Information on EC 3.4.22.38 - cathepsin K

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The enzyme appears in viruses and cellular organisms

EC NUMBER
COMMENTARY hide
3.4.22.38
-
RECOMMENDED NAME
GeneOntology No.
cathepsin K
REACTION
REACTION DIAGRAM
COMMENTARY hide
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
show the reaction diagram
endopeptidase
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-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
CAS REGISTRY NUMBER
COMMENTARY hide
94716-09-3
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ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
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UniProt
Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
C57BL/6 mice
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Manually annotated by BRENDA team
C57Bl6/J mice
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Manually annotated by BRENDA team
DBA/1J mice
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Manually annotated by BRENDA team
FVB/N mice
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Manually annotated by BRENDA team
olive flounder
UniProt
Manually annotated by BRENDA team
Italian Duroc and Italian Large White breeds
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Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
physiological function
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
2-aminobenzoyl-Gly-Pro-Hyp-Gly-Phe(NO2)-Gly-OH + H2O
?
show the reaction diagram
-
-
-
?
2-aminobenzoyl-RPPGFSPFR-(3-nitrotyrosine) + H2O
?
show the reaction diagram
-
-
-
-
?
Abz-His-Pro-Gly-Gly-Pro-Gln-EDDnp + H2O
?
show the reaction diagram
-
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)
-
-
?
Abz-HPGGPQ-EDDnp + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Lys-His-Pro-Lys-7-amido-3-carbamoylmethyl-4-methylcoumarin + H2O
Ac-Lys-His-Pro-Lys + 7-amino-3-carbamoylmethyl-4-methylcoumarin
show the reaction diagram
-
assay at pH 5.5, 37°C
-
-
?
Acetyl-Phe-Arg 4-methylcoumarin 7-amide + H2O
Acetyl-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
-
aggrecan + H2O
?
show the reaction diagram
Ala-Ala-Phe-7-amido-4-methylcoumarin + H2O
Ala-Ala-Phe + 7-amino-4-methylcoumarin
show the reaction diagram
31.29% activity compared to benzyloxycarbonyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin
-
-
?
alpha-isomerized C-telopeptide + H2O
?
show the reaction diagram
-
-
-
-
?
azocasein + H2O
?
show the reaction diagram
-
-
-
-
?
Benzoyl-Arg 4-methylcoumarin 7-amide + H2O
Benzoyl-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
-
Benzoyl-Phe-Val-Arg 4-methylcoumarin 7-amide + H2O
Benzoyl-Phe-Val-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
-
Benzyloxycarbonyl-Arg-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Arg-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
-
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Arg-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
47.92% activity compared to benzyloxycarbonyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin
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-
?
Benzyloxycarbonyl-Glu-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Glu-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
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-
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benzyloxycarbonyl-Gly-Gly-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Gly-Gly-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
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
show the reaction diagram
Benzyloxycarbonyl-Gly-Pro-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Gly-Pro-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
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benzyloxycarbonyl-Gly-Pro-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Gly-Pro-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Benzyloxycarbonyl-Leu-Arg 4-methoxy-2-naphthylamide + H2O
Benzyloxycarbonyl-Leu-Arg + 4-methoxy-2-naphthylamine
show the reaction diagram
Benzyloxycarbonyl-Leu-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Leu-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
benzyloxycarbonyl-Leu-Arg-4-methylcoumarin 7-amide + H2O
benzyloxycarbonyl-Leu-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Benzyloxycarbonyl-Leu-Leu-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Leu-Leu-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
benzyloxycarbonyl-Leu-Leu-Glu-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Leu-Leu-Glu + 7-amino-4-methylcoumarin
show the reaction diagram
23.91% activity compared to benzyloxycarbonyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin
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-
?
