Information on EC 3.4.22.27 - cathepsin S

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The expected taxonomic range for this enzyme is: Bilateria

EC NUMBER
COMMENTARY hide
3.4.22.27
-
RECOMMENDED NAME
GeneOntology No.
cathepsin S
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
similar to cathepsin L, but with much less activity on Z-Phe-Arg-/-NHMec, and more activity on the Z-Val-Val-Arg-/- compound
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
CAS REGISTRY NUMBER
COMMENTARY hide
71965-46-3
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
UniProt
Manually annotated by BRENDA team
rafinesque 1818, channel catfish
UniProt
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
mature female cynomolgus
-
-
Manually annotated by BRENDA team
italian large white pig
UniProt
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
metabolism
-
cathepsin S cleaves cathepsin K (cathepsin cannibalism) which reduces the total elastin- and collagen-degradative activity in the multiple cathepsin system. Cathepsin cannibalism protects type I collagen through a reduction in the amount of highly collagenolytic cathepsin K available due to cathepsin S degradation of cathepsin K
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
(4-methyl-7-[[(2S)-2-(4-[(1S)-1-(4-methylcyclohexyl)-1-[(thiophen-3-ylcarbonyl)amino]ethyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-2-oxo-2H-chromen-3-yl)acetic acid + H2O
?
show the reaction diagram
-
-
-
-
?
(7-methoxycoumarin-4-yl)-acetyl-GRWHPMGAPWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
(7-methoxycoumarin-4-yl)-acetyl-GRWHPMG + APWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
specific substrate for CatS
-
-
?
(7-methoxycoumarin-4-yl)-acetyl-GRWPPMGLPWEK(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
(7-methoxycoumarin-4-yl)-acetyl-GRWPPMG + LPWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
specific substrate for CatS
-
-
?
(7-[[(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(thiophen-3-ylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-2H-chromen-3-yl)acetic acid + H2O
?
show the reaction diagram
-
-
-
-
?
(7-[[(2S)-2-(4-[(1S)-1-cyclohexyl-1-[(phenylcarbonyl)amino]ethyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-2H-chromen-3-yl)acetic acid + H2O
?
show the reaction diagram
-
-
-
-
?
(7-[[(2S)-2-(4-[(1S)-1-cyclohexyl-1-[(thiophen-3-ylcarbonyl)amino]ethyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-2H-chromen-3-yl)acetic acid + H2O
?
show the reaction diagram
-
-
-
-
?
(benzyloxycarbonyl-Phe-Arg)2-rhodamine 110 + H2O
?
show the reaction diagram
-
-
-
-
?
10 kDa fragment of the lysosomal MHCII-bound invariant chain + H2O
class II associated invariant chain peptide fragments
show the reaction diagram
-
li p10
-
-
?
Ac-His-Pro-Val-Lys-7-amido-3-carbamoylmethyl-4-methylcoumarin + H2O
Ac-His-Pro-Val-Lys + 7-amino-3-carbamoylmethyl-4-methylcoumarin
show the reaction diagram
-
assay at pH 5.5, 37°C
-
-
?
Albumin + H2O
?
show the reaction diagram
Arg-7-amido-4-methylcoumarin + H2O
Arg + 7-amino-4-methylcoumarin
show the reaction diagram
arresten + H2O
?
show the reaction diagram
-
degradation, recombinant enzyme
-
-
?
azocasein + H2O
?
show the reaction diagram
benzoyl-Phe-Val-Arg-7-amido-4-methylcoumarin + H2O
benzoyl-Phe-Val-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Leu-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
benzyloxycarbonyl-Leu-Leu-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Leu-Leu-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
benzyloxycarbonyl-Lys-4-nitrophenyl ester + H2O
benzyloxycarbonyl-Lys + 4-nitrophenol
show the reaction diagram
-
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
benzyloxycarbonyl-Phe-Val-Arg-7-amido-4-methylcoumarin
benzyloxycarbonyl-Phe-Val-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
benzyloxycarbonyl-Phe-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Val-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
benzyloxycarbonyl-Val-Val-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
benzyloxycarbonyl-Val-Val-Arg-4-methyl-coumaryl-7-amide + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
Boc-Val-Leu-Lys-7-amido-4-methylcoumarin + H2O
Boc-Val-Leu-Lys + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
butyloxycarbonyl-Val-Leu-Lys-7-amido-4-methylcoumarin + H2O
butyloxycarbonyl-Val-Leu-Lys + 7-amino-4-methylcoumarin
show the reaction diagram
canstatin + H2O
?
show the reaction diagram
-
degradation, recombinant enzyme
-
-
?
cathepsin K + H2O
?
show the reaction diagram
-
cathepsin S cleaves cathepsin K (cathepsin cannibalism) which reduces the total elastin- and collagen-degradative activity in the multiple cathepsin system
-
-
?
