa-3-aza-cyclopenta[a]naphthalene-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
-
-
piperidine-4-carboxylic acid [3-methyl-1[1-(1-oxa-3-aza-cyclopenta[a]naphthalene-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
-
-
piperidine-4-carboxylic acid [3-methyl-1[1-(naphtho[1,2-d]oxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
-
-
piperidine-4-carboxylic acid [3-methyl-1[1-(naphtho[1,2-d]oxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
-
-
relacatib
-
highly potent versus human Cat K, but lacks selectivity versus Cat L, S, and F
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
i.e. E-64
additional information
-
not inhibitory are pepstatin, phenylmethylsulfonylfluoride, EDTA, 1,10-phenanthroline
-
additional information
-
physiological inhibitors of osteoclast differentiation and activation, such as osteoprotegerin, interleukin-6, INF-gamma, can also directly suppress cathepsin K expression
-
additional information
-
structure-based design of diverse pyrimidine-based scaffolds for inhibitor design
-
additional information
-
inhibitory activities of N-cyano-tetrahydro-pyridazine derivatives, docking studies, overview
-
additional information
-
inhibitor development and structure-activity relationships, overview
-
additional information
-
construction of a three-dimensional pharmacophore model for cathepsin K inhibitor screening and development using the enzyme crystal structure complexed with a ketoamide inhibitor, docking and inhibitor binding structure, validation of pharmacophore hypothesis, overview
-
additional information
-
P2/S2 and P3/S3 interaction of cathepsin K inhibitors with pyrrolopyrimidine scaffold and structure of the common intermediate, overview
-
additional information
-
not inhibited by N-benzoyl-4-aminosalicylic acid (NSC159686), (2-biphenylylmethyl)malonic acid (NSC94914), 1,4,7,9B-tetraazaphenalene (NSC81462), 1-[1-(2-phenylethyl)-4-piperidinyl]-methanamine, 2-[(3-nitrophenyl)carbamoyl]benzoic acid (NSC408860), and methyl N-[1-(4-methoxyphenyl)-2,5-dioxopyrrolidin-3-yl]glycinate
-
additional information
a fluorescence polarization assay is developed to screen 4761 compounds for substrate-specific ectosteric collagenase inhibitors of cathepsin K. A total of 38 compounds are identified that block the collagenase activity without interfering with the hydrolysis of active site substrates such as the synthetic peptide substrate, benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin, and gelatin. The identified inhibitors can be divided into two main classes, negatively charged and polyaromatic compounds which suggest the binding to different ectosteric sites
-
additional information
irreversible covalent inhibitors can have a beneficial pharmacokinetic/pharmacodynamics profile but are still often avoided due to the risk of indiscriminate ovalent reactivity and the resulting adverse effects. To overcome this potential liability, we introduced an alkyne moiety as a latent electrophile into small molecule inhibitors of cathepsin K (CatK). Alkyne-based inhibitors do not show indiscriminate thiol reactivity but potently inhibit CatK protease activity by formation of an irreversible covalent bond with the catalytic cysteine residue. Binding mode of alkynes is irreversible and covalent
-
additional information
-
irreversible covalent inhibitors can have a beneficial pharmacokinetic/pharmacodynamics profile but are still often avoided due to the risk of indiscriminate ovalent reactivity and the resulting adverse effects. To overcome this potential liability, we introduced an alkyne moiety as a latent electrophile into small molecule inhibitors of cathepsin K (CatK). Alkyne-based inhibitors do not show indiscriminate thiol reactivity but potently inhibit CatK protease activity by formation of an irreversible covalent bond with the catalytic cysteine residue. Binding mode of alkynes is irreversible and covalent
-
additional information
-
stem bark extracts of Ulmus davidiana, a deciduous tree from Korea and an antiinflammatory in traditional Korean medicine, prevents the osteoclast-mediated intracellular processing of Cat K, suggesting that it may disrupt the intracellular transport of pro Cat K. Ulmus davidiana dose-dependently inhibits in vitro bone resorption with a potency similar to that observed for inhibition of Cat K processing
-
additional information
-
not inhibitory are phenylmethylsulfonylfluoride, disopropyfluorophosohate, soybean inhibitor, pepstatin A
-
additional information
-
inhibitor synthesis and pharnacokinetics, overview
-
additional information
not inhibited by EGTA and 1,10-phenanthroline
-
additional information
-
not inhibited by EGTA and 1,10-phenanthroline
-
additional information
-
P2/S2 and P3/S3 interaction of cathepsin K inhibitors with pyrrolopyrimidine scaffold and structure of the common intermediate, overview
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
chondroitin sulfate
-
non-essential activator in assays using low-molecular-mass substrates, 4fold stimulation of activity at 0.2 mM
dermatan sulfate
-
non-essential activator in assays using low-molecular-mass substrates, 4fold stimulation of activity at 0.2 mM
chondroitin 4-sulfate
-
18.5 kDa and 37 kDa fractions, the unique triple-helical collagen-degrading activity of cathepsin K depends on the formation of complexes with bone-or cartilage-resident glycosaminoglycans, such as chondroitin 4-sulfate, structure of the complex involving Asp6, Arg8, Lys9, Lys10, Ile171, Glu172, and Asn190 for interaction, the binding sites with chondroitin 4-sulfate are located in the R-domain of cathepsin K and are distant from its active site, detailed overview
additional information
-
cathepsin K is increased by a suppressive L-thyroxine therapy
-
additional information
procathepsin K is activated by incubation at 37°C in the presence of DTT and dextran sulfate at final concentrations of 1 mM and 100 mg/ml, respectively
-
additional information
-
procathepsin K is activated by incubation at 37°C in the presence of DTT and dextran sulfate at final concentrations of 1 mM and 100 mg/ml, respectively
-
additional information
procathepsin K is activated by incubation at 37°C in the presence of DTT and dextran sulfate at final concentrations of 1 mM and 100 mg/ml, respectively
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000087
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-alaninamide
-
-
0.000006
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-methioninamide
-
-
0.000119
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucylglycinamide
-
-
0.013
Benzyloxycarbonyl-Leu-Leu-Arg 4-methylcoumarin 7-amide
-
tert-butyloxycarbonyl-Ala-Gly-Pro- Arg 4-methylcoumarin 7-amide
0.0051
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
-
enzyme in the presence of 300 mM NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C
0.021
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
-
enzyme in the absence of NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C
0.0032
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
-
enzyme in the presence of 300 mM NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C
0.0077
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
-
enzyme in the absence of NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C
0.005
carbobenzyloxy-Leu-Arg-4-methylcoumaryl-7-amide
pH 7.0, 37°C, recombinant mutant S134A/V160L
0.0075
carbobenzyloxy-Leu-Arg-4-methylcoumaryl-7-amide
pH 7.0, 37°C, recombinant enzyme
0.016
carbobenzyloxy-Leu-Arg-4-methylcoumaryl-7-amide
pH 7.0, 37°C, recombinant mutant S134A
0.026
carbobenzyloxy-Leu-Arg-4-methylcoumaryl-7-amide
pH 7.0, 37°C, recombinant mutant V160L
0.293
carbobenzyloxy-Leu-Arg-4-methylcoumaryl-7-amide
pH 7.0, 37°C, recombinant wild-type enzyme
0.0034
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
0.0037
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E/I171E/Q172S, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
0.0038
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin
mutant enzyme N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
0.0043
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E/N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
0.0058
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E/I171E/Q172S/N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
0.048
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin
wild type enzyme, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
0.0024
Z-Leu-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E/I171E/Q172S, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
0.0033
Z-Leu-Arg-7-amido-4-methylcoumarin
wild type enzyme, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
0.0035
Z-Leu-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
0.0037
Z-Leu-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E/I171E/Q172S/N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
0.0037
Z-Leu-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E/N190M/K191G/L195K , in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
0.0046
Z-Leu-Arg-7-amido-4-methylcoumarin
mutant enzyme N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.00011
2,2'-N,N'-bis(benzyloxycarbonyl)-L-leucinylcarbohydrazide
-
pH 5.5, room temperature
23.2
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-alaninamide
-
-
3.25
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-methioninamide
-
-
23.2
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucylglycinamide
-
-
39
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
-
enzyme in the presence of 300 mM NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C
91
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
-
enzyme in the absence of NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C
0.19
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
-
enzyme in the presence of 300 mM NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C
0.37
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
-
enzyme in the absence of NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C
21.1
carbobenzyloxy-Leu-Arg-4-methylcoumaryl-7-amide
pH 7.0, 37°C, recombinant mutant S134A/V160L
46.3
carbobenzyloxy-Leu-Arg-4-methylcoumaryl-7-amide
pH 7.0, 37°C, recombinant mutant V160L
56.1
carbobenzyloxy-Leu-Arg-4-methylcoumaryl-7-amide
pH 7.0, 37°C, recombinant enzyme
95.7
carbobenzyloxy-Leu-Arg-4-methylcoumaryl-7-amide
pH 7.0, 37°C, recombinant wild-type enzyme
97.5
carbobenzyloxy-Leu-Arg-4-methylcoumaryl-7-amide
pH 7.0, 37°C, recombinant mutant S134A
1.9
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E/N190M/K191G/L195K , in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
2
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
2.1
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E/I171E/Q172S, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
2.9
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin
wild type enzyme, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
3.6
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E/I171E/Q172S/N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
3.7
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin
mutant enzyme N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
5.6
Z-Leu-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E/I171E/Q172S/N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
5.7
Z-Leu-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
6.2
Z-Leu-Arg-7-amido-4-methylcoumarin
wild type enzyme, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
6.4
Z-Leu-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E/I171E/Q172S, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
7.6
Z-Leu-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E/N190M/K191G/L195K , in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
9.1
Z-Leu-Arg-7-amido-4-methylcoumarin
mutant enzyme N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
118.8
benzyloxycarbonyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin
-
pH and temperature not specified in the publication
4300
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
-
enzyme in the absence of NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C
7600
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
-
enzyme in the presence of 300 mM NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C
48
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
-
enzyme in the absence of NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C
59
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
-
enzyme in the presence of 300 mM NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C
4400
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E/N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
5700
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E/I171E/Q172S, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
5900
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
6000
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin
wild type enzyme, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
6200
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E/I171E/Q172S/N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
9700
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin
mutant enzyme N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
1500
Z-Leu-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E/I171E/Q172S/N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
1600
Z-Leu-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
1900
Z-Leu-Arg-7-amido-4-methylcoumarin
wild type enzyme, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
2000
Z-Leu-Arg-7-amido-4-methylcoumarin
mutant enzyme N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
2100
Z-Leu-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E/N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
2700
Z-Leu-Arg-7-amido-4-methylcoumarin
mutant enzyme K9E/I171E/Q172S, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000002 - 0.000015
((S)-1-[1-[4(R,S)-((S)-2-benzyloxycarbonylamino-4-methylpentanoylamino)-3-oxoazepan-1-yl]methanoyl]-3-methylbutl)carbamic acid benzyl ester
0.0000023
((S)-1-[[(3R,S)-((S)-2-benzyloxycarbonylamino-4-methylpentanoylamino)-4-oxopyrrolidin-1-yl]methanoyl]-3-methylbutyl)carbamic acid benzyl ester
-
-
0.0000006
((S)-1-[[(3R,S)-((S)-2-benzyloxycarbonylmethylamino-4-methylpentanoylamino)-4-oxopyrrolidin-1-yl]methanoyl]-3-methylbutyl)carbamic acid benzyl ester
-
-
0.288
(1'S)-7-(1-aminoethyl)-2-(2-methoxyphenyl)pyrazolo[1,5-a] pyrimidine hydrochloride
25°C, pH 5.5
0.241
(1'S)-7-(1-aminoethyl)-2-(3-trifluoromethylphenyl)pyrazolo-[1,5-a]pyrimidine hydrochloride
25°C, pH 5.5
0.077
(1'S)-7-(1-aminoethyl)-2-benzyl-3-phenylpyrazolo[1,5-a]pyrimidine hydrochloride
25°C, pH 5.5
0.236
(1'S)-7-(1-aminoethyl)-2-phenylpyrazolo[1,5-a]pyrimidine hydrochloride
25°C, pH 5.5
0.595
(1'S)-7-(1-aminoethyl)pyrazolo[1,5-a]pyrimidine-3-(N-methylcarboxamide) hydrochloride
25°C, pH 5.5
0.714
(1'S)-7-(1-aminoethyl)pyrazolo[1,5-a]pyrimidine-3-carboxylate hydrochloride
25°C, pH 5.5
0.0000003
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.0000017
(1R,2S)-N-(cyanomethyl)-2-[2-[4-(methylsulfanyl)phenyl]ethyl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.00000013
(2R)-2-[3'-[2-(4-tert-butylpiperazin-1-yl)-1,3-thiazol-4-yl]biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
-
-
0.0000003
(2R)-N-(cyanomethyl)-2-[3'-(2-[[3-(dimethylamino)pyrrolidin-1-yl]methyl]-1,3-thiazol-4-yl)biphenyl-3-yl]-4-methylpentanamide
-
-
0.00000048
(2R)-N-(cyanomethyl)-4-methyl-2-[3'-[2-(piperazin-1-ylmethyl)-1,3-thiazol-4-yl]biphenyl-3-yl]pentanamide
-
-
0.0000008
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methylpiperazin-1-yl)biphenyl-3-yl]pentanamide
-
-
0.0019
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([2-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00024
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00073
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0015
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00029
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00043
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00045
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00057
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-3-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0011
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-4-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.001
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(thiophen-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000098
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[methyl(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0012
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(methylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0022
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(phenylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000025
1,4-anhydro-3,5,6-trideoxy-3-[(1-[4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamido]cyclohexane-1-carbonyl)amino]-L-erythro-hex-2-ulose
pH and temperature not specified in the publication
0.0003
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-([[4-([[(dimethylamino)methyl]sulfonyl]amino)phenyl]carbonyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.005
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([2-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0007
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-fluoro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00056
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00047
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([4-[(ethylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0018
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00098
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00052
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00027
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00037
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0005
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0023
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-(methylsulfamoyl)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0017
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-([[4-(1-methylethyl)-1,3-thiazol-2-yl]sulfonyl]amino)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00042
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-sulfamoylphenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00064