Benzyloxycarbonyl-Phe-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
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-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
Benzyloxycarbonyl-Phe-Arg-Phe-Arg-rhodamin 110 + H2O
?
show the reaction diagram
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-
-
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Benzyloxycarbonyl-Phe-Pro-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Phe-Pro-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
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-
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Benzyloxycarbonyl-Val-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Val-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
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Benzyloxycarbonyl-Val-Val-Arg 4-methylcoumarin 7-amide + H2O
Benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
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benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
beta-endorphin + H2O
met-enkephalin + ?
show the reaction diagram
-
-
-
-
?
beta-isomerized C-telopeptide + H2O
?
show the reaction diagram
-
-
-
-
?
Bradykinin + H2O
?
show the reaction diagram
-
-
-
-
?
bradykinin + H2O
bradykinin(1-4) + bradykinin(5-9)
show the reaction diagram
calf skin collagen + H2O
?
show the reaction diagram
-
-
-
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?
calf skin collagen type I + H2O
?
show the reaction diagram
-
-
-
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?
carbobenzoxy-Gly-Pro-Arg-7-amido-4-methylcoumarin + H2O
carbobenzoxy-Gly-Pro-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
carbobenzoxy-Phe-Arg-7-amido-4-methylcoumarin + H2O
carbobenzoxy-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
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?
carbobenzyloxy-Gly-Pro-Arg-4-methylcoumaryl-7-amide + H2O
carbobenzyloxy-Gly-Pro-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
carbobenzyloxy-Leu-Arg-4-methoxy-2-naphthylamide + H2O
carbobenzyloxy-Leu-Arg + 4-methoxy-2-naphthylamine
show the reaction diagram
-
-
-
-
?
carbobenzyloxy-Leu-Arg-4-methylcoumaryl-7-amide + H2O
carbobenzyloxy-Leu-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
carbobenzyloxy-Phe-Arg-4-methylcoumaryl-7-amide + H2O
carbobenzyloxy-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Cbz-Phe-Arg-4-methylcoumarin 7-amide + H2O
Cbz-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
Cbz-Phe-Arg-7-amido-4-methylcoumarin + H2O
Cbz-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Collagen + H2O
?
show the reaction diagram
-
cathepsin K cleaves within the telo as well as triple helical domains of collagens
-
-
?
Collagen + H2O
Fragments of collagen
show the reaction diagram
-
poor substrate
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collagen I + H2O
?
show the reaction diagram
collagen II + H2O
?
show the reaction diagram
collagen III + H2O
?
show the reaction diagram
-
-
-
?
Collagen IV + H2O
?
show the reaction diagram
Collagen type I + H2O
?
show the reaction diagram
Collagen type I + H2O
Fragemnts of collagen type I
show the reaction diagram
collagen type II + H2O
?
show the reaction diagram
-
-
-
-
?
Collagen type II + H2O
Fragments of collagen type II
show the reaction diagram
-
-
cleavage near the N-terminal region within the helical domain, Pro in P2- position
-
collagen VI + H2O
?
show the reaction diagram
-
-
-
?
D-Ala-Leu-Lys-7-amido-4-methylcoumarin + H2O
D-Ala-Leu-Lys + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
D-Phe-Phe-Arg 4-methylcoumarin 7-amide + H2O
D-Phe-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
-
desArg-bradykinin + H2O
?
show the reaction diagram
Elastin + H2O
?
show the reaction diagram
Fibrinogen + H2O
Fragments of fibrinogen
show the reaction diagram
-
poor substrate
-
-
Gelatin + H2O
?
show the reaction diagram
Gelatin + H2O
Fragments of gelatin
show the reaction diagram
-
-
-
-
Gly-Pro-Arg-p-nitroanilide + H2O
Gly-Pro-Arg + p-nitroaniline
show the reaction diagram
-
-
-
-
?
human plasma fibronectin + H2O
?
show the reaction diagram
-
recombinant enzyme
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-
?
kinin + H2O
?
show the reaction diagram
Lys-Bradykinin + H2O
?
show the reaction diagram
Lys-Gln-Lys-Leu-Arg-4-methylcoumarin-7-amide + H2O
Lys-Gln-Lys-Leu-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
N-succinyl-Ala-Ala-Pro-Phe-7-amido-4-methylcoumarin + H2O
N-succinyl-Ala-Ala-Pro-Phe + 7-amino-4-methylcoumarin
show the reaction diagram
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
show the reaction diagram
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
show the reaction diagram
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
show the reaction diagram
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
?
show the reaction diagram
-
-
-
-
?