CBZ-Val-Val-Arg- 7-amino-4-trifluoromethyl coumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Cbz-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
Cbz-Val-Val-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Collagen + H2O
?
show the reaction diagram
Collagen type I + H2O
?
show the reaction diagram
CX3CL1 + H2O
?
show the reaction diagram
-
cathepsin S is able to cleave membrane-anchored CX3CL1, releasing a 55-kDa fragment to the medium
-
-
?
Elastin + H2O
?
show the reaction diagram
elastin + H2O
elastin fragments
show the reaction diagram
-
-
catS generates soluble elastin peptides
-
?
fractalkine + H2O
?
show the reaction diagram
-
-
-
-
?
Gelatin + H2O
?
show the reaction diagram
GRWH-norleucine-VGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWH-norleucine-VG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHDVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHDVG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHFVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHFVG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHGVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHGVG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHIVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHIVGL + RWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHKFSVRWE + H2O
?
show the reaction diagram
-
-
-
-
?
GRWHKISVRWE + H2O
?
show the reaction diagram
-
-
-
-
?
GRWHKLSVRWE + H2O
?
show the reaction diagram
-
-
-
-
?
GRWHKVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHKVG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHKVSVRWE + H2O
GRWHKVS + VRWE
show the reaction diagram
-
-
-
-
?
GRWHPVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHPVG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHT-norleucine-GLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHT-norleucine-G + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTDGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTDG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTFGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTFG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTGGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTGG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTIGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTIG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTKGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTKG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTMGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTMG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTPGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTPG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTTGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTTG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTV-norleucine-LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTV-norleucine + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVDLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVD + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVFLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVF + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVG-citrulline-RWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + citrulline-RWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVG-norleucine-RWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + norleucine-RWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVGFRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + FRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVGIRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + IRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVGKRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + KRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVGLDWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LDWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVGLFWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LFWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVGLHWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LHWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVGLIWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LIWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVGLKWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LKWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVGLPWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LPWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVGLQWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LQWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVGLRDE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LRDE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVGLRFE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LRFE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVGLRGE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LRGE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVGLRHE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LRHE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVGLRIE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LRIE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVGLRKE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LRKE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVGLRRE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LRRE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
GRWHTVG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
specific substrate for CatS
-
-
?
GRWHTVGRRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + RRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVGVRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + VRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVILRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVI + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVKLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVK + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVPLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVP + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVQLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVQ + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHTVTLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVT + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
GRWHVVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHVVG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
haemoglobin + H2O
?
show the reaction diagram
-
-
-
-
?
Hemoglobin + H2O
?
show the reaction diagram
Ii protein + H2O
Ii fragments
show the reaction diagram
Ii-p10 + H2O
?
show the reaction diagram
-
i.e. MHC classe-associated invariant chain, cathepsin S is the only human cysteine protease able to efficiently degrade the Ii-p10 fragment in epithelial cells
-
-
?
insulin + H2O
?
show the reaction diagram
invariant chain + H2O
?
show the reaction diagram
-
invariant chain li is degraded by CatS to the class II-associated invariant chain peptide which dissociates from the MHC-II molecule by forming a complex with the human leucocyte antigen-DM
-
-
?
L-Leu-Leu-Arg-7-amido-4-methylcoumarin + H2O
L-Leu-Leu-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
laminin alpha5-chain + H2O
?
show the reaction diagram
-
the laminin-alpha5-chain is cleaved by CatS specifically at the Ser-Val bond
-
-
?
laminin-5 + H2O
laminin-5 gamma-2 fragments
show the reaction diagram
leupeptin-induced peptide LIP10 + H2O
?
show the reaction diagram
-
-
-
-
?