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methyl-1H-imidazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0005
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methylethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0012
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2,2,2-trifluoroethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00055
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2-methylphenyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.003
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00026
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methylpyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0023
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(5-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00038
1,4-anhydro-3,5,6-trideoxy-3-[[4-methyl-N-(thiophen-3-ylcarbonyl)-L-leucyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00084
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0016
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0017
1,4-anhydro-3-[[(2S)-2-[([4-[(benzylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0015
1,4-anhydro-3-[[(2S)-2-[([4-[(butylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00044
1,4-anhydro-3-[[(2S)-2-[([4-[(cyclopropylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0008
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-chloropyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00082
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00073
1,4-anhydro-3-[[(2S)-2-[[(4-[[(3-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00095
1,4-anhydro-3-[[(2S)-2-[[(4-[[(4-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00095
1,4-anhydro-3-[[(2S)-2-[[(4-[[(cyclohexylmethyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000006
1-(N-benzyloxycarbonyl-leucyl)-5-(N-Boc-phenylalanylleucyl)carbohydrazide
-
at 37°C, pH 6.0
0.0000097
1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
37°C, pH 5.6
0.0000027
2,2'-N,N'-bis(benzyloxycarbonyl)-L-leucinylcarbohydrazide
-
pH 5.5, room temperature
0.00001
2-amino-4-bromo-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
pH and temperature not specified in the publication
0.0005
2-methylpropyl [(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamate
-
-
0.0000025
3-(4-([4'-((1-[(cyanomethyl)carbamoyl]cyclohexyl)carbamoyl)biphenyl-4-yl]oxy)piperidin-1-yl)propanoic acid
-
Ki-value is below 0.0000025 mM
0.00075
3-[[(2S)-2-[([3-acetyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00095
3-[[(2S)-2-[[(4-[[(4-aminophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000025
4'-(4-tert-butylpiperazin-1-yl)-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-4-carboxamide
-
Ki-value is below 0.0000025 mM
0.0000025
4'-[4-(tert-butylamino)piperidin-1-yl]-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-4-carboxamide
-
Ki-value is below 0.0000025 mM
0.0000014
4-(2-[(3R)-3-aminopyrrolidin-1-yl]-1,3-thiazol-4-yl)-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
0.00000095
4-(dimethylamino)-N-[1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]benzamide
-
-
0.000054
4-(trifluoromethoxy)-N-(1-[[(1S)-1-([5-[3-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]carbonyl)butyl]carbamoyl]cyclohexyl)benzamide
-
-
0.00055
4-(trifluoromethoxy)-N-(1-[[(1S)-1-([5-[4-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]carbonyl)butyl]carbamoyl]cyclohexyl)benzamide
-
-
0.000019
4-fluoro-N-[1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]benzamide
-
-
0.00000045
4-[2-(1,4'-bipiperidin-1'-yl)-1,3-thiazol-4-yl]-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
0.00000029
4-[2-(4-tert-butylpiperazin-1-yl)-1,3-thiazol-4-yl]-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
0.000016
5-bromo-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)thiophene-2-carboxamide
-
-
0.0000016
benzofuran-2-carboxylic acid [(S)-3-methyl-1-[2-oxo-3-(pyridin-2-ylsulfonylamino)propylcarbamoyl]butyl]amide
-
-
0.00000025
benzyl (2S)-2-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)-4-methylpentanoate
-
Ki: value below 0.00000025 mM
0.003
benzyl [(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamate
-
-
0.03
benzyl [(1S)-2-[(cyanomethyl)amino]-1-(naphthalen-2-ylmethyl)-2-oxoethyl]carbamate
-
-
0.000084
benzyl [1-[(cyanomethyl)carbamoyl]cyclohexyl]carbamate
-
pH and temperature not specified in the publication
0.000006
Boc-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
37°C, pH 5.6
0.000022
dibenzyl [(2-oxopropane-1,3-diyl)bis[azanediyl[(2S)-4-methyl-1-oxopentane-1,2-diyl]]]biscarbamate
pH and temperature not specified in the publication
0.0000066
mPEG-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
37°C, pH 5.6
0.00000721
N'-cyano-N,N',4-trimethyl-2-(4'-(methylsulfonyl)-[1,1'-biphenyl]-3-yl)pentanehydrazide
racemic, pH and temperature not specified in the publication
0.00000114
N'-cyano-N,N',4-trimethyl-2-(4'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)pentanehydrazide
racemic, pH and temperature not specified in the publication
0.0000029
N'-cyano-N,N',4-trimethyl-2-([11,21:24,31-terphenyl]-14-yl)pentanehydrazide
pH and temperature not specified in the publication
0.000000073
N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
-
recombinant cathepsin K
0.0000043
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(2-hydroxypropan-2-yl)biphenyl-4-yl]ethyl]-L-leucinamide
-
pH and temperature not specified in the publication
0.0000017
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1R)-2,2-difluoro-1-hydroxyethyl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
-
pH and temperature not specified in the publication
0.00001
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1S)-2,2-difluoro-1-hydroxyethyl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
-
pH and temperature not specified in the publication
0.00015
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-2-pyridin-4-yl-1,3-thiazole-4-carboxamide
-
-
0.0000025
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-(4-fluoropiperidin-4-yl)biphenyl-4-carboxamide
-
Ki-value is below 0.0000025 mM
0.000002
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-(dimethylamino)biphenyl-4-carboxamide
-
-
0.0000025
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-(piperazin-1-ylsulfonyl)biphenyl-4-carboxamide
-
Ki-value is below 0.0000025 mM
0.0000025
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-([(2S)-1-methylpyrrolidin-2-yl]methoxy)biphenyl-4-carboxamide
-
Ki-value is below 0.0000025 mM
0.0000025
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-([1-(2-hydroxyethyl)piperidin-4-yl]oxy)biphenyl-4-carboxamide
-
Ki-value is below 0.0000025 mM
0.0000061
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-([4-(2,2,2-trifluoroethyl)piperazin-1-yl]sulfonyl)biphenyl-4-carboxamide
-
-
0.0000054
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-isoxazol-5-ylbiphenyl-4-carboxamide
-
-
0.0000025
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-piperazin-1-ylbiphenyl-4-carboxamide
-
Ki-value is below 0.0000025 mM
0.00000067
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-[(1-methylpiperidin-3-yl)oxy]biphenyl-4-carboxamide
-
-
0.0000025
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-[(1-methylpiperidin-4-yl)oxy]biphenyl-4-carboxamide
-
Ki-value is below 0.0000025 mM
0.0000025
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-[methyl(1-methylpyrrolidin-3-yl)amino]biphenyl-4-carboxamide
-
Ki-value is below 0.0000025 mM
0.00000059
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-(4-[(1-methylethyl)amino]piperidin-1-yl)-1,3-thiazol-4-yl)benzamide
-
-
0.0000016
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-(4-[methyl(1-methylethyl)amino]piperidin-1-yl)-1,3-thiazol-4-yl)benzamide
-
-
0.0000023
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-morpholin-4-yl-1,3-thiazol-4-yl)benzamide
-
-
0.00000025
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[(4-methylpiperazin-1-yl)amino]-1,3-thiazol-4-yl)benzamide
-
-
0.0000016
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[(4-methylpiperazin-1-yl)methyl]-1,3-thiazol-4-yl)benzamide
-
-
0.00000079
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[3-(dimethylamino)pyrrolidin-1-yl]-1,3-thiazol-4-yl)benzamide
-
-
0.00000048
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[4-(2-methoxyethyl)piperazin-1-yl]-1,3-thiazol-4-yl)benzamide
-
-
0.00000047
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[4-(tetrahydro-2H-pyran-4-yl)piperazin-1-yl]-1,3-thiazol-4-yl)benzamide
-
-
0.0000015
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(4-methylpiperazin-1-yl)benzamide
-
-
0.0000014
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(4-propylpiperazin-1-yl)benzamide
-
-
0.0000033
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(dimethylamino)benzamide
-
-
0.000014
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[(4-methylpiperazin-1-yl)carbonyl]benzamide
-
-
0.000013
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[(4-methylpiperazin-1-yl)sulfonyl]benzamide
-
-
0.00000095
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(1,4-dimethylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
-
-
0.00000094
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(1-methylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
-
-
0.0000025
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(4-morpholin-4-ylpiperidin-1-yl)-1,3-thiazol-4-yl]benzamide
-
Ki-value is below 0.0000025 mM
0.0000087
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(morpholin-4-ylmethyl)-1,3-thiazol-4-yl]benzamide
-
-
0.00000057
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(piperidin-4-yloxy)-1,3-thiazol-4-yl]benzamide
-
-
0.000035
N-(1-[[(1S)-1-[[5-(1-methylethyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamoyl]cyclohexyl)-4-(trifluoromethoxy)benzamide
-
-
0.000037
N-(1-[[(1S)-1-[[5-(3-methoxyphenyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamoyl]cyclohexyl)-4-(trifluoromethoxy)benzamide
-
-
0.000022
N-(1-[[(1S)-1-[[5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamoyl]cyclohexyl)-4-(trifluoromethoxy)benzamide
-
-
0.000011
N-(2,3-dichlorophenyl)triazolyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
standard assay conditions
0.0000014
N-(3-[[(3R)-3-([1,1'-biphenyl]-3-yl)-5-methylhex-1-en-2-yl]amino]-2-oxopropyl)-4-phenoxybenzene-1-sulfonamide
pH and temperature not specified in the publication
0.00000016
N-(4-methyl-1-oxo-1-[[3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]amino]pentan-2-yl)-1-benzofuran-2-carboxamide
-
pH and temperature not specified in the publication
0.00000008
N-(cyanomethyl)-4-methyl-2-[3'-(2-piperazin-1-yl-1,3-thiazol-4-yl)biphenyl-3-yl]pentanamide
-
-
0.00000013
N-(cyanomethyl)-4-methyl-2-[3'-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]biphenyl-3-yl]pentanamide
-
-
0.00000035
N-(cyanomethyl)-4-methyl-2-[4'-(2-piperazin-1-yl-1,3-thiazol-4-yl)biphenyl-3-yl]pentanamide
-
-
0.000015
N-4-benzyloxybenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
standard assay conditions
0.00002
N-[(1-cyano-3-azetidinyl)methyl]benzenesulfonamide
-
pH 5.5, room temperature
0.00012
N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-norvalinamide
-
-
0.000054
N-[(1S)-1-((3-hydroxy-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl)carbamoyl)-3-methylbutyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
-
-
0.0000001
N-[(1S)-1-cyclohexyl-3-[(2Z)-2-[(4R)-3,4-dimethyl-1,3-thiazolidin-2-ylidene]hydrazinyl]-2,3-dioxopropyl]cycloheptanecarboxamide
pH and temperature not specified in the publication
0.052
N-[(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]-2-phenylacetamide
-
-
0.0096
N-[(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]-3-phenylpropanamide
-
-
0.00012
N-[(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]-N2-(2,2,2-trifluoroethyl)-L-leucinamide
-
-
0.0000047
N-[(1S)-3-methyl-1-(((4R)-3-oxo-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl)carbamoyl)butyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
-
-
0.0000000048 - 0.0000048
N-[(1S)-3-methyl-1-([(4S)-3-oxo-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl]carbamoyl)butyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
0.00000014
N-[(2S)-1-[[(2R,4S)-2,4-dimethyl-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]amino]-4-methyl-1-oxopentan-2-yl]-1-benzofuran-2-carboxamide
-
pH and temperature not specified in the publication
0.0000000099
N-[(2S)-1-[[(4S,5S)-4,5-dimethyl-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]amino]-4-methyl-1-oxopentan-2-yl]-1-benzofuran-2-carboxamide
-
pH and temperature not specified in the publication
0.0000087
N-[(2S)-4-methyl-1-oxo-1-[(3aS,6aR)-3-oxohexahydro-4H-furo[3,2-b]pyrrol-4-yl]pentan-2-yl]-4-(4-methylpiperazin-1-yl)benzamide
pH and temperature not specified in the publication
0.00000016
N-[(2S)-4-methyl-1-oxo-1-[[(4R)-3-oxo-1-(pyridine-2-sulfonyl)azepan-4-yl]amino]pentan-2-yl]-2,3-dihydro-1-benzofuran-2-carboxamide
pH and temperature not specified in the publication
0.0000006
N-[(2S)-4-methyl-1-[(3aS,6S,6aR)-6-methyl-3-oxohexahydro-4H-furo[3,2-b]pyrrol-4-yl]-1-oxopentan-2-yl]-4-[2-(1-methylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
pH and temperature not specified in the publication
0.000000041
N-[(2S)-4-methyl-1-[[(4S,7R)-7-methyl-3-oxo-1-(pyridine-2-sulfonyl)azepan-4-yl]amino]-1-oxopentan-2-yl]-2,3-dihydro-1-benzofuran-2-carboxamide
pH and temperature not specified in the publication
0.0000079
N-[1-([(1S)-1-[(5-ethyl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
0.00000025 - 0.0000017
N-[1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
0.0000033
N-[1-([(1S)-1-[(5-methoxy-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
0.000029
N-[1-([(1S)-1-[(5-phenyl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
0.0013
N-[1-([(1S)-1-[(5-tert-butyl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
0.0000052
N-[1-([(1S)-1-[(5-thiophen-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
0.0000016
N-[4-methyl-1-oxo-1-([2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]amino)pentan-2-yl]-1-benzofuran-2-carboxamide
-
pH and temperature not specified in the publication
0.0000012
N2-(morpholin-4-ylcarbonyl)-N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-leucinamide
-
-
0.00035
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-5,5,5-trifluoro-D-leucinamide
-
-
0.00027
PHPMA-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
37°C, pH 5.6
0.000392
PHPMAGG-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
37°C, pH 5.6
0.000001 - 0.000002
piperidine-4-carboxylic acid [3-methyl-1[1-(naphtho[1,2-d]oxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
0.000044
quinoline-2-carboxylic acid [(S)-1-((3R,S)-4-oxotetrahydrofuran-3ylcarbamoyl)-3-methylbutyl]amide
-
-
0.000000041
relicatib
-
apparent value, pH and temperature not specified in the publication
0.0000113
STPHPMA-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
37°C, pH 5.6
0.033
tert-butyl [(1S)-1-([5-[4-(dimethylamino)phenyl]-1,3,4-oxadiazol-2-yl]carbonyl)butyl]carbamate
-
-
0.00081
tert-butyl [(1S)-1-[(5-thiophen-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamate
-
-
0.0056
tert-butyl [(1S)-1-[[5-(1-methylethyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamate
-
-
0.017
tert-butyl [(1S)-1-[[5-(2-methoxyphenyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamate
-
-
0.000043
tert-butyl [1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]carbamate
-
-
0.00025
[(S)-1-((3R,S)-1-acetyl-4-oxopyrrolidin-3-ylcarbamoyl)-3-methylbutyl]carbamic acid benzyl ester
-
-
0.00014
[(S)-1-((3R,S)-4-oxotetrahydrofuran-3-ylcarbamoyl)-3-methylbutyl]carbamic acid benzyl ester
-
-
0.00015
[(S)-1-((4R,S)-3-oxotetrahydropyran-4-ylcarbamoyl)-3-methylbutyl]carbamic acid benzyl ester
-
-
0.000002
((S)-1-[1-[4(R,S)-((S)-2-benzyloxycarbonylamino-4-methylpentanoylamino)-3-oxoazepan-1-yl]methanoyl]-3-methylbutl)carbamic acid benzyl ester
-
the faster eluting diastereomer C34H46N4O7*0.4H2O
0.000015
((S)-1-[1-[4(R,S)-((S)-2-benzyloxycarbonylamino-4-methylpentanoylamino)-3-oxoazepan-1-yl]methanoyl]-3-methylbutl)carbamic acid benzyl ester
-
the slower eluting diastereomer C34H46N4O7*0.3H2O
0.0000000048
N-[(1S)-3-methyl-1-([(4S)-3-oxo-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl]carbamoyl)butyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
-
-
0.0000048
N-[(1S)-3-methyl-1-([(4S)-3-oxo-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl]carbamoyl)butyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
-
-
0.00000025
N-[1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
Ki: value below 0.00000025 mM
0.0000017
N-[1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
0.000001
piperidine-4-carboxylic acid [3-methyl-1[1-(naphtho[1,2-d]oxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
-
21-24°C, pH 5.5
0.000002
piperidine-4-carboxylic acid [3-methyl-1[1-(naphtho[1,2-d]oxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
-
21-24°C, pH 5.5
0.000000041
relacatib
-
pH and temperature not specified in the publication
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.00000028
(11R,12R)-14,14-difluoro-34-(methylsulfanyl)-N-(prop-2-yn-1-yl)-11,12,13,14,15,16-hexahydro[11,21:22,31-terphenyl]-12-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00000033
(1R)-1-benzyl-2-methylpropyl [(1S)-1-[(E)-[(morpholin-4-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.0000005
(1R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
0.000009
(1R,2R)-2-[1-benzyl-5-[4-(methylsulfanyl)phenyl]-1H-1,2,3-triazol-4-yl]-N-(cyanomethyl)-5,5-difluorocyclohexanecarboxamide
0.0000061
(1R,2R)-5,5-dichloro-N-(1-cyanocyclopropyl)-2-[4-[4-(methylsulfonyl)phenyl]-1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.0000093
(1R,2R)-N-(1-cyanocyclopropyl)-5,5-difluoro-2-[4-[4-(methylsulfonyl)phenyl]-1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.000002
(1R,2R)-N-(cyanomethyl)-2-(4-[4-[(difluoromethyl)sulfanyl]phenyl]pyridin-3-yl)-5,5-difluorocyclohexanecarboxamide
0.0000004 - 0.00000041
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[1-methyl-4-[4-(methylsulfanyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
0.0000045
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[1-methyl-4-[4-(methylsulfonyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.0000001
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-methyl-4-[4-(methylsulfanyl)phenyl]-1,3-thiazol-5-yl]cyclohexanecarboxamide
0.000001
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-[4-(methylsulfanyl)phenyl]pyridin-3-yl]cyclohexanecarboxamide