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-methioninamide + H2O
?
show the reaction diagram
-
-
-
-
?
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucylglycinamide + H2O
?
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-bradykinin-(3-NO2-Tyr) + H2O
?
show the reaction diagram
-
-
-
-
?
Osteonectin + H2O
Fragments of osteonectin
show the reaction diagram
-
-
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
-
Pro-Phe-Arg 4-methylcoumarin 7-amide + H2O
Pro-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
Protein + H2O
?
show the reaction diagram
soluble calf-skin collagen + H2O
?
show the reaction diagram
-
-
-
-
?
Succinyl-Leu-Tyr 4-methylcoumarin 7-amide + H2O
Succinyl-Leu-Tyr + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
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tartrate resistant acid phosphatase + H2O
?
show the reaction diagram
-
-
-
-
?
tartrate-resistant acid phosphatase + H2O
?
show the reaction diagram
tert-Butyloxycarbonyl-Ala-Gly-Pro-Arg 4-methylcoumarin 7-amide + H2O
tert-Butyloxycarbonyl-Ala-Gly-Pro-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
-
tert-Butyloxycarbonyl-Phe-Val-Arg 4-methylcoumarin 7-amide + H2O
tert-Butyloxycarbonyl-Phe-Val-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
-
tert-Butyloxycarbonyl-Val-Leu-Lys 4-methylcoumarin 7-amide + H2O
tert-Butyloxycarbonyl-Val-Leu-Lys + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
-
tert-Butyloxycarbonyl-Val-Pro-Arg 4-methylcoumarin 7-amide + H2O
tert-Butyloxycarbonyl-Val-Pro-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
tissue growth factor beta1 + H2O
?
show the reaction diagram
-
-
-
-
?
Tosyl-Gly-Pro-Arg 4-methylcoumarin 7-amide + H2O
Tosyl-Gly-Pro-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
-
Type I collagen + H2O
?
show the reaction diagram
type I collagen + H2O
C-terminal telopeptide of type I collagen + ?
show the reaction diagram
-
-
-
-
?
type II collagen + H2O
?
show the reaction diagram
-
cathepsin K cleaves the triple helix of type II collagen
-
-
?
type III collagen + H2O
?
show the reaction diagram
-
-
-
-
?
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin + H2O
Z-Gly-Pro-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Z-Leu-Arg-4-methylcoumarin 7-amide + H2O
Z-Leu-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
Z-Leu-Arg-7-amido-4-methylcoumarin + H2O
Z-Leu-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Z-Phe-Arg-4-methylcoumarin 7-amide + H2O
Z-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
Z-Phe-Arg-7-amido-4-methylcoumarin + H2O
Z-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
aggrecan + H2O
?
show the reaction diagram
alpha-isomerized C-telopeptide + H2O
?
show the reaction diagram
-
-
-
-
?
beta-endorphin + H2O
met-enkephalin + ?
show the reaction diagram
-
-
-
-
?
beta-isomerized C-telopeptide + H2O
?
show the reaction diagram
-
-
-
-
?
Bradykinin + H2O
?
show the reaction diagram
-
-
-
-
?
calf skin collagen type I + H2O
?
show the reaction diagram
-
-
-
-
?
Collagen + H2O
?
show the reaction diagram
-
cathepsin K cleaves within the telo as well as triple helical domains of collagens
-
-
?
collagen I + H2O
?
show the reaction diagram
collagen II + H2O
?
show the reaction diagram
collagen III + H2O
?
show the reaction diagram
B2Z447
-
-
-
?