MHC class II-associated invariant chain Ii + H2O
?
show the reaction diagram
MHCII-class assosciated invariant chain li + H2O
class II invariant chain peptide fragments
show the reaction diagram
-
-
-
-
?
myelin basic protein + H2O
?
show the reaction diagram
N-benzyloxycarbonyl-L-Phe-Arg-7-amido-4-methylcoumarin + H2O
N-benzyloxycarbonyl-L-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1,2-dimethylpropyl]benzamide + H2O
?
show the reaction diagram
-
-
-
-
?
o-aminobenzoic acid-Ala-Thr-Pro-Leu-Leu-Met-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Ala-Thr-Pro-Leu-Leu + Met-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
show the reaction diagram
-
-
80% cleavage site, 20% cleavage site: o-aminobenzoic acid-Ala-Thr-Pro-Leu-Leu-Met + Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
?
o-aminobenzoic acid-Gly-Arg-Leu-Asp-Lys-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Gly-Arg-Leu-Asp + Lys-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
show the reaction diagram
-
-
-
-
?
o-aminobenzoic acid-Gly-Phe-Phe-Val-Thr-Thr-Pro-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Gly-Phe-Phe + Val-Thr-Thr-Pro-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
show the reaction diagram
-
-
-
-
?
o-aminobenzoic acid-His-Leu-Val-Glu-Ala-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-His-Leu-Val-Glu + Ala-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
show the reaction diagram
-
-
-
-
?
o-aminobenzoic acid-His-Leu-Val-Glu-Ala-Leu-Tyr-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-His-Leu-Val-Glu + Ala-Leu-Tyr-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
show the reaction diagram
-
-
56% cleavage site, 44% cleavage site: o-aminobenzoic acid-His-Leu-Val-Glu-Ala-Leu + Tyr-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
?
o-aminobenzoic acid-Leu-Arg-Met-Lys-Leu-Pro-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Leu-Arg-Met-Lys + Leu-Pro-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
show the reaction diagram
-
-
74% cleavage site, 26% cleavage site: o-aminobenzoic acid-Leu-Arg + Met-Lys-Leu-Pro-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
?
o-aminobenzoic acid-Leu-Gln-Leu-Glu-Asn-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Leu-Gln + Leu-Glu-Asn-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
show the reaction diagram
-
-
57% cleavage site, 42% cleavage site: o-aminobenzoic acid-Leu-Gln-Leu-Glu + Asn-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
?
o-aminobenzoic acid-Leu-Glu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Leu-Glu + Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
show the reaction diagram
-
-
-
-
?
o-aminobenzoic acid-Leu-Phe-Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine + H2O
o-aminobenzoic acid-Leu-Phe + Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine
show the reaction diagram
-
-
-
-
?
o-aminobenzoic acid-Leu-Tyr-Leu-Val-Cys-Gly-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Leu-Tyr-Leu + Val-Cys-Gly-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
show the reaction diagram
-
-
70% cleavage site, 30% cleavage site: o-aminobenzoic acid-Leu-Tyr + Leu-Val-Cys-Gly-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
?
o-aminobenzoic acid-Lys-Pro-Pro-Val-Val-Leu-Leu-Pro-Asp-Gln-N-(2,4-dinitrophenyl)ethylendiamine + H2O
o-aminobenzoic acid-Lys-Pro-Pro-Val-Val-Leu + Leu-Pro-Asp-Gln-N-(2,4-dinitrophenyl)ethylendiamine
show the reaction diagram
-
-
-
-
?
o-aminobenzoic acid-Lys-Pro-Val-Ser-Thr-Glu-Gln-Leu-Ala-Gln-N-(2,4-dinitrophenyl)ethylendiamine + H2O
o-aminobenzoic acid-Lys-Pro-Val-Ser + Thr-Glu-Gln-Leu-Ala-Gln-N-(2,4-dinitrophenyl)ethylendiamine
show the reaction diagram
-
-
-
-
?
o-aminobenzoic acid-Phe-Val-Asn-Gln-His-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Glu-Val-Asn + Gln-His-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
show the reaction diagram
-
-
69% cleavage site, 31% cleavage site: o-aminobenzoic acid-Glu-Val + Asn-Gln-His-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
?
o-aminobenzoic acid-Ser-Arg-His-Ser-Leu-Glu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Ser-Arg-His-Ser-Leu-Glu + Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
show the reaction diagram
-
-
-
-
?
o-aminobenzoic acid-Val-Leu-Phe-Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine + H2O
o-aminobenzoic acid-Val-Leu-Phe + Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine
show the reaction diagram
-
-
-
-
?
o-aminobenzoic acid-Val-Leu-Phe-Glu-Lys-Lys-Val-Tyr-Leu-Gln-N-(2,4-dinitrophenyl)ethylendiamine + H2O
o-aminobenzoic acid-Val-Leu-Phe-Glu-Lys-Lys-Val-Tyr + Leu-Gln-N-(2,4-dinitrophenyl)ethylendiamine
show the reaction diagram
-
-
-
-
?