0.000005
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-1-oxidopyridin-4-yl]cyclohexanecarboxamide
0.000006 - 0.000008
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
0.000001
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]pyridin-4-yl]cyclohexanecarboxamide
0.0000003 - 0.00000032
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
0.0000186
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4-[4-(methylsulfonyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.000004 - 0.000005
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[5-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
0.00000094
(1S)-1-methyl-2-phenylethyl [(1S)-1-[(E)-[(morpholin-4-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.0000014
(1S)-1-[(5,6-dichloro-1H-benzimidazol-1-yl)methyl]-2,2-dimethylpropyl [(1S)-1-methyl-2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamate
Homo sapiens
-
-
0.0000032
(1S)-1-[(5,6-dichloro-1H-benzimidazol-1-yl)methyl]-2,2-dimethylpropyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
Homo sapiens
-
-
0.0000021
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-([[(6-fluoropyridin-2-yl)carbonyl]amino]acetyl)pentyl]carbamate
Homo sapiens
-
-
0.000018
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-methyl-2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamate
Homo sapiens
-
-
0.000000072
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[oxo(1H-pyrazol-5-ylamino)acetyl]pentyl]carbamate
Homo sapiens
-
-
0.00025
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[[(morpholin-4-ylcarbonyl)amino]acetyl]pentyl]carbamate
Homo sapiens
-
value above 0.000250 mM
0.0000004
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
Homo sapiens
-
-
0.000065
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamate
Homo sapiens
-
-
0.0000064
(1S)-2,2-dimethyl-1-([4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]methyl)propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
Homo sapiens
-
-
0.0000076
(1S)-2,2-dimethyl-1-([4-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
Homo sapiens
-
-
0.0000055
(1S)-2,2-dimethyl-1-[(3-pyridin-3-yl-1H-pyrazol-1-yl)methyl]propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
Homo sapiens
-
-
0.0000038
(1S)-2,2-dimethyl-1-[(3-pyridin-4-yl-1H-pyrazol-1-yl)methyl]propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
Homo sapiens
-
-
0.0003
(1S)-2,2-dimethyl-1-[[3-(trifluoromethyl)-1H-pyrazol-1-yl]methyl]propyl [(1S)-1-methyl-2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamate
Homo sapiens
-
-
0.000032
(1S)-2,2-dimethyl-1-[[3-(trifluoromethyl)-1H-pyrazol-1-yl]methyl]propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
Homo sapiens
-
-
0.0195
(2E,4E)-5-(1-hydroxy-2,6,6-trimethyl-4-oxocyclohex-2-en-1-yl)-3-methylpenta-2,4-dienoic acid
Homo sapiens
pH 5.5, 25°C, collagenase activity, 4.9% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate
0.000028
(2R)-2-[3'-[2-(4-tert-butylpiperazin-1-yl)-1,3-thiazol-4-yl]biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
Homo sapiens
-
IC50: in vitro bone resorption assay
0.00001
(2R)-4-fluoro-4-methyl-N-(3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl)-2-((R)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.000172
(2R)-N-(cyanomethyl)-2-[3'-(2-[[3-(dimethylamino)pyrrolidin-1-yl]methyl]-1,3-thiazol-4-yl)biphenyl-3-yl]-4-methylpentanamide
Homo sapiens
-
IC50: in vitro bone resorption assay
0.000043
(2R)-N-(cyanomethyl)-4-methyl-2-[3'-[2-(piperazin-1-ylmethyl)-1,3-thiazol-4-yl]biphenyl-3-yl]pentanamide
Homo sapiens
-
IC50: in vitro bone resorption assay
0.000003
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)-[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC 50: 3 nM, reversible inhibition
0.000095
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methylpiperazin-1-yl)biphenyl-3-yl]pentanamide
Homo sapiens
-
IC50: in vitro bone resorption assay
0.000003
(2R)-N-cyano-4-methyl-2-[4'-(piperazin-1-yl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
pH and temperature not specified in the publication
0.0012
(2S)-2-(biphenyl-2-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
Homo sapiens
-
-
0.00009
(2S)-2-(biphenyl-3-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
Homo sapiens
-
-
0.0001
(2S)-2-(biphenyl-4-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
Homo sapiens
-
-
0.0000002
(2S)-4,4-dichloro-N-(1-cyanocyclopropyl)-2-([(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]amino)butanamide
Oryctolagus cuniculus
-
above, humanized rabbit cathepsin K
0.0000069
(2S)-4-fluoro-4-methyl-N-(1-(2-(methylsulfonyl)phenyl)-3-oxopiperidin-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.000016
(2S)-4-fluoro-4-methyl-N-(1-(methylsulfonyl)-3-oxoazepan-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.000027
(2S)-4-fluoro-4-methyl-N-(1-(methylsulfonyl)-4-oxopyrrolidin-3-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.0000018 - 0.000002
(2S)-4-fluoro-4-methyl-N-(3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
0.0000057
(2S)-4-fluoro-4-methyl-N-(3-oxo-1-(pyridin-2-ylsulfonyl)piperidin-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.0000083
(2S)-4-fluoro-4-methyl-N-(3-oxo-1-phenylpiperidin-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.000033
(2S)-4-fluoro-4-methyl-N-(3-oxoazepan-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.000085
(2S)-4-fluoro-4-methyl-N-(4-oxo-1-(pyridin-2-ylsulfonyl)pyrrolidin-3-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.0000098
(2S)-4-fluoro-4-methyl-N-(4-oxopyrrolidin-3-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.000159
(2S)-N-(1-(benzylsulfonyl)-3-oxoazepan-4-yl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.0000042
(2S)-N-(1-acetyl-4-oxopyrrolidin-3-yl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.0000029
(2S)-N-(1-benzoyl-4-oxopyrrolidin-3-yl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.0000015
(2S)-N-(1-cyanocyclopropyl)-4,4,4-trifluoro-2-([(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]amino)butanamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.000069
(2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-(3-phenoxyphenoxy)pentanamide
Homo sapiens
-
-
0.0006
(2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-(4-phenoxyphenoxy)pentanamide
Homo sapiens
-
-
0.003
(2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-phenoxypentanamide
Homo sapiens
-
-
0.0000048
(4-[[(2S)-2-([1-[([1,1'-biphenyl]-3-yl)amino]cyclohexane-1-carbonyl]amino)butyl]amino]phenoxy)acetic acid
Homo sapiens
pH and temperature not specified in the publication
0.0000004
(4R)-N-(1-cyanocyclopropyl)-5,5,5-trifluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.0000003
(4S)-N-(1-cyanocyclopropyl)-5,5,5-trifluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.0000002
(S)-N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.0062
1,6-dimethyl-1,2-dihydrophenanthro[1,2-b]furan-10,11-dione
Homo sapiens
pH and temperature not specified in the publication
0.000011
1-(3-chlorophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
Homo sapiens
-
pH 5.5, 30°C
0.000024
1-(4-chlorophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
Homo sapiens
-
pH 5.5, 30°C
0.000004
1-(4-cyanophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
Homo sapiens
-
pH 5.5, 30°C
0.000099
1-(4-cyclohexylphenoxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.00013
1-(4-ethylphenoxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.02
1-(biphenyl-2-ylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
Homo sapiens
-
value above 20 mM
0.000082
1-(biphenyl-3-ylamino)-N-[(1R)-2-[(4-methoxyphenyl)amino]-1-methylethyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.0000039
1-(biphenyl-3-ylamino)-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]butyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.0000056
1-(biphenyl-3-ylamino)-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]pentyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.0000027
1-(biphenyl-3-ylamino)-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]propyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.000019
1-(biphenyl-3-ylamino)-N-[(1S)-2-[(4-methoxyphenyl)amino]-1-methylethyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.000083
1-(biphenyl-3-ylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.00032
1-(biphenyl-3-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.0001
1-(biphenyl-4-ylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.00019
1-(biphenyl-4-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.00000011
1-benzylcyclopentyl [(1S)-1-[(E)-[(2,3-dihydro-1H-indol-1-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.000014
1-Isopropyl-2-methylpropyl (1S)-1-cyclohexylmethyl-2,3-dioxo-3-[(thien-2-ylmethyl)-amino]propylcarbamate
Homo sapiens
-
IC50: 14 nM
0.000047
1-Isopropyl-2-methylpropyl (1S)-1-isoprpyl-2,3-dioxo-3-[(thien-2-ylmethyl)-amino]propylcarbamate
Homo sapiens
-
IC50: 47 nM
0.00036
1-Isopropyl-2-methylpropyl (1S)-1-methyl-2,3-dioxo-3-[(thien-2-ylmethyl)-amino]propylcarbamate
Homo sapiens
-
IC50: 360 nM
0.0000051
1-Isopropyl-2-methylpropyl (1S)-1-[(isoxazol-3-ylamino)(oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 5.1 nM
0.000083
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1,3,4-thiadiazol-2-ylamino)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 83 nM
0.00004
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1,3-thiazol-2-ylamino)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 40 nM
0.00000077 - 0.000013
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1H-pyrazol-5-ylamino)acetyl]pentylcarbamate
0.0000048
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(isoquinolin-2-ylamino)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 4.8 nM
0.000052
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(pyrazin-2-ylamino)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 52 nM
0.000032
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(pyridin-2-ylamino)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 32 nM
0.000095
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(pyridin-3-ylamino)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 95 nM
0.00025
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(quinolin-2-ylamino)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 250 nM
0.000015 - 0.00079
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
0.000062 - 0.0012
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-2-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
0.000025 - 0.00047
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-4-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
0.00000065 - 0.000012
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(3-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
0.00000021 - 0.0000018
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(4-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
0.0000092
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(thien-2-ylmethyl)-amino]acetyl]pentylcarbamate
Homo sapiens
-
IC50: 9.2 nM
0.000015 - 0.0011
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
0.000022 - 0.0012
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclohexyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
0.00002 - 0.0011
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclopentyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
0.000026 - 0.0015
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-ethyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
0.000039 - 0.0027
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
0.000017 - 0.001
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isopropyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
0.00000041 - 0.000011
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-3-yl)amino](oxo)acetyl]pentylcarbamate
0.000032 - 0.0017
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
0.00000071
1-Isopropyl-2-methylpropyl (1S)-1-[[(3-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 0.71 nM
0.00000024
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-bromo-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 0.24 nM
0.00000091
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-cyano-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 0.91 nM
0.00000026
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-fluoro-1H-indazol-3-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 0.26 nM
0.00000047 - 0.0000055
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
0.000062 - 0.0016
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(3,3-dimethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
0.000027 - 0.0017
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(cyclopropylmethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
0.000027
1-Isopropyl-2-methylpropyl (1S)-2,3-dioxo--1-phenyl-3-[(thien-2-ylmethyl)-amino]propylcarbamate
Homo sapiens
-
IC50: 27 nM
0.000024
1-Isopropyl-2-methylpropyl (1S)-3-methyl-1-[oxo[(thien-2-ylmethyl)-amino]acetyl]butylcarbamate
Homo sapiens
-
IC50: 24 nM
0.000087
1-Isopropyl-2-methylpropyl (1S,2S)-2-methyl-1-[oxo[(thien-2-ylmethyl)-amino]acetyl]butylcarbamate
Homo sapiens
-
IC50: 87 nM
0.012
1-Isopropyl-2-methylpropyl 2,3-dioxo-3-[(thien-2-ylmethyl)-amino]propylcarbamate
Homo sapiens
-
IC50: 0.012 mM
0.00013
1-methylethyl (2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazinecarboxylate
Homo sapiens
-
-
0.000026
1-[(1H-imidazol-4-yl)methyl]-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole
Homo sapiens
pH and temperature not specified in the publication
0.000006
1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-(3-methylphenyl)urea
Homo sapiens
-
pH 5.5, 30°C
0.000025
1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-phenylurea
Homo sapiens
-
pH 5.5, 30°C
0.000023
1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-[3-(trifluoromethyl)phenyl]urea
Homo sapiens
-
pH 5.5, 30°C
0.186
13-methyl-2H,10H-[1,3]benzodioxolo[5,6-c][1,3]dioxolo[4,5-i]phenanthridin-13-ium
Homo sapiens
pH 5.5, 25°C, collagenase activity, 14% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate
0.0088 - 0.02724
2-(2,4-dihydroxyphenyl)-5,7-dihydroxy-6-[5-methyl-2-(prop-1-en-2-yl)hex-4-en-1-yl]-2,3-dihydro-4H-1-benzopyran-4-one
0.01
2-(3-methoxyphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.0035
2-(3-methylphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000288
2-(3-tert-butylphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000026
2-(4-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-3-oxoazepan-1-ylsulfonyl)pyridine 1-oxide
Homo sapiens
-
-
0.01
2-(biphenyl-3-yl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.00012
2-(cyclohexylamino)pyrimidine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0011
2-(cyclohexylmethyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00000001 - 0.00001
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
0.000000009
2-cyano-4-(cyclohexylamino)-N-[2-(3-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000000022 - 0.000022
2-cyano-4-(cyclohexylamino)-N-[2-(4-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
0.00000075
2-cyano-4-(cyclohexylamino)-N-[2-(4-pyrrolidin-1-ylphenyl)ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000000047 - 0.000047
2-cyano-4-(cyclohexylamino)-N-[2-[4-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
0.000009
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.000000031
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[3-[2-(1H-imidazol-1-yl)ethoxy]-4-methoxyphenyl]ethyl)pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000000003
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[3-[2-(1H-imidazol-1-yl)ethoxy]phenyl]ethyl)pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000000013
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[4-[(1-methylpiperidin-4-yl)oxy]phenyl]ethyl)pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000000011
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]ethyl)pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000000003 - 0.000003
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[4-[2-(1H-imidazol-1-yl)ethoxy]phenyl]ethyl)pyrimidine-5-carboxamide
0.000000003
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-(3-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
value below 0.000000003 mM
0.000000003 - 0.000003
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-(4-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
0.0000003
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-(4-pyrrolidin-1-ylphenyl)ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000000011
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-[3-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000000025 - 0.000025
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-[4-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
0.000034
2-cyano-4-[(cyclohexylmethyl)(methyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.000015
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.00013
2-cyano-4-[[(4,4-difluorocyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.00017
2-cyano-N-[(1-methyl-4-phenylpiperidin-4-yl)methyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.000038
2-cycloheptyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0001
2-cycloheptyl-3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00011
2-cycloheptyl-4-[2-(dimethylamino)ethyl]-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0005
2-cycloheptyl-4-[3-(morpholin-4-yl)propyl]-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000197
2-cyclohexyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00087
2-cyclopentyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.01
2-[3-(hydroxymethyl)phenyl]-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.0000062
2-[[2-cyano-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methyl]-N-cyclohexyl-1,3-dioxo-2,8-diazaspiro[4.5]decane-8-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000042
2-[[2-cyano-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methyl]-N-methyl-1,3-dioxo-2,8-diazaspiro[4.5]decane-8-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.009
3,3'-[(3-carboxy-4-oxocyclohexa-2,5-dien-1-ylidene)methylene]bis(6-hydroxybenzoic acid)
Homo sapiens
pH 5.5, 25°C, collagenase activity, 1.7% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate
0.01
3,5-dioxo-2-phenyl-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.000072
3,5-dioxo-2-[3-(propan-2-yl)phenyl]-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00446