Collagen IV + H2O
?
show the reaction diagram
Collagen type I + H2O
?
show the reaction diagram
collagen type II + H2O
?
show the reaction diagram
-
-
-
-
?
collagen VI + H2O
?
show the reaction diagram
B2Z447
-
-
-
?
Elastin + H2O
?
show the reaction diagram
Gelatin + H2O
?
show the reaction diagram
kinin + H2O
?
show the reaction diagram
Protein + H2O
?
show the reaction diagram
soluble calf-skin collagen + H2O
?
show the reaction diagram
-
-
-
-
?
tartrate resistant acid phosphatase + H2O
?
show the reaction diagram
-
-
-
-
?
tartrate-resistant acid phosphatase + H2O
?
show the reaction diagram
-
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
-
-
?
tissue growth factor beta1 + H2O
?
show the reaction diagram
-
-
-
-
?
Type I collagen + H2O
?
show the reaction diagram
type I collagen + H2O
C-terminal telopeptide of type I collagen + ?
show the reaction diagram
-
-
-
-
?
type II collagen + H2O
?
show the reaction diagram
-
cathepsin K cleaves the triple helix of type II collagen
-
-
?
type III collagen + H2O
?
show the reaction diagram
-
-
-
-
?
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Ca2+
390.04% relative activity at 1 mM
K+
332.4%7 relative activity at 1 mM
Mg2+
125.02% relative activity at 5 mM
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
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
-
-
(1R)-1-benzyl-2-methylpropyl [(1S)-1-formylpentyl]carbamate
-
-
(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-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)-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
-
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(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
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-
(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
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-
(1S)-1-methyl-2-phenylethyl [(1S)-1-formylpentyl]carbamate
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-
(1S)-1-methyl-2-phenylethyl [(1S)-1-[(E)-[(morpholin-4-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
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-
(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
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-
(1S)-1-[(5,6-dichloro-1H-benzimidazol-1-yl)methyl]-2,2-dimethylpropyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
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-
(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
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(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
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(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
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(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[[(morpholin-4-ylcarbonyl)amino]acetyl]pentyl]carbamate
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-
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
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(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamate
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(1S)-2,2-dimethyl-1-([4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]methyl)propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
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(1S)-2,2-dimethyl-1-([4-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
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(1S)-2,2-dimethyl-1-[(3-pyridin-3-yl-1H-pyrazol-1-yl)methyl]propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
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(1S)-2,2-dimethyl-1-[(3-pyridin-4-yl-1H-pyrazol-1-yl)methyl]propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
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-
(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
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-
(1S)-2,2-dimethyl-1-[[3-(trifluoromethyl)-1H-pyrazol-1-yl]methyl]propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
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(2R)-2-[3'-[2-(4-tert-butylpiperazin-1-yl)-1,3-thiazol-4-yl]biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
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-
(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
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-
(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
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-
(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
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-
(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
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-
(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
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-
(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
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-
(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
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-
(2R)-N-(cyanomethyl)-2-[3'-(2-[[3-(dimethylamino)pyrrolidin-1-yl]methyl]-1,3-thiazol-4-yl)biphenyl-3-yl]-4-methylpentanamide
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(2R)-N-(cyanomethyl)-4-methyl-2-[3'-[2-(piperazin-1-ylmethyl)-1,3-thiazol-4-yl]biphenyl-3-yl]pentanamide
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-
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)-[1,1'-biphenyl]-3-yl]pentanamide
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methylpiperazin-1-yl)biphenyl-3-yl]pentanamide
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-
(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
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(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
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(2S)-2-(biphenyl-2-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
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(2S)-2-(biphenyl-3-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
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(2S)-2-(biphenyl-4-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