Oxidized insulin B-chain + H2O
?
show the reaction diagram
-
major cleavage sites: Glu13-Ala14, Leu17-Val18 and Phe25-Tyr26. Minor cleavage sites: Asn3-Gln4, Ser9-His10 and Leu15-Tyr16
-
-
?
plasminogen + H2O
?
show the reaction diagram
-
-
cleavage occurs at the Leu469-Leu470 peptide bond resulting in 2 fragments: 60000 Da and 38000 Da
-
?
prion protein 94-233 + H2O
prion protein 135-233 + prion protein 117-233 + prion protein 114-233
show the reaction diagram
-
in vitro, enzyme causes specific and limited N-terminal truncation of prion protein 94-233
major soluble fragments, the region of prion protein between S135 and N146 is a major target for selective cleavage cathepsins S
-
?
pro-dipeptidyl peptidase I + H2O
?
show the reaction diagram
-
i.e. cathepsin C, less efficient activation than with cathepsin L
-
-
?
tert-butyloxycarbonyl-Phe-Leu-Arg-7-amido-4-methylcoumarin + H2O
tert-butyloxycarbonyl-Phe-Leu-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
tert-butyloxycarbonyl-Phe-Phe-Arg-7-amido-4-methylcoumarin + H2O
tert-butyloxycarbonyl-Phe-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
Val-Arg-coumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Val-Val-Arg + H2O
?
show the reaction diagram
-
-
-
-
?
Z-Leu-Arg-7-amido-4-methylcoumarin + H2O
Z-Leu-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Z-Leu-Leu-Arg-7-amido-4-methylcoumarin + H2O
Z-Leu-Leu-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
Z-Phe-Arg-AMC + H2O
?
show the reaction diagram
-
-
-
-
?
Z-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
Z-Val-Val-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Z-Val-Val-Arg-AMC + H2O
?
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
Albumin + H2O
?
show the reaction diagram
-
degradation
-
-
?
Collagen + H2O
?
show the reaction diagram
-
degradation
-
-
?
Collagen type I + H2O
?
show the reaction diagram
-
degradation in plasma membranes
-
-
?
CX3CL1 + H2O
?
show the reaction diagram
-
cathepsin S is able to cleave membrane-anchored CX3CL1, releasing a 55-kDa fragment to the medium
-
-
?
Elastin + H2O
?
show the reaction diagram
elastin + H2O
elastin fragments
show the reaction diagram
-
-
catS generates soluble elastin peptides
-
?
Hemoglobin + H2O
?
show the reaction diagram
-
degradation
-
-
?
Ii protein + H2O
Ii fragments
show the reaction diagram
Ii-p10 + H2O
?
show the reaction diagram
-
i.e. MHC classe-associated invariant chain, cathepsin S is the only human cysteine protease able to efficiently degrade the Ii-p10 fragment in epithelial cells
-
-
?
insulin + H2O
?
show the reaction diagram
-
degradation
-
-
?
invariant chain + H2O
?
show the reaction diagram
-
invariant chain li is degraded by CatS to the class II-associated invariant chain peptide which dissociates from the MHC-II molecule by forming a complex with the human leucocyte antigen-DM
-
-
?
laminin alpha5-chain + H2O
?
show the reaction diagram
-
the laminin-alpha5-chain is cleaved by CatS specifically at the Ser-Val bond
-
-
?
laminin-5 + H2O
laminin-5 gamma-2 fragments
show the reaction diagram
MHC class II-associated invariant chain Ii + H2O
?
show the reaction diagram
-
degradation, cathepsin S and MHC class II-associated invariant chain Ii are responsible for in vivo control of endosomal size and multivesicular morphology
-
-
?
myelin basic protein + H2O
?
show the reaction diagram
-
degradation
-
-
?
prion protein 94-233 + H2O
prion protein 135-233 + prion protein 117-233 + prion protein 114-233
show the reaction diagram
-
in vitro, enzyme causes specific and limited N-terminal truncation of prion protein 94-233
major soluble fragments, the region of prion protein between S135 and N146 is a major target for selective cleavage cathepsins S
-
?
Val-Val-Arg + H2O
?
show the reaction diagram
-
-
-
-
?