3,5-dioxo-4-(2-phenylethyl)-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.012
3,5-dioxo-4-phenyl-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.01
3,5-dioxo-4-propyl-2-[4-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.000182
3,5-dioxo-4-[2-(piperidin-1-yl)ethyl]-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000038
3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2-[3-(propan-2-yl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000017
3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000045
3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-2-oxopropylcarbamate
Homo sapiens
-
-
0.000068
3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxo-N-(phenylsulfonyl)pyrrolidine-1-carboxamide
Homo sapiens
-
-
0.0000073
3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxo-N-phenylpyrrolidine-1-carboxamide
Homo sapiens
-
-
0.0000073
3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxamide
Homo sapiens
-
-
0.0000048
3-(4-[[(2S)-2-([[1-(biphenyl-3-ylamino)cyclohexyl]carbonyl]amino)butyl]amino]phenoxy)propanoic acid
Homo sapiens
-
-
0.001
3-(cyclohexylamino)benzonitrile
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
1
3-amino-4-[(tetrahydro-2-furanylmethyl)amino] benzoic acid
Homo sapiens
-
at pH 5.5 and 28°C
0.0000045
3-[4-([(2S)-2-[(N-biphenyl-3-yl-L-leucyl)amino]butyl]amino)phenoxy]propanoic acid
Homo sapiens
-
-
0.00039
3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzamide
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.0000002
4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-fluoro-4-methyl-1-oxopentan-2-yl]amino)-2,2,2-trifluoroethyl][1,1'-biphenyl]-4-sulfonic acid
Homo sapiens
pH and temperature not specified in the publication
0.0000002
4'-[(1S)-1-([(2S)-1-[(cyanomethyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2,2-trifluoroethyl][1,1'-biphenyl]-4-sulfonic acid
Homo sapiens
pH and temperature not specified in the publication
0.000096
4-(3,4-dimethylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000293
4-(3-cyanophenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000457
4-(3-cyclopentylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000181
4-(3-methylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000011
4-(3-tert-butylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000009
4-(4-acetylpiperazin-1-yl)-5-amino-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00017
4-(cyclohexylamino)pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000132
4-(dimethylamino)-N-[1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]benzamide
Homo sapiens
-
IC50: in vitro bone resorption assay
0.001
4-benzyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0074
4-butyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000084
4-cycloheptyl-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00068
4-cyclohexyl-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000011
4-cyclooctyl-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.002
4-cyclopentyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0025
4-ethyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000033
4-fluoro-N-(3-oxoazepan-4-yl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.0000098
4-fluoro-N-(4-oxopyrrolidin-3-yl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.0000083
4-fluoro-N-(5-oxo-2-phenylpiperidin-4-yl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.00029
4-fluoro-N-prop-2-yn-1-yl-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
Homo sapiens
50 mM MES pH 5.5, 25 mM EDTA and 2.5 mM DTT. 0.05% Tween20 (v/v), 37°C
0.000016
4-fluoro-N-[1-(methylsulfonyl)-3-oxoazepan-4-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.000027
4-fluoro-N-[1-(methylsulfonyl)-4-oxopyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.0000069
4-fluoro-N-[2-[2-(methylsulfonyl)phenyl]-5-oxopiperidin-4-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.000002
4-fluoro-N-[3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.0000057
4-fluoro-N-[3-oxo-1-(pyridin-2-ylsulfonyl)piperidin-4-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.0000073
4-fluoro-N-[4-oxo-1-(phenylcarbamoyl)pyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.0000029
4-fluoro-N-[4-oxo-1-(phenylcarbonyl)pyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.000085
4-fluoro-N-[4-oxo-1-(pyridin-2-ylsulfonyl)pyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.000068
4-fluoro-N-[4-oxo-1-[(phenylsulfonyl)carbamoyl]pyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.00478
4-methyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000985
4-phenyl-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.004074
4-propyl-6-[2-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000033
4-propyl-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.001
4-propyl-6-[4-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000019
4-[(2,2-dimethylpropyl)(4-iodobenzyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000071
4-[(2,2-dimethylpropyl)amino]-5-(3-[4-[(4-methoxyphenyl)sulfonyl]piperazin-1-yl]prop-1-yn-1-yl)pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000086
4-[(2,2-dimethylpropyl)amino]-5-[3-(pyridin-3-yloxy)prop-1-yn-1-yl]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000071
4-[(2,2-dimethylpropyl)amino]-5-[3-[4-(4-methylpiperazin-1-yl)phenyl]prop-1-yn-1-yl]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000048
4-[(2,2-dimethylpropyl)[4-(1H-1,2,4-triazol-1-ylmethyl)benzyl]amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000073
4-[(2,2-dimethylpropyl)[4-(3-piperidin-1-ylprop-1-yn-1-yl)benzyl]amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000086
4-[(2,2-dimethylpropyl)[4-[3-(1H-1,2,4-triazol-1-yl)prop-1-yn-1-yl]benzyl]amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000038
4-[(2,2-dimethylpropyl)[4-[3-(4-methylpiperazin-1-yl)prop-1-yn-1-yl]benzyl]amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00024
4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.0000048
4-[2-(4-methylpiperazin-1-yl)-4,5-dihydro-1,3-thiazol-4-yl]-N-(1-[[(3S,4R)-2-oxo-4-phenoxyazetidin-3-yl]carbamoyl]cyclohexyl)benzamide
Homo sapiens
pH and temperature not specified in the publication
0.00081
4-[2-(dimethylamino)ethyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.001
4-[2-chloro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0001
4-[3-(dimethylamino)propyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000148
4-[3-(methylsulfonyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000112
4-[3-(morpholin-4-yl)propyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000004
4-[3-(pentan-3-ylamino)propyl]-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000004
4-[3-(piperidin-1-yl)propyl]-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00001
4-[3-(tert-butylamino)propyl]-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000034
4-[4-chloro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00028
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzamide
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.0000036
4-[[4-[3-(1,4'-bipiperidin-1'-yl)prop-1-yn-1-yl]benzyl](2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000064
4-[[4-[3-(4-acetylpiperazin-1-yl)prop-1-yn-1-yl]benzyl](2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000037
5-(3-[4-[(3-chloropropyl)sulfonyl]piperazin-1-yl]prop-1-yn-1-yl)-4-[(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000032
5-amino-4-(3-hydroxyazetidin-1-yl)-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000002
5-amino-4-(bicyclo[2.2.1]hept-2-ylamino)-6-morpholin-4-ylpyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000023
5-amino-4-(cyclohexylamino)-6-morpholin-4-ylpyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000013
5-amino-4-(cyclopentylamino)-6-morpholin-4-ylpyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00034
5-amino-4-morpholin-4-yl-6-(tetrahydrofuran-3-ylamino)pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000022
5-amino-4-morpholin-4-yl-6-pyrrolidin-1-ylpyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000014
5-amino-4-[(1,1-dioxidotetrahydrothiophen-3-yl)amino]-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00056
5-amino-4-[(1-methylethyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0003
5-amino-4-[(1-methylpropyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000017
5-amino-4-[(2,2-dimethylpropyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000024
5-amino-4-[(2-methoxyethyl)amino]-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000018
5-amino-4-[(2-methylpropyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000006
5-amino-4-[(2-methylpropyl)amino]-6-piperazin-1-ylpyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000062
5-amino-4-[(2-methylpropyl)amino]-6-[(tetrazolidin-5-ylmethyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0001
5-bromo-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.00001
5-[3-(1,3-dihydro-2H-isoindol-2-yl)prop-1-yn-1-yl]-4-[(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000032
5-[3-(3,4-dihydroisoquinolin-2(1H)-yl)prop-1-yn-1-yl]-4-[(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000072
5-[3-(4,5-dichloro-1H-imidazol-1-yl)prop-1-yn-1-yl]-4-[(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.075
6,8-dihydroxy-3-(3,4,5-trihydroxyphenyl)-2,3-dihydro-1,4-benzodioxin-2-yl 3,4,5-trihydroxybenzoate
Homo sapiens
pH 5.5, 25°C, collagenase activity, 12% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate
0.000001
6-(4-chlorobenzyl)-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.001
6-(4-chlorobenzyl)-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.00022 - 0.0022
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.001
6-(4-chlorobenzyl)-7-(2-cyclooctylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000017
6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.0001 - 0.00011
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000001
6-(4-chlorobenzyl)-7-(3,3,3-trifluoropropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.001
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.0001
6-(4-chlorobenzyl)-7-(4,4,4-trifluorobutyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0001
6-(4-chlorobenzyl)-7-(4,4-dimethylpentyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000006
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.0000023
6-(4-chlorobenzyl)-7-cyclohexyl-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.001
6-(4-chlorobenzyl)-7-[2-(3-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.001
6-(4-chlorobenzyl)-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.001
6-(4-chlorobenzyl)-7-[2-(piperidin-1-yl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000014
6-(cyclohexylamino)-9-[(2S,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-9H-purine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000006
6-(cyclohexylamino)-9-[2-(4-methylpiperazin-1-yl)ethyl]-9H-purine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.001
6-(cyclohexylamino)pyrazine-2-carbonitrile
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.001
6-(cyclohexylamino)pyridine-2-carbonitrile
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.0000012
6-benzyl-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000015
6-benzyl-7-cyclohexyl-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.002
6-cyano-2-(3-trifluoromethyl-phenyl)-3,5-dioxo-1,2,4-triazine
Homo sapiens
-
pH and temperature not specified in the publication
0.0000065
6-[(1'-acetyl-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000004
6-[(4,5-dichloro-1H-imidazol-1-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000004
6-[(5,5-dimethyl-2,4-dioxo-1,3-oxazolidin-3-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000027
6-[(8-acetyl-1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
6-[(8-benzyl-1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.000001
6-[4-[(diethylamino)methyl]benzyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.00029
6-[[4-(4-acetyl-1,4-diazepan-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
0.0059
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
0.00165
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
0.000079
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
0.0054
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
0.0000054
6-[[8-(2,4-dimethoxyphenyl)-1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl]methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000001 - 0.00003
7-(2,2-dimethyl-propyl)-6-(1,3-dioxo-2,8-diaza-spiro[4.5]dec-2-ylmethyl)-7H-pyrrolo[2,3-d] pyrimidine-2-carbonitrile
0.000005
7-(2,2-dimethylpropyl)-6-(1H-1,2,3-triazol-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000006
7-(2,2-dimethylpropyl)-6-(1H-imidazol-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000002
7-(2,2-dimethylpropyl)-6-[(1'-methyl-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
7-(2,2-dimethylpropyl)-6-[(1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.000001
7-(2,2-dimethylpropyl)-6-[(1,3-dioxo-2,8-diazaspiro[4.5]decan-2-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
IC50 below 1 nM, pH and temperature not specified in the publication
0.000001 - 0.000076
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000001
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000001
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-3-propyl-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000001 - 0.000027
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-8-propyl-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000001
7-(2,2-dimethylpropyl)-6-[(2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.000001 - 0.000012
7-(2,2-dimethylpropyl)-6-[(3-methyl-2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.0000017
7-(2,2-dimethylpropyl)-6-[(5-fluoro-1'-methyl-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000017 - 0.0000078
7-(2,2-dimethylpropyl)-6-[(5-fluoro-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.0000019
7-(2,2-dimethylpropyl)-6-[(5-methoxy-1'-methyl-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000001 - 0.000044
7-(2,2-dimethylpropyl)-6-[(5-methoxy-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000003
7-(2,2-dimethylpropyl)-6-[(pyridin-4-yloxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
7-(2,2-dimethylpropyl)-6-[4-(4-methylpiperazin-1-yl)benzyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.000001
7-(2,2-dimethylpropyl)-6-[4-(morpholin-4-yl)benzyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.0000017
7-(2,2-dimethylpropyl)-6-[[2-oxo-1'-(propan-2-yl)spiro[indole-3,4'-piperidin]-1(2H)-yl]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
7-(2,2-dimethylpropyl)-6-[[4-(4-fluorophenyl)piperazin-1-yl]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000022
7-(2,2-dimethylpropyl)-6-[[8-(morpholin-4-ylacetyl)-1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00028
7-(2-cyclohexylethyl)-6-(4-methoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00025
7-(2-cyclohexylethyl)-6-[(pyridin-2-yloxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00048
7-(2-cyclohexylethyl)-6-[(pyridin-2-ylsulfanyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.0143
acetyl-strophanthidin
Homo sapiens
pH 5.5, 25°C, collagenase activity, 5.4% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate
0.0000006 - 0.000044
benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate
0.00066 - 0.00071
carbobenzyloxy-Phe-Phe-CH2F
Homo sapiens
-
pH 5.5, 22°C, recombinant enzyme, dependent on the substrate
0.000181 - 0.00426
dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate
0.088
ellipticine
Homo sapiens
pH 5.5, 25°C, 4.0% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate
0.0016
ethyl 3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxylate
Homo sapiens
-
-
0.0000016
ethyl 3-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-4-oxopyrrolidine-1-carboxylate
Oryctolagus cuniculus
-
-
0.000054
ethyl 4-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-3-oxoazepane-1-carboxylate
Homo sapiens
-
-
0.000009
ethyl 4-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-3-oxopiperidine-1-carboxylate
Homo sapiens
-
-
0.000054
ethyl 4-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-3-oxoazepane-1-carboxylate
Oryctolagus cuniculus
-
-
0.000009
ethyl 4-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-5-oxopiperidine-2-carboxylate
Oryctolagus cuniculus
-
-
0.0000017
Ethyl 5-[((3S)-3[[(isopropyl-2-methylpropoxy)carbonyl]amide]-2-oxoheptanoyl)amino]-1H-pyrazole-4-carboxylate
Homo sapiens
-
IC50: 1.7 nM
0.00047
ethyl N-[[(2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazino]carbonyl]-b-alaninate
Homo sapiens
-
-
0.00052
ethyl N-[[(2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazino]carbonyl]glycinate
Homo sapiens
-
-
0.0000043
methyl 3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxylate
Homo sapiens
-
-
0.0000043
methyl 3-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-4-oxopyrrolidine-1-carboxylate
Oryctolagus cuniculus
-
-
0.000001
methyl 4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-fluoro-4-methyl-1-oxopentan-2-yl]amino)-2,2-difluoroethyl]biphenyl-4-sulfinate
Oryctolagus cuniculus
-
pH and temperature not specified in the publication
0.0000003
methyl 4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2,2-trifluoroethyl]biphenyl-4-sulfinate
Oryctolagus cuniculus
-
pH and temperature not specified in the publication
0.0000008
methyl 4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2-difluoroethyl]biphenyl-4-sulfinate
Oryctolagus cuniculus
-
pH and temperature not specified in the publication
0.0000003
methyl 4'-[(1S)-1-([(2S)-1-[(cyanomethyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2-difluoroethyl]biphenyl-4-sulfinate
Oryctolagus cuniculus
-
pH and temperature not specified in the publication
0.0335 - 0.037
methyl 5-acetoxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
Homo sapiens
-
pH 5.5, 22°C, recombinant enzyme, dependent on the substrate
0.000021
methyl 5-hydroxy-7,12-dioxo-7,12-dihydrodinaphtho[1,2-b:2',3'-d]furan-6-carboxylate
Homo sapiens
pH and temperature not specified in the publication
0.0215 - 0.028
methyl 5-hydroxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
Homo sapiens
-
pH 5.5, 22°C, recombinant enzyme, dependent on the substrate
0.045 - 0.067
methyl 5-methoxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
Homo sapiens
-
pH 5.5, 22°C, recombinant enzyme, dependent on the substrate
0.04 - 0.042
methyl 5-propoxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