-
-
(2S)-2-amino-N-[(1S)-2-(biphenyl-4-yl)-1-cyanoethyl]butanamide
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(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
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(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
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(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
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(2S)-4,4-dichloro-N-(1-cyanocyclopropyl)-2-([(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]amino)butanamide
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(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
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(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
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(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
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(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
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(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
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(2S)-4-fluoro-4-methyl-N-(3-oxoazepan-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
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(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
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(2S)-4-fluoro-4-methyl-N-(4-oxopyrrolidin-3-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
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(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
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(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
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(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
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(2S)-N-(1-cyanocyclopropyl)-4,4,4-trifluoro-2-([(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]amino)butanamide
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-
(2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-(3-phenoxyphenoxy)pentanamide
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-
(2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-(4-phenoxyphenoxy)pentanamide
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-
(2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-phenoxypentanamide
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-
(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
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(3S)-1-(2,2-dimethylpropoxy)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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(3S)-1-(benzylcarbamoyl)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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(3S)-1-(benzylsulfonyl)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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(3S)-1-(biphenyl-4-ylcarbonyl)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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(3S)-1-(dicyclopentylmethoxy)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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(3S)-1-(heptan-4-yloxy)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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(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
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(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
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(3S)-1-benzyl-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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(3S)-1-tert-butoxy-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[(thiophen-2-ylmethyl)amino]heptan-3-yl]carbamate
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(3S)-1-tert-butoxy-4,4-dimethylpyrrolidin-3-yl [(3S)-1-(ethylamino)-1,2-dioxoheptan-3-yl]carbamate
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(3S)-1-[(1-benzylcyclobutyl)methoxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(3S)-2-oxo-N-[(1R)-1-phenylethyl]-3-[([[1-(2-phenylethyl)cyclobutyl]oxy]acetyl)amino]heptanamide
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(3S)-2-oxo-N-[(1R)-1-phenylethyl]-3-[([[1-(3-phenylpropyl)cyclobutyl]oxy]acetyl)amino]heptanamide
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(3S)-3-([[(2-methyl-1-phenylpropan-2-yl)oxy]acetyl]amino)-2-oxo-N-[(1R)-1-phenylethyl]heptanamide
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-
(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
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(3S)-4,4-dimethyl-1-(4-phenylbutanoyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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(3S)-4,4-dimethyl-1-(naphthalen-2-ylcarbonyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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(3S)-4,4-dimethyl-1-(pentan-3-yloxy)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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(3S)-4,4-dimethyl-1-(phenylacetyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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(3S)-4,4-dimethyl-1-(phenylcarbamoyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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(3S)-4,4-dimethyl-1-(phenylsulfonyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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(3S)-4,4-dimethyl-1-(pyridin-3-ylcarbonyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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(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
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(3S)-4,4-dimethyl-1-[(2-phenylethyl)carbamoyl]pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
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(3S)-4,4-dimethyl-1-[4-(trifluoromethyl)benzoyl]pyrrolidin-3-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-3-ylamino)heptan-3-yl]carbamate