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
CoCl2
-
decreased activity
HgCl2
-
decreased activity
Na+
-
almost twofold activation in the presence of 1.0 M NaCl, pH 6.5
Zn2+
-
bound at the active site, structure and ligand overview
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2R)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
(2R)-2-(2-cyclohexylethyl)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(2-cyclopentylethyl)-4-morpholin-4-yl-4-oxo-N-[(1S)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
(2R)-2-(2-cyclopentylethyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)butanamide
-
-
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)butyl]butanamide
-
-
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-phenyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]butanamide
-
-
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
(2R)-2-(cyclohexylmethyl)-N-[(1R)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(cyclohexylmethyl)-N-[(1R)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(cyclopentylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)butyl]butanamide
-
-
(2R)-2-(cyclopentylmethyl)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(cyclopentylmethyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)-2-phenylethanol
-
-
(2R)-2-benzyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-[4'-(1-azabicyclo[2.2.2]oct-4-yl)-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
-
IC50: 1991 nM
(2R)-2-[4'-(4-tert-butylpiperazin-1-yl)-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
-
IC50: 8340 nM
(2R)-2-[4'-[1-(2-amino-2-methylpropyl)piperidin-4-yl]-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
-
IC50: 1427 nM
(2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-N-(1-cyanocyclopropyl)-3-(methylsulfanyl)propanamide
-
-
(2R)-4-dimethyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-2-(2-morpholin-4-yl-2-oxoethyl)pentanamide
-
-
(2R)-4-morpholin-4-yl-4-oxo-2-(2-phenylethyl)-N-[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
(2R)-5-dimethyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-2-(2-morpholin-4-yl-2-oxoethyl)hexanamide
-
-
(2R)-N-(1-benzyl-4-cyanopiperidin-4-yl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-(1-cyanocyclopropyl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-(1-cyanocyclopropyl)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-(4-cyano-1-methylpiperidin-4-yl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-(cyanomethyl)-2-[4'-[4-(2-hydroxy-2-methylpropyl)-1-piperazinyl][1,1'-biphenyl]-3-yl]-4-methylpentanamide
-
IC50 above 0.01 mM
(2R)-N-(cyanomethyl)-2-[4'-[4-(2-hydroxyethyl)-1-piperazinyl][1,1'-biphenyl]-3-yl]-4-methylpentanamide
-
IC50: 609 nM
-
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)-[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 2010 nM
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1H-tetraazol-5-yl)-1,1'-biphenyl-3-yl]pentanamide
-
IC50 above 0.01 mM
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methyl-1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 3931 nM
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-pyrimidinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 1365 nM
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-[4-(2-oxopropyl)-piperazin-1-yl]-1,1'-biphenyl-3-yl]pentanamide
-
IC50: 2364 nM
(2R)-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(1R)-2-[(4-chlorobenzyl)oxy]-1-cyanoethyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-2-carboxamide
-
IC50: 658 nM
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
(2R)-N-[(1S)-1-cyano-3-phenylpropyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-2-(2-morpholin-4-yl-2-oxoethyl)-5-phenylpentanamide
-
-
(2R)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-(2-phenylethyl)butanamide
-
-
(2R)-N-[(3R)-1-benzyl-3-cyanopiperidin-4-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-(1-methylethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-(2-methylpropyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-(2-phenylethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-(cyclopropylmethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-(propan-2-yl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cycloheptylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cycloheptylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(2,3-dihydro-1H-inden-2-ylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(2,3-dihydro-1H-inden-2-ylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclopentylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(1-methylcyclohexyl)methyl]-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(1-methylcyclohexyl)methyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(4-methylcyclohexyl)methyl]-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(4-methylcyclohexyl)methyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-(morpholin-4-yl)-4-oxo-2-(1,2,3,4-tetrahydronaphthalen-2-ylmethyl)butanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-(morpholin-4-yl)-4-oxo-2-[(4-phenylcyclohexyl)methyl]butanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-morpholin-4-yl-4-oxo-2-(1,2,3,4-tetrahydronaphthalen-2-ylmethyl)butanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-morpholin-4-yl-4-oxo-2-[(4-phenylcyclohexyl)methyl]butanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclopentylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclopentylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-methylpiperidin-4-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-methylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-methylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3S)-1-benzyl-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3S)-3-cyano-1-(cyclohexylmethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-1-(4,4'-bipiperidin-1-yl)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
-
-
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxypropan-1-one
-
-
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(propan-2-ylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(propylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
(2S)-1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(1'-methyl-4,4'-bipiperidin-1-yl)propan-2-ol
-
-