Homo sapiens
-
pH 5.5, 22°C, recombinant enzyme, dependent on the substrate
0.000027
methyl N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-methioninate
Homo sapiens
-
-
0.00018
methyl [[(2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazino]carbonyl]carbamate
Homo sapiens
-
-
0.00000016
N-((S)-4-methyl-1-oxo-1-((S)-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-ylamino)pentan-2-yl)benzofuran-2-carboxamide
Homo sapiens
-
-
0.0000024 - 0.000028
N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
0.0000042
N-(1-acetyl-4-oxopyrrolidin-3-yl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.0000073
N-(1-carbamoyl-4-oxopyrrolidin-3-yl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.000004
N-(1-cyano-1-methylethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.0000006 - 0.0000051
N-(1-cyano-2-phenylethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
0.0000002
N-(1-cyanocyclopropyl)-4,4-difluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-norvalinamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.0000002
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(1-hydroxycyclopropyl)biphenyl-4-yl]ethyl]-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000021
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(1-hydroxycyclopropyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000002
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(2-hydroxypropan-2-yl)biphenyl-4-yl]ethyl]-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000002
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4-(4-methyl-4,5-dihydro-1,3-thiazol-2-yl)phenyl]ethyl]-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000003
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4-(quinolin-6-yl)phenyl]ethyl]-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000003
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4-[5-(1-hydroxycyclopropyl)pyridin-2-yl]phenyl]ethyl]-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000004
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4-[6-(methylsulfonyl)pyridin-3-yl]phenyl]ethyl]-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000004
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1R)-2,2-difluoro-1-hydroxyethyl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000004
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1S)-2,2-difluoro-1-hydroxyethyl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000016
N-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(2,2,2-trifluoro-1-hydroxyethyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
pH and temperature not specified in the publication
0.0000019
N-(1-cyanocyclopropyl)-N2-[(1S)-2,2-difluoro-1-[4'-(2,2,2-trifluoro-1-hydroxyethyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
pH and temperature not specified in the publication
0.026
N-(1-ethynylcyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
Homo sapiens
50 mM MES pH 5.5, 25 mM EDTA and 2.5 mM DTT. 0.05% Tween20 (v/v), 37°C
0.000009
N-(2,3-dichlorophenyl)triazolyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
Homo sapiens
-
IC50: 9 nM
0.000006
N-(2-chlorophenyl)triazolyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
Homo sapiens
-
IC50: 6 nM
0.000047
N-(3-bromoprop-2-yn-1-yl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
Homo sapiens
50 mM MES pH 5.5, 25 mM EDTA and 2.5 mM DTT. 0.05% Tween20 (v/v), 37°C
0.00014
N-(4-benzyl-1-methylpiperidin-4-yl)-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.000001
N-(4-chlorophenyl)-2-methylalanyl-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-L-leucinamide
Homo sapiens
-
IC50 is below 1 nM
0.000003
N-(5-isopropyl)pyridine-2-carboxyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
Homo sapiens
-
IC50: less than 3 nM
0.00000057
N-(cyanomethyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
Homo sapiens
50 mM MES pH 5.5, 25 mM EDTA and 2.5 mM DTT. 0.05% Tween20 (v/v), 37°C
0.000349
N-(cyanomethyl)-4-methyl-2-[3'-(2-piperazin-1-yl-1,3-thiazol-4-yl)biphenyl-3-yl]pentanamide
Homo sapiens
-
IC50: in vitro bone resorption assay
0.000059
N-(cyanomethyl)-4-methyl-2-[3'-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]biphenyl-3-yl]pentanamide
Homo sapiens
-
IC50: in vitro bone resorption assay
0.000012
N-(cyanomethyl)-4-methyl-2-[4'-(2-piperazin-1-yl-1,3-thiazol-4-yl)biphenyl-3-yl]pentanamide
Homo sapiens
-
IC50: in vitro bone resorption assay
0.0000002
N-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Homo sapiens
-
-
0.000000005
N-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(piperazin-1-yl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
Homo sapiens
IC50 below 5 pM, pH and temperature not specified in the publication
0.000006
N-4-benzyloxybenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
Homo sapiens
-
IC50: 6 nM
0.000003
N-4-isopropylbenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
Homo sapiens
-
IC50: less than 3 nM
0.000003
N-4-propylbenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
Homo sapiens
-
IC50: less than 3 nM
0.000015
N-benzyl-3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxamide
Homo sapiens
-
-
0.00035
N-but-3-yn-2-yl-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
Homo sapiens
50 mM MES pH 5.5, 25 mM EDTA and 2.5 mM DTT. 0.05% Tween20 (v/v), 37°C
0.0000002
N-cyano-N2-[4-[4-(piperazin-1-yl)phenyl]thiophen-3-yl]-L-leucinamide
Homo sapiens
pH and temperature not specified in the publication
0.000044
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.00019
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[(2-methyl-1H-imidazol-1-yl)acetyl]-L-leucinamide
Homo sapiens
-
IC50: 190 nM
0.000084
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[(4-phenylpiperidin-1-yl)acetyl]-L-leucinamide
Homo sapiens
-
IC50: 84 nM
0.000009
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[(4-pyridin-4-ylpiperazin-1-yl)acetyl]-L-leucinamide
Homo sapiens
-
IC50: 9 nM
0.000024
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[(5-methyl-1H-imidazol-4-yl)acetyl]-L-leucinamide
Homo sapiens
-
IC50: 24 nM
0.000001
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[2-(4-chlorophenoxy)-2-methylpropanoyl]-L-leucinamide
Homo sapiens
-
IC50 is below 1 nM
0.000001
N-[(1S)-1-([(1R)-2-(benzyloxy)-1-cyanoethyl]carbamoyl)-3-methylbutyl]-1-methyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50 is below 1 nM
0.00043
N-[(1S)-1-([(1R)-2-(benzyloxy)-1-cyanoethyl]carbamoyl)-3-methylbutyl]-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 430 nM
0.0002
N-[(1S)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.000151
N-[(1S)-1-carbamoyl-3-(methylsulfonyl)propyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Homo sapiens
-
-
0.000273
N-[(1S)-1-carbamoyl-3-phenylpropyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Homo sapiens
-
-
0.0000006
N-[(1S)-1-cyano-2-phenylethyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Homo sapiens
-
-
0.0000002
N-[(1S)-1-cyano-3-(methylsulfanyl)propyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Homo sapiens
-
-
0.0000009 - 0.0000012
N-[(1S)-1-cyanoethyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
0.000041
N-[(1S)-1-[2-(methylsulfanyl)ethyl]-2-oxopropyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Homo sapiens
-
-
0.000109
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-3-(methylsulfonyl)-L-alaninamide
Homo sapiens
-
-
0.000174
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-alaninamide
Homo sapiens
-
-
0.000013
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-methioninamide
Homo sapiens
-
-
0.00012
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-methionine
Homo sapiens
-
-
0.00001
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-phenylalaninamide
Homo sapiens
-
-
0.000277
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-(2,2,2-trifluoroethyl)-L-methioninamide
Homo sapiens
-
-
0.000238
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-(methylsulfonyl)-L-methioninamide
Homo sapiens
-
-
0.000087
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-benzyl-L-methioninamide
Homo sapiens
-
-
0.001045
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-dimethyl-L-methioninamide
Homo sapiens
-
-
0.000067
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-methyl-L-methioninamide
Homo sapiens
-
-
0.000066
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-S-methyl-L-cysteinamide
Homo sapiens
-
-
0.000238
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucylglycinamide
Homo sapiens
-
-
0.0000075
N-[(1S)-3-methyl-1-([(1S)-1-methyl-2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamoyl)butyl]-1-benzofuran-2-carboxamide
Homo sapiens
-
-
0.000016
N-[(1S)-3-methyl-1-[[3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]carbamoyl]butyl]-1-benzofuran-2-carboxamide
Oryctolagus cuniculus
-
-
0.0000068
N-[(2S)-1-[4-(benzyloxy)anilino]butan-2-yl]-N2-(morpholine-4-carbonyl)-L-leucinamide
Homo sapiens
pH and temperature not specified in the publication
0.000003
N-[(2S)-4-methyl-1-([2-[4-(2-methylpropoxy)anilino]ethyl]amino)-1-oxopentan-2-yl]-2,3-dihydro-1-benzofuran-2-carboxamide
Homo sapiens
IC50 below 3 nM, pH and temperature not specified in the publication
0.000015
N-[1-(benzylcarbamoyl)-4-oxopyrrolidin-3-yl]-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.000159
N-[1-(benzylsulfonyl)-3-oxoazepan-4-yl]-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.0000014
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(4-propylpiperazin-1-yl)benzamide
Homo sapiens
pH and temperature not specified in the publication
0.0000002
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.011
N-[2-[(4-methoxyphenyl)amino]ethyl]-1-(phenylamino)cyclohexanecarboxamide
Homo sapiens
-
-
0.0002
N-[2-[(4-methoxyphenyl)amino]ethyl]-1-[4-(1-methylethyl)phenoxy]cyclohexanecarboxamide
Homo sapiens
-
-
0.000016
N-[cyano(dicyclobutyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.0000003
N-[cyano(dicyclopropyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.0000006
N-[cyano(phenyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.00006
N2-(3-cyclohexylphenyl)-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-leucinamide
Homo sapiens
-
-
0.000011
N2-biphenyl-3-yl-N-[(1S)-1-[([4-[2-(1H-tetrazol-5-yl)ethoxy]phenyl]amino)methyl]propyl]-L-leucinamide
Homo sapiens
-
-
0.0000038
N2-biphenyl-3-yl-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]propyl]-L-leucinamide
Homo sapiens
-
-
0.00001
N2-biphenyl-3-yl-N-[(1S)-2-[(4-methoxyphenyl)amino]-1-methylethyl]-L-leucinamide
Homo sapiens
-
-
0.0000003
N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)-2'-fluorobiphenyl-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
Oryctolagus cuniculus
-
pH and temperature not specified in the publication
0.0000003
N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)-2'-fluorobiphenyl-4-yl]-2,2-difluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
Oryctolagus cuniculus
-
pH and temperature not specified in the publication
0.0000005
N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)biphenyl-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000002
N2-[(1S)-1-[4'-(2-amino-2-oxoethyl)[1,1'-biphenyl]-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000002
N2-[(1S)-1-[4'-[(2S)-1-amino-1-oxopropan-2-yl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000002
N2-[(1S)-1-[4-[5-(1-carbamoylcyclopropyl)pyridin-2-yl]phenyl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000043
N2-[(benzyloxy)carbonyl]-N-((1S)-1-cyano-2-[4-(trifluoromethyl)phenyl]ethyl)-L-leucinamide
Homo sapiens
-
IC50: 43 nM
0.000009
N2-[(benzyloxy)carbonyl]-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-L-leucinamide
Homo sapiens
-
IC50: 9 nM
0.00024
N2-[(benzyloxy)carbonyl]-N-[(1R)-2-tert-butoxy-1-cyanoethyl]-L-leucinamide
Homo sapiens
-
IC50: 240 nM
0.00012
N2-[(benzyloxy)carbonyl]-N-[(1S)-1-cyano-2-(3-methylphenyl)ethyl]-L-leucinamide
Homo sapiens
-
IC50: 120 nM
0.000063
N2-[(benzyloxy)carbonyl]-N-[(1S)-1-cyano-2-(4-methoxyphenyl)ethyl]-L-leucinamide
Homo sapiens
-
IC50: 63 nM
0.000048
N2-[(benzyloxy)carbonyl]-N-[(1S)-1-cyano-2-(4-methylphenyl)ethyl]-L-leucinamide
Homo sapiens
-
IC50: 48 nM
0.000398
N2-[(benzyloxy)carbonyl]-N-[(1S)-2-(4-tert-butoxyphenyl)-1-cyanoethyl]-L-leucinamide
Homo sapiens
-
IC50: 398 nM
0.00009
N2-[(benzyloxy)carbonyl]-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-leucinamide
Homo sapiens
-
-
0.000064
Nalpha-4-methoxybenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
Oryctolagus cuniculus
-
IC50: 64 nM
0.00047
Nalpha-benzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
Oryctolagus cuniculus
-
IC50: 470 nM
0.000047
Phe-Phe-fluoromethylketone
Homo sapiens
pH and temperature not specified in the publication
0.5
piperidin-2-yl-[2-(trifluoromethyl)-6-[4-(trifluoromethyl)phenyl]pyridin-4-yl] methanol
Homo sapiens
-
at pH 5.5 and 28°C
0.00083
S-(1-methylethyl) (2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazinecarbothioate
Homo sapiens
-
-
0.08
S-[2-[2-(dihydroxymethyl)anilino]-2-oxoethyl] carbamothioate
Homo sapiens
pH and temperature not specified in the publication
0.0093
sclareol
Homo sapiens
pH 5.5, 25°C, 3.7% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate
0.0000345
sodium (2S,3S)-3-[[(2S)-4-methyl-1-(2-methylpropoxy)pentan-2-yl]amino]oxirane-2-carboxylate
Homo sapiens
pH and temperature not specified in the publication
0.0272
sophoraflavanone G
Homo sapiens
pH and temperature not specified in the publication
0.005
suramin
Homo sapiens
pH 5.5, 25°C, 16.0% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate
0.000055
tert-butyl ([1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]carbamoyl)carbamate
Homo sapiens
-
pH 5.5, 30°C
0.0000039
tert-butyl 3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxylate
Homo sapiens
-
-
0.0000048
tert-butyl 3-(4-[[(2S)-2-([[1-(biphenyl-3-ylamino)cyclohexyl]carbonyl]amino)butyl]amino]phenoxy)propanoate
Homo sapiens
-
-
0.0000039
tert-butyl 3-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-4-oxopyrrolidine-1-carboxylate
Oryctolagus cuniculus
-
-
0.0000064
tert-butyl 3-[4-([(2S)-2-[(N-biphenyl-3-yl-L-leucyl)amino]butyl]amino)phenoxy]propanoate
Homo sapiens
-
-
0.00047
tert-butyl [(1S)-1-[(E)-(4,5-dihydro-1,3-thiazol-2-ylhydrazono)methyl]pentyl]carbamate
Homo sapiens
-
-
0.033
tert-butyl [(1S)-1-[(E)-(carbamimidoylhydrazono)methyl]pentyl]carbamate
Homo sapiens
-
-
0.000048
tert-butyl [(1S)-1-[(E)-[(2,3-dihydro-1H-indol-1-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.000093
tert-butyl [(1S)-1-[(E)-[(3,4-dihydroisoquinolin-2(1H)-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.000059
tert-butyl [(1S)-1-[(E)-[(3,4-dihydroquinolin-1(2H)-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.0002
tert-butyl [(1S)-1-[(E)-[(3-methylbutanoyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
IC50: 0.00016 mM (after addition of the semicarbazide in 15fold excess at pH 5.5) 0.011 mM (after addition of the semicarbazide in 15fold excess at pH 7.0)
0.00041
tert-butyl [(1S)-1-[(E)-[(benzylcarbamoyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.00004
tert-butyl [(1S)-1-[(E)-[(diethylcarbamoyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
IC50: 0.000047 mM (after addition of the semicarbazide in 15fold excess at pH 5.5) 0.0018 mM (after addition of the semicarbazide in 15fold excess at pH 7.0)
0.000072
tert-butyl [(1S)-1-[(E)-[(dimethylcarbamoyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.000072
tert-butyl [(1S)-1-[(E)-[(dimethylsulfamoyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
IC50: 0.00022 mM (after addition of the semicarbazide in 15fold excess at pH 5.5) 0.0019 mM (after addition of the semicarbazide in 15fold excess at pH 7.0)
0.00049
tert-butyl [(1S)-1-[(E)-[(ethylcarbamoyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
IC50: 0.0009 mM (after addition of the semicarbazide in 15fold excess at pH 5.5) above 0.013 mM (after addition of the semicarbazide in 15fold excess at pH 7.0)
0.00028
tert-butyl [(1S)-1-[(E)-[(methylcarbamoyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.000035
tert-butyl [(1S)-1-[(E)-[(morpholin-4-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
IC50: 0.00005 mM (after addition of the semicarbazide in 15fold excess at pH 5.5) 0.0021 mM (after addition of the semicarbazide in 15fold excess at pH 7.0)
0.0004
tert-butyl [(1S)-1-[(E)-[(phenylcarbamoyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.00022
tert-butyl [(1S)-1-[(E)-[(phenylcarbonyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.000058
tert-butyl [(1S)-1-[(E)-[(piperidin-1-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.000036
tert-butyl [(1S)-1-[(E)-[(pyrrolidin-1-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.00016
tert-butyl [(1S)-1-[(E)-[(tert-butylcarbamoyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.000024
tert-butyl [(1S)-1-[(E)-[(trifluoroacetyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.011
tert-butyl [(1S)-1-[(E)-[methyl[(2-phenylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.00052
tert-butyl [(1S)-1-[(E)-[methyl[methyl(2-phenylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.00017
tert-butyl [(1S)-1-[(E)-[[(1-methylethyl)carbamothioyl]hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.00017
tert-butyl [(1S)-1-[(E)-[[(1-methylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.00026
tert-butyl [(1S)-1-[(E)-[[(2-phenylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.0011
tert-butyl [(1S)-1-[(E)-[[(morpholin-4-ylcarbonyl)oxy]imino]methyl]pentyl]carbamate
Homo sapiens
-
-
0.000045
tert-butyl [(1S)-1-[(E)-[[methyl(2-phenylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.000001
[1-(2-cyano-tetrahydro-pyridazine-1-carbonyl)-2-methyl-propyl]-carbamic acid benzyl ester
Homo sapiens
-
pH 5.5, 30°C
additional information
(3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetic acid
0.0000005
(1R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
Homo sapiens
-
-
0.0000005
(1R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.000009
(1R,2R)-2-[1-benzyl-5-[4-(methylsulfanyl)phenyl]-1H-1,2,3-triazol-4-yl]-N-(cyanomethyl)-5,5-difluorocyclohexanecarboxamide
Homo sapiens
-
-
0.000009
(1R,2R)-2-[1-benzyl-5-[4-(methylsulfanyl)phenyl]-1H-1,2,3-triazol-4-yl]-N-(cyanomethyl)-5,5-difluorocyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.000002
(1R,2R)-N-(cyanomethyl)-2-(4-[4-[(difluoromethyl)sulfanyl]phenyl]pyridin-3-yl)-5,5-difluorocyclohexanecarboxamide
Homo sapiens
-
-
0.000002