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(4R)-N-(1-cyanocyclopropyl)-5,5,5-trifluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
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(4S)-N-(1-cyanocyclopropyl)-5,5,5-trifluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
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(S)-N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
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(S,S)-piperidine-4-carboxylic acid [1-[1-(benzoxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
1,3-bis(CBZ-Leu-NH)-2-propanone
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
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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
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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
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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
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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-[[(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
-
-
1,5-(N-benzyloxycarbonylleucyl)carbohydrazide
-
-
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-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
-
-
1-benzylcyclopentyl [(1S)-1-formylpentyl]carbamate
-
-
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-cyano-3-azetidinyl cyclohexylmethyl ether
-
IC 50: 20 nM
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(1H-pyrazol-5-ylamino)acetyl]pentylcarbamate
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
-
-
2,2'-N,N'-bis(benzyloxycarbonyl)-L-leucinylcarbohydrazide
-
-
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-(cyclohexylamino)pyrimidine-4-carbonitrile
-
-
2-(cyclohexylmethyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
-
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
-
-
3,5-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-(benzyloxy)-1-cyanoazetidine
-
IC 50: 40 nM
3-(cyclohexylamino)benzonitrile
-
-
3-amino-4-[(tetrahydro-2-furanylmethyl)amino] benzoic acid
-
-
-
3-benzylpentan-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
3-bromo-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
3-bromo-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
moderate inhibition
3-[(benzyloxy)methyl]-1-cyanopyrrolidine
-
IC 50: 100 nM
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'-[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-(3,4-dimethylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-cyanophenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-cyclopentylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-methylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-tert-butylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(4-acetylpiperazin-1-yl)-5-amino-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
-
-
4-(cyclohexylamino)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-amino-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
4-amino-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
moderate inhibition
4-benzyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-bromo-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
4-bromo-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
moderate inhibition
4-butyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-cyano-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
moderate inhibition
4-cycloheptyl-6-propylpyrimidine-2-carbonitrile
-
-
4-cycloheptyl-6-[3-(piperidin-1-yl)propyl]pyrimidine-2-carbonitrile
-
-
4-cyclohexyl-6-propylpyrimidine-2-carbonitrile
-
-
4-cyclooctyl-6-propylpyrimidine-2-carbonitrile
-
-
4-cyclopentyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-dihydrotanshinone
-
potent exosite inhibitor of cathepsin K
-
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-[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-Morpholinecarbonyl-Ala-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-aminohexanoic acid-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-Gly-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-Ile-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-Leu-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-Met-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-methionine dioxide-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-Phe-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-Val-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-phenyl-6-propylpyrimidine-2-carbonitrile
-
-
4-propyl-6-[2-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-propyl-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
moderate cathepsin K potency
4-propyl-6-[4-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)(4-iodobenzyl)amino]pyrimidine-2-carbonitrile
-
-
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-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-chloro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-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-(methylsulfonyl)phenyl]-6-propylpyrimidine-2-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-[4-chloro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[benzyl(2,2-dimethylpropyl)amino]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-(cyclohexylamino)-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-(cyclopentylamino)-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-morpholin-4-yl-6-(phenylamino)pyrimidine-2-carbonitrile
-
-
5-amino-4-morpholin-4-yl-6-(tetrahydrofuran-3-ylamino)pyrimidine-2-carbonitrile
-
-
5-amino-4-morpholin-4-yl-6-piperidin-1-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-morpholin-4-yl-6-pyrrolidin-1-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-[(1,1-dioxidotetrahydrothiophen-3-yl)amino]-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-amino-4-[(1-methylethyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-[(1-methylpropyl)amino]-6-morpholin-4-ylpyrimidine-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-morpholin-4-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-[(2-methylpropyl)amino]-6-piperazin-1-ylpyrimidine-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