(2S)-2-(4-chlorophenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-2-(4-fluorophenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-2-(4-methoxyphenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-2-(4-methylphenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-2-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-2-amino-N-[(1S)-2-(biphenyl-4-yl)-1-cyanoethyl]butanamide
-
-
(2S)-3-cyclohexyl-1-(morpholin-4-yl)-1-oxopropan-2-yl [(2S)-1-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)propan-2-yl]carbamate
-
-
(2S)-4-morpholin-4-yl-4-oxo-2-phenyl-N-[(1S)-1-phenyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]butanamide
-
-
(2S)-4-morpholin-4-yl-4-oxo-2-phenyl-N-[(1S)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
(2S)-4-morpholin-4-yl-4-oxo-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-2-carboxamide
-
-
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
(2S)-N-[(1S)-1-cyclopropyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-phenylbutanamide
-
-
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[2-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[3-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(2S)-3-methyl-1-[[4-(trifluoromethoxy)phenyl]amino]butan-2-yl]-4-(morpholin-4-yl)-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
(2Z)-3-(4-[[5-(3,5-dimethylisoxazol-4-yl)-1,2,4-oxadiazol-3-yl]methoxy]phenyl)-2-(methylsulfonyl)prop-2-enenitrile
-
-
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(furan-2-yl)methanone
-
-
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(pyridin-2-yl)methanone
-
-
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(tetrahydrofuran-2-yl)methanone
-
-
(3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]phenyl)acetic acid
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
(3R)-3-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(3R)-tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
-
IC50: 42 nM
(3S)-3-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(3S)-3-[(N-1,3-benzoxazol-2-yl-3-cyclohexyl-L-alanyl)amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
-
IC50: 12 nM
(3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
(3S)-N-[2-(1H-indol-3-yl)ethyl]-3-[[(4-methylphenyl)sulfonyl]amino]-2-oxo-4-phenylbutanamide
-
-
(3S)-tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
-
IC50: 49 nM
(4R)-1-acetyl-N-[(2R)-1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
-
(4R)-1-acetyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxo-3-phenylpropan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(ethylsulfonyl)-L-prolinamide
-
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfanyl)-L-prolinamide
-
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfinyl)-L-prolinamide
-
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-phenoxy-L-prolinamide
-
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[(2-chlorophenyl)sulfonyl]-L-prolinamide
-
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[(4-fluorophenyl)sulfonyl]-L-prolinamide
-
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[[4-(1H-pyrazol-1-yl)phenyl]sulfonyl]-L-prolinamide
-
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxopropan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(2-methylpropanoyl)-4-(phenylsulfonyl)-L-prolinamide
-
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(2-oxopropyl)-4-(phenylsulfonyl)-L-prolinamide
-
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(3-chlorobenzoyl)-4-(phenylsulfonyl)-L-prolinamide
-
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(3-methoxypropanoyl)-4-(phenylsulfonyl)-L-prolinamide
-
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(4-chlorobenzoyl)-4-(phenylsulfonyl)-L-prolinamide
-
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(biphenyl-4-ylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide
-
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(cyclohexylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide
-
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(methylsulfinyl)-4-(phenylsulfonyl)-L-prolinamide
-
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-benzoyl-4-(phenylsulfonyl)-L-prolinamide
-
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-phenyl-4-(phenylsulfonyl)-L-prolinamide
-
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyridin-3-ylcarbonyl)-L-prolinamide
-
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyridin-4-ylcarbonyl)-L-prolinamide
-
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyrrolidin-1-ylcarbonyl)-L-prolinamide
-
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(trifluoroacetyl)-L-prolinamide
-
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-propanoyl-L-prolinamide
-
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
-
(4R)-N-[2-(1,3-benzoxazol-2-yl)-2-oxoethyl]-1-(cyclohexylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide
-
-
(4S)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]hexanamide
-
IC50 above 0.01 mM
(S)-[1-[1-cyano-pyrrolidin-3(R)-ylcarbamoyl]-3-methyl-butyl]-carbamic acid benzyl ester
-
-
(S)-[1-[1-cyano-pyrrolidin-3(S)-ylcarbamoyl]-3-methyl-butyl]-carbamic acid benzyl ester
-
-
1,1-bis(cyanomethyl)-3-[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]urea
-
-
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[(4-[[(2,2,2-trifluoroethyl)sulfonyl]amino]benzoyl)amino]propanoyl]amino)-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([2-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-3-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-4-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(thiophen-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[methyl(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(methylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(phenylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-([4-[(ethylsulfonyl)amino]benzoyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-([[4-([[(dimethylamino)methyl]sulfonyl]amino)phenyl]carbonyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]benzoyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose ammoniate (1:1)