(1R,2R)-N-(cyanomethyl)-2-(4-[4-[(difluoromethyl)sulfanyl]phenyl]pyridin-3-yl)-5,5-difluorocyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.0000004
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[1-methyl-4-[4-(methylsulfanyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
Homo sapiens
-
-
0.0000004
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[1-methyl-4-[4-(methylsulfanyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.00000041
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[1-methyl-4-[4-(methylsulfanyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.0000001
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-methyl-4-[4-(methylsulfanyl)phenyl]-1,3-thiazol-5-yl]cyclohexanecarboxamide
Homo sapiens
-
-
0.0000001
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-methyl-4-[4-(methylsulfanyl)phenyl]-1,3-thiazol-5-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.000001
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-[4-(methylsulfanyl)phenyl]pyridin-3-yl]cyclohexanecarboxamide
Homo sapiens
-
-
0.000001
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-[4-(methylsulfanyl)phenyl]pyridin-3-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.000005
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-1-oxidopyridin-4-yl]cyclohexanecarboxamide
Homo sapiens
-
-
0.000005
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-1-oxidopyridin-4-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.000006
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.000008
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
Homo sapiens
-
-
0.000001
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]pyridin-4-yl]cyclohexanecarboxamide
Homo sapiens
-
-
0.000001
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]pyridin-4-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.0000003
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
Homo sapiens
-
-
0.0000003
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.00000032
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.000004
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[5-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
Homo sapiens
-
-
0.000005
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[5-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.0000018
(2S)-4-fluoro-4-methyl-N-(3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.000002
(2S)-4-fluoro-4-methyl-N-(3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
racemate
0.00000077
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1H-pyrazol-5-ylamino)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 0.77 nM
0.000013
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1H-pyrazol-5-ylamino)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 13 nM
0.000015
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
Homo sapiens
-
IC50: 15 nM
0.00079
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 790 nM
0.000062
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-2-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
Homo sapiens
-
IC50: 62 nM
0.0012
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-2-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 0.0012 mM
0.000025
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-4-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
Homo sapiens
-
IC50: 25 nM
0.00047
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-4-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 470 nM
0.00000065
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(3-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
Homo sapiens
-
IC50: 0.65 nM
0.000012
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(3-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 12 nM
0.00000021
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(4-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
Homo sapiens
-
IC50: 0.21 nM
0.0000018
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(4-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 1.8 nM
0.000015
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 15 nM
0.0011
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 0.0011 mM
0.000022
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclohexyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 22 nM
0.0012
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclohexyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 0.0012 mM
0.00002
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclopentyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 20 nM
0.0011
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclopentyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 0.0011 mM
0.000026
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-ethyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 26 nM
0.0015
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-ethyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 0.0015 mM
0.000039
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 39 nM
0.0027
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 0.0027 mM
0.000017
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isopropyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 17 nM
0.001
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isopropyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 0.001 mM
0.00000041
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-3-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 0.41 nM
0.000011
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-3-yl)amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 11 nM
0.000032
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 32 nM
0.0017
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 0.0017 mM
0.00000047
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 0.47 nM
0.0000055
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 5.5 nM
0.000062
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(3,3-dimethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 62 nM
0.0016
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(3,3-dimethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 0.0016 mM
0.000027
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(cyclopropylmethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 27 nM
0.0017
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(cyclopropylmethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 0.0017 mM
0.0088
2-(2,4-dihydroxyphenyl)-5,7-dihydroxy-6-[5-methyl-2-(prop-1-en-2-yl)hex-4-en-1-yl]-2,3-dihydro-4H-1-benzopyran-4-one
Homo sapiens
pH and temperature not specified in the publication
0.02724
2-(2,4-dihydroxyphenyl)-5,7-dihydroxy-6-[5-methyl-2-(prop-1-en-2-yl)hex-4-en-1-yl]-2,3-dihydro-4H-1-benzopyran-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00000001
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
-
-
0.00001
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.000000022
2-cyano-4-(cyclohexylamino)-N-[2-(4-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000022
2-cyano-4-(cyclohexylamino)-N-[2-(4-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000000047
2-cyano-4-(cyclohexylamino)-N-[2-[4-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000047
2-cyano-4-(cyclohexylamino)-N-[2-[4-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000000003
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[4-[2-(1H-imidazol-1-yl)ethoxy]phenyl]ethyl)pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000003
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[4-[2-(1H-imidazol-1-yl)ethoxy]phenyl]ethyl)pyrimidine-5-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000000003
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-(4-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
value below 0.000000003 mM
0.000003
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-(4-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
IC50 less than 0.000003 mM, pH and temperature not specified in the publication
0.000000025
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-[4-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000025
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-[4-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
4-(cyclohexylamino)-6-(piperazin-1-yl)-1,3,5-triazine-2-carbonitrile
Homo sapiens
pH and temperature not specified in the publication
0.000004
4-(cyclohexylamino)-6-(piperazin-1-yl)-1,3,5-triazine-2-carbonitrile
Homo sapiens
pH and temperature not specified in the publication
0.0001
4-cycloheptyl-6-[3-(piperidin-1-yl)propyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0001
4-cycloheptyl-6-[3-(piperidin-1-yl)propyl]pyrimidine-2-carbonitrile
Homo sapiens
pH and temperature not specified in the publication
0.015
4-dihydrotanshinone
Homo sapiens
with collagen type I as substrate, at pH 5.5 and 37°C
0.00022
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0022
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000017
6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000017
6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0001
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00011
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000006
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000006
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
7-(2,2-dimethyl-propyl)-6-(1,3-dioxo-2,8-diaza-spiro[4.5]dec-2-ylmethyl)-7H-pyrrolo[2,3-d] pyrimidine-2-carbonitrile
Homo sapiens
-
below
0.00003
7-(2,2-dimethyl-propyl)-6-(1,3-dioxo-2,8-diaza-spiro[4.5]dec-2-ylmethyl)-7H-pyrrolo[2,3-d] pyrimidine-2-carbonitrile
Rattus norvegicus
-
-
0.000001
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
below
0.000001
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.000076
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
-
-
0.000001
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
below
0.000001
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.000001
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-3-propyl-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
below
0.000001
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-3-propyl-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.000001
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-8-propyl-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
below
0.000001
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-8-propyl-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.000027
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-8-propyl-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
-
-
0.000001
7-(2,2-dimethylpropyl)-6-[(3-methyl-2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
below
0.000001
7-(2,2-dimethylpropyl)-6-[(3-methyl-2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.000012
7-(2,2-dimethylpropyl)-6-[(3-methyl-2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
-
-
0.0000017
7-(2,2-dimethylpropyl)-6-[(5-fluoro-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000017
7-(2,2-dimethylpropyl)-6-[(5-fluoro-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000078
7-(2,2-dimethylpropyl)-6-[(5-fluoro-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
-
-
0.000001
7-(2,2-dimethylpropyl)-6-[(5-methoxy-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
below
0.000001
7-(2,2-dimethylpropyl)-6-[(5-methoxy-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.000044
7-(2,2-dimethylpropyl)-6-[(5-methoxy-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
-
-
0.0000014
balicatib
Homo sapiens
-
pH and temperature not specified in the publication
0.0000006
benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate
Homo sapiens
-
pH and temperature not specified in the publication
0.000035
benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000044
benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate
Mus musculus
-
pH and temperature not specified in the publication
0.000013
Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z
Homo sapiens
-
pH and temperature not specified in the publication
0.000269
Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000296
Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z
Mus musculus
-
pH and temperature not specified in the publication
0.000181
dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate
Homo sapiens
-
pH and temperature not specified in the publication
0.002588
dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00426
dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate
Mus musculus
-
pH and temperature not specified in the publication
0.0000002
L-873724
Oryctolagus cuniculus
-
pH and temperature not specified in the publication
0.0000023
Mu-Leu-Hph-fluoromethylketone
Homo sapiens
-
pH and temperature not specified in the publication
0.0000076
Mu-Leu-Hph-fluoromethylketone
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000018
Mu-Leu-Hph-fluoromethylketone
Mus musculus
-
pH and temperature not specified in the publication
0.0000024
N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
Mus musculus
-
recombinant cathepsin K
0.000028
N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
Homo sapiens
-
at the cellular level in human osteoclasts
0.0000006
N-(1-cyano-2-phenylethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.0000051
N-(1-cyano-2-phenylethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.0000009
N-[(1S)-1-cyanoethyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Homo sapiens
-
-
0.0000012
N-[(1S)-1-cyanoethyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.0000002
odanacatib
Homo sapiens
-
pH and temperature not specified in the publication
0.0000002
odanacatib
Oryctolagus cuniculus
-
pH and temperature not specified in the publication
0.00000056
odanacatib
Homo sapiens
50 mM MES pH 5.5, 25 mM EDTA and 2.5 mM DTT. 0.05% Tween20 (v/v), 37°C
additional information
(3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetic acid
Homo sapiens
-
KI value is above 5 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 not detected
additional information
2-cyano-4-[[(4,4-dimethylcyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
IC50 is above 0.003 mM, inhibition is determined by a fluorometric assay with recombinant Cat K
additional information
2-cyano-N-(1-methyl-4-phenylpiperidin-4-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 not detected
additional information
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 is above 0.003 mM, inhibition is determined by a fluorometric assay with recombinant Cat K
additional information
2-cyano-N-(4,5-dimethoxybiphenyl-2-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 is above 0.001 mM, inhibition is determined by a fluorometric assay with recombinant Cat K
additional information
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 not detected
additional information
2-cyano-N-[(1R)-2-pyridin-2-yl-1-(pyrrolidin-1-ylmethyl)ethyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 not detected
additional information
2-cyano-N-[5-[(1-methylpiperidin-4-yl)oxy]biphenyl-2-yl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 not detected
additional information
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzoic acid
Homo sapiens
-
KI value is above 2 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-(4-chlorobenzyl)-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is below 1 nM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-(4-chlorobenzyl)-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-(4-chlorobenzyl)-7-(2-cyclooctylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-(4-chlorobenzyl)-7-(2-piperidin-1-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-(4-chlorobenzyl)-7-(3,3-dimethylbutyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is below 1 nM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-(4-chlorobenzyl)-7-[2-(3-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-(4-chlorobenzyl)-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-[[4-(1-acetyl-1,2,3,6-tetrahydropyridin-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-[[4-(1-acetylpiperidin-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
-
IC50 is above 0.01 mM, Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)-3-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 is above 1 M, with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 is above 2 M, with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
-
IC50 is above 0.01 mM, Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1.5 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
-
IC50 is above 0.01 mM, Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 is above 1 M, with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
additional information
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
7-(2-cyclohexylethyl)-6-[[methyl(phenyl)amino]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
additional information
Mus musculus
-
Ulmus diviana stem bral extracts show an IC50 of 0.0875 mg/ml
-
additional information
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetamide
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)propanamide
Homo sapiens
-
KI value is above 1.5 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 not detected
additional information
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)oxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 not detected
additional information
N-benzyl-2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 not detected
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
0.007 - 0.014
-
substrate benzyloxycarbonyl-Phe-Arg 4-methylcoumarin 7-amide, procathepsin K
15 - 25
-
substrate benzyloxycarbonyl-Phe-Arg 4-methylcoumarin 7-amide, mature enzyme
additional information
additional information
-
cathepsin K activity is confirmed in dendritic cells
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
5 - 6
5.5
6 - 7.4
-
kcat/Km with 2-aminobenzoyl-RPPGFSPFR-(3-nitrotyrosine) is 1.4fold higher at pH 6.0 than at pH 7.4
6.5
additional information
-
CatK is a lysosomal cysteine protease that degrades type I collagen at neutral and acidic pH
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
pH RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
25
25 - 37
28
37
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
30353, 30354, 30355, 30356, 30357, 30359, 30360, 30361, 30363, 30366, 30367, 30368, 647953, 647964, 647972, 652733, 654410, 654565
-
-
brenda
-
668393, 669364, 669563, 669625, 669757, 669795, 669982, 670870, 677816, 678499, 679251, 681251, 681252, 685560, 685561, 685563, 685564, 685569, 688262, 695456, 695609, 695943, 696041, 696617, 696630, 696631