-
-
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-(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-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
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
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
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-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
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-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-cyclohexyl-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
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
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-(cyclohexylamino)pyrazine-2-carbonitrile
-
-
6-(cyclohexylamino)pyridine-2-carbonitrile
-
-
6-benzyl-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-benzyl-7-cyclohexyl-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-(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-[(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
AAE581
-
-
AFG-495
-
-
-
antipain
98.91% inhibition at 0.1 mM
Aprotinin
25.08% inhibition at 0.1 mM
balicatib
benzofuran-2-carboxylic acid [(S)-3-methyl-1-[2-oxo-3-(pyridin-2-ylsulfonylamino)propylcarbamoyl]butyl]amide
-
-
benzyl (1-[(cyanomethyl)carbamoyl]-2-hydroxypropyl)carbamate
-
-
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 1-cyano-3-pyrrolidinylcarbamate
-
IC 50: 40 nM
benzyl [(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamate
-
-
benzyl [(1S)-1-[(cyanomethyl)carbamoyl]-2,2-dimethylpropyl]carbamate
-
weak inhibition
benzyl [(1S)-2-[(cyanomethyl)amino]-1-(naphthalen-2-ylmethyl)-2-oxoethyl]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
benzyl [1-[(cyanomethyl)carbamoyl]cyclohexyl]carbamate
benzyl [1-[(cyanomethyl)carbamoyl]cyclopentyl]carbamate
-
weak inhibition
Benzyloxycarbonyl-Phe-Ala-CHN2
-
-
Benzyloxycarbonyl-Phe-Phe-CHN2
-
-
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
-
-
BML-244
Boc-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
-
-
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
Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z
Calpeptin
-
-
carbobenzyloxy-Phe-Phe-CH2F
-
-
carboxybenzoyl-Phe-Phe-CHN2
-
-
cathepsin K inhibitor II
-
-
-
cathepsin K propeptide
-
-
-
CatK-II
-
specific inhibitor
-
CatK-selective inhibitor II
chicken cystatin
-
-
-
chymostatin
CID444556
-
-
Co2+
5.09% residual activity at 5 mM
CRA-013783
-
-
Cu2+
24.86% residual activity at 5 mM
Cystatin
-
different types, expression analysis in various cell types isolated from normal and neoplastic breast tissue, overview
-
cystatin C
-
dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate
E-64d
-
-
E64d
-
-
EDTA
3.72% inhibition at 0.1 mM
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
-
Hg2+
25.27% residual activity at 5 mM
Human squamous cell carcinoma antigen 1
-
i.e. SCCA1
-
iodoacetate
-
-
L-006235
L-13006235
-
shows no selectivity in cell-based assays over cathepsins B, L, and S
L-873724
L-kininogen
-
natural inhibitor of cathepsin K, reversible, tight-binding competitive inhibitor
-
leupeptin
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-acetoxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
-
-
methyl 5-hydroxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
-
furanquinone from Paulownia tomentosa stem
methyl 5-methoxy dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
-
-
methyl 5-propoxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
-
-
methyl methanethiolsulfonate
-
-
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
-
-
MIV-701
-
-
MIV-701/710
-
-
-
MK-0674
MK-0822
-
-
mPEG-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
-
conjugate
MSX-081
-
-
-
Mu-Leu-Hph-fluoromethylketone
MV061194
-
selective, potent reversible cathepsin K inhibitor
MV061606
-
-
-
MV061645
-
-
-
MV061748
-
-
-
MV061940
-
-
-
MV076159
-
-
-
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-cyano-3-pyrrolidinyl)benzamide
-
IC 50: 370 nM
N-(1-cyano-3-pyrrolidinyl)[1,1'-biphenyl]-4-carboxamide
-
IC 50: 290 nM
N-(1-cyano-3pyrrolidinyl)benzenesulfonamide
-
IC 50: 50 nM
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'-(2-hydroxypropan-2-yl)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'-[(1S)-2,2-difluoro-1-hydroxyethyl]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-[(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-(dimethylamino)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-ethynylbenzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-morpholin-4-ylbenzamide
-
-
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-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-3-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-4-carboxamide
-
-
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-(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)-1-[(3-phenylpropanoyl)amino]cyclohexanecarboxamide
-
-
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-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-methoxybenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
-
N-4-propylbenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
IC50: less than 3 nM
N-Acetyl-Leu-Leu-methional
-
-
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-cyano-tetrahydro-pyridazine compounds
-
-
-
N-[(1-cyano-2-pyrrolidinyl)methyl]benzamide
-
IC 50: 0.013 mM
N-[(1-cyano-2-pyrrolidinyl)methyl]benzenesulfonamide
-
IC 50: 0.012 mM
N-[(1-cyano-3-azetidinyl)methyl]benzamide
-
IC 50: 70 nM
N-[(1-cyano-3-azetidinyl)methyl]benzenesulfonamide
-
IC 50: 20 nM
N-[(1-cyano-3-azetidinyl)methyl]cyclohexanecarboxamide
-
IC 50: 5 nM
N-[(1-cyano-3pyrrolidinyl)methyl]benzenesulfonamide
-
IC 50: 200 nM
N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-norvalinamide
-
-
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-[(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-[[(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-[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-(4-propylpiperazin-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
-
strong inhibition
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]cy