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[(4-[[(3-fluorophenyl)sulfonyl]amino]benzoyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[(4-[[(3-methoxyphenyl)sulfonyl]amino]benzoyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-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-([3-[(methylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([4-[(methylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([4-[(phenylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([4-[(pyridin-4-ylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-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-[[(2S)-3-(1-methylcyclopentyl)-2-[[4-(methylsulfamoyl)benzoyl]amino]propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[4-methyl-N-(thiophen-3-ylcarbonyl)-L-leucyl]amino]-L-erythro-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-([4-[(cyclohexylsulfonyl)amino]benzoyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-([4-[(cyclopropylsulfonyl)amino]benzoyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-erythro-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-(1'-[(2S)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]-4,4'-bipiperidin-1-yl)ethanone
-
-
1-(1-[(2R)-3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 350 nM
1-(1-[(2S)-3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 190 nM
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 10 nM
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 140 nM
1-(1-[3-[3-(4-chloro-3-methylphenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 60 nM
1-(1-[3-[3-[3-[(2-hydroxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)pyrrolidin-2-one
-
-
1-(1-[3-[5-(methylsulfonyl)-3-[3-[(2-phenoxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)pyrrolidin-2-one
-
-
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 80 nM
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5,6-dichloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 110 nM
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methoxy-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 140 nM
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 90 nM
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 120 nM
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-7-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 210 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 130 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-(2,2,2-trifluoroethyl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 90 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-butyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 140 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 310 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 500 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-tert-butyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 100 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 100 nM
1-(1-[3-[5-acetyl-3-(4-chlorophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 460 nM
1-(1-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 120 nM
1-(1-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-fluoro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 230 nM
1-(2-[[5-[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl]ethyl)piperidin-4-ol
-
-
1-(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)-2-hydroxyethanone
-
-
1-(4-cyclopropylpiperazin-1-yl)-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
-
-
1-(4-methylpiperazin-1-yl)-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
-
-
1-(ethenylideneamino)-3-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 100 nM
1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
1-cyano-(3,4-didehydro)-Pro-Leu methyl ester
-
-
1-cyano-(D)-Pro-(D)-Leu methyl ester
-
-
1-cyano-(D)-Pro-Ala methyl ester
-
-
1-cyano-(D)-Pro-Leu benzyl ester
-
-
1-cyano-(D)-Pro-Leu benzylamide
-
-
1-cyano-(D)-Pro-Leu dimethylamide
-
-
1-cyano-(D)-Pro-Leu methyl ester
-
-
1-cyano-(trans-benzyloxy)prolylleucine methyl ester
-
-
1-cyano-(trans-hydroxy)-Pro-Leu methyl ester
-
-
1-cyano-Pro isoamylamide
-
-
1-cyano-Pro-(D)-Leu methyl ester
-
-
1-cyano-Pro-Ala methyl ester
-
-
1-cyano-Pro-Leu benzyl ester
-
-
1-cyano-Pro-Leu methyl ester
-
-
1-cyano-Pro-Leu-Gly ethyl ester
-
-
1-cyano-Pro-Leu-Leu-Leu methyl ester
-
-
1-cyano-Pro-Phe methyl ester
-
-
1-formyl-(D)-Pro-Leu benzyl ester
-
-
1-iminomethyl-(D)-Pro-Leu benzyl ester
-
-
1-methyl-6-[4-(piperidin-4-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-(piperidin-4-yloxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-(pyridin-2-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-(pyridin-3-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-(pyridin-4-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[(3-oxopiperazin-1-yl)oxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[2-(2-oxopyrrolidin-1-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[2-(6-methylpyridin-2-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[2-(piperidin-4-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[3-(pyrrolidin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-([[1-(4-fluorophenyl)-1-methylethoxy]sulfinyl]methyl)-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(2-methylpropoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(4-fluorophenoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
1-[(3R)-4-(methylsulfonyl)-2-oxo-3-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]butyl]cyclopropanecarbonitrile
-
-
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
-
-
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)methyl]-4-fluorobenzene
-
-
1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
1-[1-(3-[3-[3-([2-[benzyl(methyl)amino]ethyl]sulfanyl)-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(2-methylpyrrolidin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(3-hydroxypyrrolidin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-hydroxypiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-methylpiperazin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-methylpiperazin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-methylpiperidin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-methylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-tert-butylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(benzylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(dimethylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(methylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[3-hydroxy-2-oxo-3-(piperidin-4-yl)propyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(4-phenylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(octahydroisoquinolin-2(1H)-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-oxo-2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-oxo-2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