-
-
brenda
-
698935, 699441, 699442, 699557, 699723, 699918, 699971, 700689, 701297, 707120, 707295, 707615, 707694, 707695, 707712, 707715, 707873, 707899, 708205, 708260, 708261, 708262, 708388, 708423, 708429, 708450, 708541, 708572, 708689, 709307, 709409, 709794, 709855, 710073, 710231, 717159, 717214
-
-
brenda
expressed in Sf9 cells with Autographa californica nuclear polyhedrosis virus
-
-
brenda
recombinant enzymes, expressed in Sf21 cells, baculovirus-infected, wild-type and mutant enzyme in which Cys139 is changed to Ser
-
-
brenda
-
30362, 30369, 667131, 667486, 670870, 677895, 682861, 697011, 697150, 697619, 700688, 707334, 707615, 708148, 731902
-
-
brenda
C57BL/6 mice either wild-type for cathepsin K, CK+/+, heterozygous for cathepsin K, CK+/-, or deficient in cathepsin K, CK-/-, all transgenically expressing human tumor necrosis factor
-
-
brenda
-
-
-
brenda
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
it is shown by fluorescence microscopy of plaque sections from using human carotid endarterectomy specimens that enzymatically active CatK (positive NIRF signal) localizes primarily in the vicinity of CatK-positive macrophages. Augmented NIRF signal (reflecting CatK activity) colocalizes with disrupted elastin fibers within the media underlying plaques
brenda
-
biopsy sites, benign lesions, ductal carcinoma in situ, and invasive breast tumors of different stages. Neither epithelial nor stromal expression of CTSK is significantly associated with recurrence-free or overall survival
brenda
-
left anterior descending coronary arteries with different degrees of atherosclerotic lesions, cathepsin K co-localizes with collagen type I in advanced atherosclerotic lesions especially at the plaque shoulders
brenda
-
in the dermis, cathepsin K is expressed only under certain circumstances such as scarring or inflammation
brenda
cathepsin K, the chemo-attractant stromal-derived factor-1alpha and its C-X-C receptor type 4 are localized in therapy-resistant glioma stem-like cell (GSLC) niches in glioblastoma
brenda
-
increased numbers of cathepsin K immunoreactive cells are found in left and right arcuate nucleus of schizophrenics
brenda
-
in stroma of pulmonary adenocarcinomas, cathepsin K expression is restricted to the desmoplastic fibrous tissue of invasive components, no expression in bronchioloalveolar carcinoma
brenda
-
immunostaining reveals strong catK expression in most primary melanomas and all cutaneous melanoma metastases. Melanocytic nevi also demonstrates catK expression, but it is less intense than in melanomas. Melanoma lines express both the pro- and the active form of catK
brenda
on the dental root side, expression pattern of cathepsin K, high expression level in the age of 4-5 weeks, when physiological root resorption occurs actively, co-expression with matrix metalloproteinase-9
brenda
-
inflamesynovial tissue associated with rheumatoid arthritis
brenda
additional information
-
visceral, cathepsin K activity gradually increases in the process of adipocyte differentiation
brenda
-
cathepsin K is increased by a suppressive L-thyroxine therapy and decreases with increasing age, overview
brenda
-
cathepsin K probe localizes adjacent to newly mineralizing bone in vivo
brenda
-
from ankylosing spondylitis and degenerative disc disease patients, strong expression in the different regions of the spine. Cathepsin K-positive multinucleated cells are located at sites of bone destruction, overview
brenda
-
cathepsin K probe localizes adjacent to newly mineralizing bone in vivo
brenda
-
articluar, from the metacarpophalangeal and healthy joints, immunohistochemic identification in different regions of the tissue from healthy and osteoarthritic animals, overview
brenda
-
osteoarthritic and nonarthritic femoral condylar articular, and normal articular
brenda
at 3 h post-challenge with Aeromonas hydrophila, the cathepsins K expression is seen only in the heart
brenda
lowest expression level of all the examined tissues
brenda
-
cathepsin K transcripts are highly increased in the lungs after silica treatment compared to cathepsin S, L and B. The upregulation is specific for the fibrotic process
brenda
-
qunatitative determination of enzyme content by immunohistochemistry, real time RT-PCR and western blotting
brenda
-
qunatitative determination of enzyme content by immunohistochemistry, real time RT-PCR and western blotting
-
brenda
-
cathepsin K is downregulated by the profibrotic growth factor TGF-beta1
brenda
-
fibroblasts from patients with lung fibrosis contain more cathepsin K activity than those from normal lungs
brenda
-
cathepsin K is downregulated by the profibrotic growth factor TGF-beta1
brenda
-
primary lung fibroblasts derived from CTSK-/- mice show a decreased collagenolytic activity
brenda
osteoblast-like culture. Osteoblastic cathepsin K may contribute to collagenous matrix maintenance and recycling of improperly processed collagen I
brenda
-
-
30355, 30361, 30365, 30366, 654410, 656456, 656457, 656472, 657251, 696654, 697010, 697257, 697775, 698935, 699557, 707899, 708260, 708689, 709855, 717159
brenda
-
cathepsin K, colocalizes with tartrate-resistant acid phosphatase in osteoclast-resorptive compartments, supporting a role for cathepsin K in the extracellular processing of monomeric tartrate-resistant acid phosphatase in the resorption lacuna
brenda
-
cathepsin K is one of the cysteine proteases expressed by osteoclasts, particularly at the cell surface adjacent to bone
brenda
-
cathepsin K is secreted by osteoclasts, when they are resorbing bone
brenda
-
from either wild-type for cathepsin K, CK+/+, heterozygous for cathepsin K, CK+/-, or deficient in cathepsin K, CK-/-, mice, phenotypes, overview
brenda
localized on the surface of alveolar bone, expression pattern of cathepsin K, no co-expression with matrix metalloproteinase-9
brenda
-
subcutaneous, the enzyme content is increased by 12fold during adipogenesis
brenda
-
cathepsin K levels are not significantly increased in serum of patients with ankylosing spondylitis, 6.41 pg/ml in patients and 3.64 pg/ml in healthy controls, overview
brenda
-
normal skin shows only low levels or no expression of cathepsin K. Dermal fibroblasts in surgical scars shows strong cytoplasmatic expression of cathepsin K. Expresson is most prominent in young scars and declines with time
brenda
-
cultured neonatal primary fibroblasts show strong cathepsin K staining in the perinuclear endosomal compartment
brenda
In goldfish at 6 h post-infection, the cathepsin K is found all the tissues, except in the spleen
brenda
highest expression level of all the examined tissues
brenda
-
stromal CTSK expression is significantly higher in invasive compared to in situ carcinomas
brenda
additional information
-
not in cell lines: promyelotic leukemia (HL-60), lymphoblastic leukemia (MOLT-4), Burkitt's lymphoma, lung carcinoma (A549), melanoma G361
brenda
additional information
-
cathepsin is also found to be strongly expressed in keloids and in dermatofibromas, but not in sclerotic areas of morphea
brenda
additional information
-
high cathepsin K levels in men with differentiated thyroid cancer on suppressive L-thyroxine therapy, overview
brenda
additional information
-
media from cells on plastic show higher CatK activation than cells on dentin, consistent with cellular expression of cathepsin K mRNA, 2fold upregulation of cathepsin K mRNA from cells cultured on plastic correlates with increased cathepsin K activation, overview
brenda
additional information
-
media from cells on plastic show higher CatK activation than cells on dentin, consistent with cellular expression of cathepsin K mRNA, 2fold upregulation of cathepsin K mRNA from cells cultured on plastic correlates with increased cathepsin K activation, overview
brenda
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
additional information
-
the enzyme is almost exclusively colocalized with Lamp-I, a common lysosomal marker in perinuclear areas and in the protrusion of fibroblasts
-
brenda
-
cathepsin K is secreted by osteoclasts, when they are resorbing bone
-
brenda
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
malfunction
metabolism
physiological function
malfunction
-
catK deficiency has major impact on various vasculopathies, catK deficiency does not protect against aneurysm formation nor does it affect medial elastin breaks, cathepsin K deficiency with angiotensin II infusion increases granulocyte population and activates T cell numbers
malfunction
-
down-regulation of cathepsin K in synovium at the initial stage of osteoarthritis significantly accelerates cartilage degeneration
malfunction
-
ablation of cathepsin K mitigates injury-induced neointimal hyperplasia. Smooth muscle cell movement is impaired in enzyme-deficient mice. Enzyme inhibition alleviates vascular remodeling. Enzyme deficiency also impairs the smooth muscle cell proliferation ability induced by platelet-derived growth factor-BB. Enzyme deficiency impairs inflammatory action in response to injury
malfunction
-
specific cathepsin K knockdown significantly reduces HSC-3 cell invasion in the myoma organotypic invasion model
metabolism
cathepsin K can cleave and activate MMP-9 in acidic environments such as seen in tumors and during bone resorption
metabolism
the enzyme accounts for the increase in bone resorption in metabolic bone disorders such as postmenopausal osteoporosis
physiological function
-
cathepsin K acts as the major collagenase responsible for the degradation of the organic bone matrix during the bone remodeling process
physiological function
-
cathepsin K expression is essential for normal bone resorption
physiological function
-
cathepsin K has a pivotal function in bone matrix degradation
physiological function
-
cathepsin K is a potent extracellular matrix degrading enzyme that plays a critical role in osteoclast-mediated bone resorption
physiological function
-
cathepsin K is involved in osteoclast-mediated bone resorption
physiological function
-
cathepsin K is the major enzyme involved in bone resorption, associated with obesity and inflammation, major contributor to skeletal and vascular health, Cathepsin K plays a functional role in atherogenesis
physiological function
cathepsin K may play a role in the immune system of fish skin and muscle, in addition to its principal bone-specific function as a collagenolytic enzyme
physiological function
-
cathepsin K may significantly contribute to altered opioid levels in brains of schizophrenics
physiological function
-
cathepsin K plays a protective role in cartilage degeneration at the initial stage of osteoarthritis
physiological function
-
cathepsin K plays a role in intracellular collagen degradation after endocytosis
physiological function
-
cathepsin K plays a role in skeletal development/bone turnover, lung homeostasis, skin homeostasis during scar formation, amyloidosis, thyroid carcinoma, artherosclerosis/cardiovascular disease, breast carcinoma, lung adenocarcinoma, osteoporosis, prostate cancer, bone metastases, obesity, rheumatoid arthritis, osteoarthritis, melanoma, memory disorders, lung inflammation/fibrosis, and pycndysostosis
physiological function
-
cathepsin K-mediated intracellular elastin degradation may play a role in the formation of solar elastosis
physiological function
-
human macrophage foam cells degrade atherosclerotic plaques though cathepsin K-mediated processes, resulting in increase in levels of C-terminal fragments of type I collagen
physiological function
-
cathepsin K in the invasive tumor microenvironment front has a protective role in the complex progression of tongue cancer
physiological function
-
cathepsin K preferentially solubilizes matured bone matrix
Show AA Sequence and Transmembrane Helices (603 entries)
Please use the AA Sequence and Transmembrane Helices Search for a specific query.
Please use the AA Sequence and Transmembrane Helices Search for a specific query.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
PDB
SCOP
CATH
UNIPROT
ORGANISM
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
23500
29000
35000
-
procathepsin K, mature enzyme produced by incubation at pH 4.0, 24 h, 4°C, gel filtration
35300
36370
-
procathepsin K, MALDI-Mass spectromety, procathepsin K is autocatalytically activated at 4 C, pH 4, the activation is enhanced by 1% mature cathepsin K, cleavage of procathepsin K after Ala15
37000
23500
-
cathepsin O2, identical with cathepsin K in sequence, calculation from amino acid sequence
23500
-
1 * 35300, procathepsin K, 1 * 23500, mature enzyme, calculation from amino acid sequence without sugar chains
35300
-
procathepsin K, calculation from amino acid sequence, procathepsin K is autocatalytically activated at 4 C, pH 4, the activation is enhanced by 1% mature cathepsin K, cleavage of procathepsin K after Ala15
35300
-
1 * 35300, procathepsin K, 1 * 23500, mature enzyme, calculation from amino acid sequence without sugar chains
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
monomer
additional information
monomer
-
1 * 35300, procathepsin K, 1 * 23500, mature enzyme, calculation from amino acid sequence without sugar chains
additional information
the human sequence contains Asp and Tyr at S3 positions 61 and 67, and residues Met, Ala, Leu, Ala and Leu at S2 positions 68, 134, 160, 163, and 209, respectively, comparison with the rat enzyme
additional information
-
the human sequence contains Asp and Tyr at S3 positions 61 and 67, and residues Met, Ala, Leu, Ala and Leu at S2 positions 68, 134, 160, 163, and 209, respectively, comparison with the rat enzyme
additional information
the human sequence contains Tyr at S3 positions 61 and 67, and residues Met, Ser, Val, Ala, and Leu at S2 positions 68, 134, 160, 163, and 209, respectively, comparison with the human enzyme
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
glycoprotein
proteolytic modification
glycoprotein
-
sugars comprise 3% of the enzyme mass, Asn103 is the only site of glycosylation
glycoprotein
-
one of the two putative N-linked glycosylation sites is located in the propeptide and the other is in the mature protease
proteolytic modification
-
cathepsin K is synthesized as an inactive pre-proenzyme
proteolytic modification
-
the recombinant proenzyme is activated by cleavage through pepsin
proteolytic modification
-
trypsin cleaves at the cathepsin K recognition site activating cathepsin K
proteolytic modification
-
processing of the proenzyme for activation involving reentry and delivery of proenzyme into lysosome which is enhanced by mannose-6-phosphate and mediated by the mannose-6-phosphate receptor, overview
proteolytic modification
-
trypsin cleaves at the cathepsin K recognition site activating cathepsin K
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
crystal structure of enzyme-inhibitor complex, inhibitor: N-[1S-(2-phenylethyl)-3-phenylsulfonylallyl]-4-methyl-2R-piperazinyl carbonylaminovaleramide, i.e. APC3328
-
in complex with NSC13345, sitting drop vapor diffusion method, using 0.2 M ammonium sulfate, pH 5.5, 30% (w/v) PEG-8000
mutant K9E/I171E/Q172S/N190M/K191G/L195K (E-64 inhibited) in complex with the 17000 Da fraction of chondroitin 4-sulfate, hanging drop vapor diffusion method, using 30% (v/v) 2-methyl-2,4-pentanediol, 0.1 M sodium acetate buffer, pH 4.5, and 20 mM CaCl2
purified and activated, recombinant cathepsin K in complex with chondroitin sulfate in presence or absence of inhibitor E64, which prevents autocatalytic cleavage of cathepsin K, 25 mg/ml enzyme-inhibitor complex of ratio 1:1 in 50 mM sodium acetate buffer, pH 5.5, hanging drop vapor diffusion method, mixing with an equal volume of reservoir solution containing 30% v/v 2-methyl-2,4-pentanediol, 0.1 M sodium acetate buffer, pH 4.5, and 20 mM calcium chloride, macroseeding, X-ray diffraction structure determination and analysis at 1.8 A resolution
-
the overall organization of the catalytic site, which consists of two domains folds together to give a V-shaped active site cleft configuration. The central helix is the most prominent feature of the left domain, whereas the right domain is mostly dominated by beta-barrel motifs (5-6 strands). The active site lies at the interface between the two domains
-
crysallized from 20% MPD, 0.1 M Tris, pH 7 and 0.1 M MES, pH 6, crystals were flash frozen in a nitrogen stream after increasing the MPD concentration to aproximately 30%
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
G243E
-
the missense mutation is associated with autosomal recessive pycnodysostosis
K9E
the mutant shows decreased catalytic efficiencies towards Z-Leu-Arg-7-amido-4-methylcoumarin and Z-Gly-Pro-Arg-7-amido-4-methylcoumarin compared to the wild type enzyme
K9E/I171E/Q172S
the mutant shows decreased catalytic efficiency towards Z-Leu-Arg-7-amido-4-methylcoumarin and increased catalytic efficiency towards Z-Gly-Pro-Arg-7-amido-4-methylcoumarin compared to the wild type enzyme
K9E/I171E/Q172S/N190M/K191G/L195K
the mutant shows decreased catalytic efficiency towards Z-Leu-Arg-7-amido-4-methylcoumarin and increased catalytic efficiency towards Z-Gly-Pro-Arg-7-amido-4-methylcoumarin compared to the wild type enzyme
K9E/N190M/K191G/L195K
the mutant shows increased catalytic efficiency towards Z-Leu-Arg-7-amido-4-methylcoumarin and decreased catalytic efficiency towards Z-Gly-Pro-Arg-7-amido-4-methylcoumarin compared to the wild type enzyme
N190M/K191G/L195K
the mutant shows increased catalytic efficiencies towards Z-Leu-Arg-7-amido-4-methylcoumarin and Z-Gly-Pro-Arg-7-amido-4-methylcoumarin compared to the wild type enzyme
Q187P
-
a naturally occurring mutant gene, the c.684 A-C point mutation in exon 5 of the CTSK gene results in the typical clinical features found in Chinese patients with pycnodysostosis
Y67L/L205A
Y61D/V157L
-
corresponding to the amino acid at that position in human enzyme, yields an enzyme with kinetic constants and inhibitor specificity profiles equivalent to human ortholog
S134A
site-directed mutagenesis of the rat residue Ser to the correspondent Ala of the human sequence, the mutant looses the P2 Hyp specificity
S134A/V160L
site-directed mutagenesis of the rat residues Ser and Val to the correspondent Ala and Leu, respectively, of the human sequence, the mutant looses the P2 Hyp specificity
V160L
site-directed mutagenesis of the rat residue Val to the correspondent Leu of the human sequence, the mutant looses the P2 Hyp specificity
additional information
Y67L/L205A
-
10fold lower interaction with inhibitor stefin B (Ki: 0.0000000008) suggesting that Tyr67 and Leu205 are critical for interaction with stefin B. Inhibitor cystatin C Ki: 0.0000000087, inhibitor L-kininogen Ki: 0.0000000135, inhibitor H-kininogen Ki: 0.0000000145
Y67L/L205A
-
this mutant fails to degrade bradykinin, indicating that Tyr67 and Leu205 are key active site residues for the kinin degrading activity of cathepsin
Y67L/L205A
-
2-aminobenzoyl-RP-PGFSPFR-(3-nitrotyrosine) is not cleaved by the the mutant enzyme
additional information
-
determination of six naturally occuring mutations in cathepsin K: an A-G transition at cDNA position 1095, a G-C transition at nucleotide 541, a C-T transition at nucleotide, a C-T transition at nucleotide 935, a G-A transition at nucleotide 236, and a T-C transition at nucleotide 926, overview
additional information
site-directed mutagenesis of the rat residues Ser and Val to the correspondent Ala and Leu, respectively, of the human sequence causes a loss of the P2 Hyp specificity, overview
additional information
-
site-directed mutagenesis of the rat residues Ser and Val to the correspondent Ala and Leu, respectively, of the human sequence causes a loss of the P2 Hyp specificity, overview
additional information
-
targeted disruption of cathepsin K results in defective Toll-like receptor 9 signaling in dendritic cells in response to unmethylated CpG DNA, which in turn leads to an attenuated induction of T helper 17 cells, without affecting the antigen-presenting ability of dendritic cells
additional information
-
the effects of cathepsin K deficiency (ctsK-/-) on atherosclerotic plaque formation in brachiocephalic arteries in an aggressive atherosclerosis model using apoE-deficient mice on cholate-containing high fat diet is examined. Cathepsin K deficiency appears to increase lesion stability in brachiocephalic arteries by maintaining the integrity of the tunica media and by decreasing plaque vulnerability to rupture
additional information
-
10-week-old male cathepsin K-deficient knockout mice show bones that are mechanically more brittle, while both osteoclasts and osteoblasts show impaired activity relative to the wild type, phenotype with significant hypercalcification of the calcified cartilage and cortices, overview
additional information
-
bone marrow transplantation for selective disruption of CatK in the haematopoietic system, usage of total bone marrow progenitor cells from CatK-/-, CatK-/+, and CatK+/+, and low-density lipoprotein receptor knockout mice. Silencing of leucocyte CatK results in phenotypic changes in bone formation with an increased total bone mineral density in the CatK2/2 chimeras, effect of leucocyte cathepsin K deficiency on bone remodelling, overview
additional information
-
catK-deficient cells show a similar suppression of actin rings as wild-type osteoclasts treated with inhibitor LHVS
additional information
-
construction of male and female wild-type, heterozygous, and homozygous CatK null mice, phenotypes in young mice, bone mass, strength, resorption, and formation, overview. CatK-/- mice show higher bone mineral density at the central and distal femur. Central femur ultimate load is positively influenced by genotype, and is positively correlated with both cortical area and bone mineral content. Lumbar vertebral body ultimate load is also positively correlated to bone mineral content. Genotype does not influence the relationship of ultimate load to bone mineral content in either the central femur or vertebral body
additional information
-
construction of transgenic UTU17 mice, overexpression of cathepsin K accelerates the resorption cycle and osteoblast differentiation in vitro, cathepsin K overexpression enhances osteogenesis and induces the formation of exceptionally small, actively resorbing osteoclasts from their bone marrow precursors in vitro, intracellular mechanisms, overview. The number of cathepsin K-containing vesicles in UTU17+/+ osteoclasts is highly increased
additional information
-
enzyme deficiency leads to blocked adipogenesis in 3T3-L1 preadipocytes, while CatK overexpression leads to enhanced adipogenesis, phenotypes, overview
additional information
-
overexpression of cathepsin K in mice decreases collagen deposition and lung resistance in response to bleomycin-induced pulmonary fibrosis, overview. Cathepsin K protein levels are strongly increased in alveolar macrophages and lung parenchymal tissue of mock-treated cathepsin K transgenic mice relative to wild-type mice
additional information
-
phenotype comparisons of C57BL/6 mice either wild-type for cathepsin K, CK+/+, heterozygous for cathepsin K, CK+/-, or deficient in cathepsin K, CK-/-, no influence of cathepsin K deficiency on the severity of inflammation in arthritic knee joints, overview, Maintenance of the osteopetrosis phenotype of cathepsin K-deficient mice in arthritic mice
additional information
-
catK-deficient cells show a similar suppression of actin rings as wild-type osteoclasts treated with inhibitor LHVS
-
additional information
-
10-week-old male cathepsin K-deficient knockout mice show bones that are mechanically more brittle, while both osteoclasts and osteoblasts show impaired activity relative to the wild type, phenotype with significant hypercalcification of the calcified cartilage and cortices, overview
-
additional information
-
overexpression of cathepsin K in mice decreases collagen deposition and lung resistance in response to bleomycin-induced pulmonary fibrosis, overview. Cathepsin K protein levels are strongly increased in alveolar macrophages and lung parenchymal tissue of mock-treated cathepsin K transgenic mice relative to wild-type mice
-
additional information
-
the single nucleotide polymorphism G15A in intron 4 of the porcine cathepsin K gene is associated with back fat thickness and production traits in Italian Duroc pigs, but not in Italian Large White pigs
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
pH STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
5.5 - 7.5
-
91% residual activity at pH 5.5, 85% residual activity at pH 6.5, and 11% residual activity at pH 7.5 (at 37°C after 30 min)
708260
6
the activity of cathepsin K is profoundly reduced at pH values of 6.0 (lysosomal pH) and below
708216
7.2
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
50
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
the activity of cathepsin K alone is relatively unstable in aqueous solution, having a half-life of approx. 7 min at pH 7.4 and 37°C. Increasing the ionic strength of the incubation mixture to 300 mM with NaCl decreases the half-life by 7fold. The presence of chondrotin sulfate and dermatan sulfate slightly reduces the stability of cathepsin K (half lives of 5.5 and 6.0 min respectively), whereas heparin has a strong stabilizing effect and increases the enzyme's half-life by more than 5fold (38 min)
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
recombinant procathepsin K from Pichia pastoris, processed to the mature form and purified
-
recombinant procathepsin K, expressed in baculovirus infected SF21 cells, processed to cathepsin K
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
CTSK expression analysis in healthy, benign tumor and malign tumor breast tissues, overview
-
expressed in Escherichia coli
expressed in Escherichia coli strain DH5alphaMCR using the pGEX-4T-1 expression vector system
expressed in Pichia pastoris
expression in Escherichia coli
expression in Pichia pastoris
expression in Spodoptera frugiperda Sf21 cells driven by a polyhedrin promotor
-
expression of the propeptide in Escherichia coli as gluthatione S-transferase fusion protein
-
gene CTSK, DNA and amino acid sequence determination and analysis of wild-type genes and a pycnodysostosis patient mutation, sequence comparison
-
genotyping of C57BL/6 mice either wild-type for cathepsin K, CK+/+, heterozygous for cathepsin K, CK+/-, or deficient in cathepsin K, CK-/-, overview
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
a marked increase in cathepsin K expression is seen in the lungs of patients with emphysema compared to normal subjects
-
cathepsin K becomes up-regulated in its cerebral expression by neuroleptic treatment
-
cathepsin K expression level is decreased in all tissues at 12 h post-infection with Aeromonas hydrophila
cathepsin K gene and protein expression is significantly up-regulated in synovium at the initial stage of osteoarthritis in rabbits
-
cathepsins K is elevated in endothelial cells by tumor necrosis factor-alpha stimulation
CtK expression is significantly increased in the muscle and gill at 3-24 h post-injection with bacterial lipopolysaccharide
CTSK expression is stimulated by nuclear factor kappaB ligand. Both, nuclear factor kappaB ligand treatment and overexpression of nuclear factor of activated T-cells c1 dramatically enhances CTSK promoter activity. Proximal nuclear factor of activated T-cells binding sites play a significant role in the nuclear factor of activated T-cells c1-mediated stimulation of CTSK gene expression by nuclear factor kappaB ligand
-
expression of cathepsin K is significantly increased (2.7-1.6fold) in the low-energy laser irradiated group on days 2-7 compared with those in the non-irradiated group
-
in fibroblasts, interleukin-1alpha and cellular confluence upregulate cathepsin K expression
-
in osteosarcoma cells, tissue growth factor beta1 induces the secretion of cathepsin K by about 3fold
-
increased expression of cathepsin K in tumors and tumor-associated cells may be a direct result of transcriptional regulation by ETS family members
-
induction of cathepsin K expression in fibroblasts from young donors but not from old donors is observed both in vitro and in vivo after exposure to longwave UV-A (100-500 kJ/m2) in a time-dependent manner with a maximum 2 days after exposure. Induction of active cathepsin K is also seen 1 day after irradiation with UV-B and less so after exposure to ionizing radiation followed by decreased levels on the following days
-
inhibiting calcineurin or chelation of intracellular Ca2+, prevents the stimulation of CTSK expression by nuclear factor kappaB ligand
-
ligand of receptor activator of nuclear factor-kappaB does not induce cathepsin K expression in fibroblasts
-
receptor activator of nuclear factor-kappaB or small GTPase Rab do not mediate cathepsin K induction
-
serum cathepsin K decreases gradually after alendronate treatment (17% at 3 months, 22% at 6 months and 41% at 12 months)
-
serum cathepsin K levels are higher in postmenopausal women with osteoporosis compared with healthy postmenopausal women and premenopausal women
-
significantly down-regulated in intestine following Gram-negative bacteria Vibrio anguillarum immersion challenge
SM934-testosterone inhibits proliferation and metastasis ability of breast cancer cells via inhibiting the expression of cathepsin K followed by the inhibition of Bcl-xL
the levels of Cath K in serum of non-small cell lung cancer are comparable to those in controls
-
there is a 3fold increase in cathepsin K activity in the lungs of guinea pigs after 12 weeks smoke exposure
-
upregulated in three tissues (gill, skin and intestine) following Gram-positive bacteria Streptococcus iniae immersion challenge
vasoprotective shear stress inhibits cathepsin K protein expression and activation downstream of TNFalpha stimulation via reduced NF-kappaB activation and expression. TNFalpha stimulation activates JNK/c-jun phosphorylation, but reduction of NF-kappaB protein prevents induction of cathepsin K transcription under vasoprotective shear stress conditions
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
RENATURED/Commentary
ORGANISM
UNIPROT
LITERATURE
using 50 mM Tris-HCl pH 8.0, 500 mM NaCl, 0.5 M urea, 0.7 M arginine, 5 mM EDTA, 1% CHAPS, 15% (v/v) glycerol, 10 mM GSH and 1 mM GSSG
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
diagnostics
-
to assess better the biology of CatK activity in vivo, a novel near-infrared fluorescence (NIRF) probe for imaging of CatK is developed
drug development
medicine
pharmacology
drug development
-
Cat K inhibitors might be useful for the treatment of osteoporosis
drug development
Cat S is an attractive therapeutic target and selective Cat S inhibitors may also modulate a number of other diseases such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, asthma, atherosclerosis and neuropathic pain
drug development
-
cathepsin K inhibitors are regarded as a potential therapy for the treatment of bone loss, such as osteoporosis
drug development
-
cathepsin K is seen as an attractive target for intervention in the treatment of both osteoporosis and osteoarthritis
drug development
-
development of cathepsin K inhibitors as an approach for bone diseases with enhanced bone resorption
drug development
-
lysosomal cysteine protease is an interesting target molecule with therapeutic potential to attenuate bleomycin-induced pulmonary fibrosis in mice
drug development
-
lysosomal cysteine protease is an interesting target molecule with therapeutic potential to attenuate bleomycin-induced pulmonary fibrosis in mice
-
medicine
-
cathepsin K immunodetection may be a valuable adjunct in the correct classification of pulmonary adenocarcinomas, especially in small sclerosing bronchioloalveolar carcinomas, especially in small sclerosing bronchioloalveolar carcinomas and mixed adenocarcinoma subtypes with minimal infiltrative growth
medicine
-
cathepsin K is an attractive target for the development of therapies to treat osteoporosis
medicine
-
the serum level of cathepsin K could serve as a marker for fracture preduction and bone mineral density. The correlation between cathepsin K concentration in subjects without fractures and in those with multiple nontraumatic fractures are statistically significant. The cathepsin K levels of controls and patients with osteoporosis are significantly different
medicine
-
cathepsin K is linked to the pathogenesis of osteoporosis, arthritis, cardiovascular and respiratory diseases
medicine
-
cathepsin K is shown to play an essential role in rheumatoid arthritis, osteoarthritis, atherosclerosis, lung inflammation, amyloidosis, gaucher disease and obesity
medicine
-
catK plays an important role in melanoma invasion and metastasis by mediating intracellular degradation of matrix proteins after phagocytosis. Clinical use of catK inhibitors may be promising for the treatment of melanoma
medicine
-
it is shown that cathepsin K acts as a potent kinin-degrading enzyme in bloodstream. Contrary to cathepsin L, cathepsin K attenuates kallikrein-induced decrease of rat blood pressure, and reduces the hypotensive effect of bradykinin in a dose-dependant manner
medicine
-
it is suggested that cathepsin K plays an important role in the homeostasis of the dermal extracellular matrix and the dynamic equilibrium between matrix synthesis and proteolytic degradation, by counteracting deposition of matrix proteins during scar formation with its matrix-degrading activity
medicine
-
one genetic disorder is traced to cathepsin K: peridontopathia. Osteoblasts from these patients accumulate undigested collagen fibrils. Nonsense, missense and stop codon mutations have been shown in patients
medicine
-
the results suggest that cathepsin K plays an important role in the immune system and serves as a valid therapeutic target in autoimmune diseases
medicine
-
the results suggest that cathepsin K plays an important role in the immune system and serves as a valid therapeutic target in autoimmune diseases
medicine
-
inhibition of CTSK activity may decrease the risk of breast tumor progression
medicine
-
introduction of the enzyme, influencing the bone resorption, into bones might be helpful to stimulate and/or induce bone formation mechanisms, overview
medicine
-
because excessive bone remodeling is a key element in the pathogenesis of postmenopausal osteoporosis and other skeletal disorders, cathepsin K is a potential target for therapeutic intervention
medicine
-
cathepsin K is a marker of osteoclastic activity in periodontal disease
medicine
-
cathepsin K is a target for the pharmacological treatment of osteoporosis
medicine
-
cathepsin K is a target for the pharmacological treatment of osteoporosis
medicine
-
cathepsin K is a target for the pharmacological treatment of osteoporosis
medicine
-
cathepsin K is associated with skeletal and cardiovascular disorders, cathepsin K is a pharmaceutical industry target for treatment of osteoporosis
medicine
-
CTSK inhibitors are a potential novel therapeutic option to decrease squamous cell carcinoma progression
medicine
-
determination of cathepsin K and Cystatin C concentrations has no clinical significance in the prognosis of the survival time in lung cancer
medicine
-
serum cathepsin K is a marker of bone metabolism in postmenopausal women treated with alendronate
medicine
-
treatment with the potent cathepsin K inhibitor relacatib preserves cortical and trabecular bone mass in ovariectomized monkeys
medicine
-
cathepsin K inhibitors may aid in the management of canine osteosarcoma-related malignant osteolysis
medicine
human cathepsinK is a major drug target for the treatment of osteoporosis
medicine
activation of cathepsin K may be a promising strategy to prevent homing of therapy-resistant glioma stem-like cells (GSLCs) in niches and thus render these cells sensitive to chemotherapy and radiation
medicine
selective inhibition of cathepsin K has a therapeutic potential for diseases associated with bone loss and osseous inflammation, such as osteoarthritis, periodontitis, and osteoporosis. Cathepsin K inhibition may have anabolic effects on bone and cartilage regeneration that may be explained as a feedback response to cathepsin K depletion. The use of cathepsin K inhibition to reduce inflammation and associated bone resorption in equine osseous disorders may offer advantages to other therapeutics
pharmacology
-
CTSK is a possible therapeutic target in the treatment of obesity
Select items on the left to see more content.
EXTERNAL LINKS (specific for EC-Number 3.4.22.38)
html completed
Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.
Release 2023.1 (January 2023)
About BRENDA
Social media
Help
Survey
Download
Contribution
Legal
Curated at
Member of