1-[1-(3-[5-acetyl-3-[4-(trifluoromethoxy)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 130 nM
1-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 100 nM
1-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 110 nM
1-[1-[(2R)-3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl]-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 180 nM
1-[1-[(2S)-3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl]-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 200 nM
1-[2-(dimethylamino)ethyl]-6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-[3-(dimethylamino)propyl]-6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-[3-[3-[(2-aminoethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidine-4-carboxamide
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-(methylsulfanyl)ethanone
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxyethanone
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-methoxyethanone
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]ethanone
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]propan-1-one
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-methyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[3-[4-(2-cyanophenyl)piperazin-1-yl]-2-hydroxypropyl]-3-(4-iodophenyl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide
-
IC50: 50 nM
1-[3-[4-(5-methyl-1H-indol-3-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(morpholin-4-yl)propan-2-ol
-
-
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperazin-1-yl)propan-2-ol
-
-
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[4-(2-[[5-[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl]ethyl)piperazin-1-yl]ethanone
-
-
1-[4-(dimethylamino)piperidin-1-yl]-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
-
-
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(3,4-dichlorobenzyl)methanamine
-
-
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(4-methoxybenzyl)methanamine
-
-
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(4-methylbenzyl)methanamine
-
-
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-methylmethanamine
-
-
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(morpholin-4-yl)propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(propylamino)propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(pyrrolidin-1-yl)propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-[4-(pyridin-2-yl)piperidin-1-yl]propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-[4-(pyrrolidin-1-yl)piperidin-1-yl]propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
2,2'-[[3-(trifluoromethyl)phenyl]imino]bis[N-(4-methylphenyl)acetamide]
-
-
2,3,4,5,6-pentafluoro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 0.020 mM
2-(1,1'-biphenyl-3-yl)-N-(cyanomethyl)-4-methylpentanamide
-
IC50: 1578 nM
2-(1,1'-biphenyl-4-yl)-N-(cyanomethyl)-4-methylpentanamide
-
IC50: 3343 nM
2-(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)-2-oxoethyl acetate
-
-
2-(4-tert-butylphenyl)-5-[[2-(3,4-dimethoxyphenyl)ethyl]amino]-1,3-oxazole-4-carbonitrile
-
-
2-(4-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperazin-1-yl)benzonitrile
-
IC50: 120 nM
2-([5-[1-[2-hydroxy-3-[(3S)-3-methylmorpholin-4-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(3-methyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(piperidin-1-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(pyrrolidin-1-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-[(3R)-3-hydroxypyrrolidin-1-yl]ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-[(3S)-3-hydroxypyrrolidin-1-yl]ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyrrolidin-1-ylcarbonyl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([5-[1-[3-[4-(2-fluorophenyl)piperazin-1-yl]-2-hydroxypropyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)-1,3-thiazolidine
-
-
2-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)-2,3-dihydro-1,3-benzothiazole
-
-
2-amino-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]ethanone
-
-
2-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 35 nM
2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-[(1,4-dioxaspiro[4.5]dec-8-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
-
brain-penetrating cathepsin S inhibitors
2-cyano-4-[(2-cyclopentylethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
-
brain-penetrating cathepsin S inhibitors
2-cyano-4-[(6,8-dioxaspiro[3.5]non-7-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
-
brain-penetrating cathepsin S inhibitors
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-4-[[1-(2-hydroxyethyl)piperidin-4-yl]methoxy]-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
brain-penetrating cathepsin S inhibitors
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-methyl-4-(piperidin-4-ylmethoxy)-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
brain-penetrating cathepsin S inhibitors
2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
brain-penetrating cathepsin S inhibitors
2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[4.5]dec-8-ylmethyl)amino]pyrimidine-5-carboxamide
-
brain-penetrating cathepsin S inhibitors
2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]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-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
2-cyano-N-methyl-4-[[1-(1-methylethyl)piperidin-4-yl]methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
brain-penetrating cathepsin S inhibitors
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-hydroxy-1-(1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)ethanone
-
-
2-hydroxy-1-(1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)ethanone
-
-
2-hydroxy-N'-[1H-indol-3-yl(oxo)acetyl]-2,2-diphenylacetohydrazide
-
-
2-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)sulfanyl]ethanol
-
-
2-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-1,3-difluorobenzene
-
-
2-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]biphenyl
-
-
2-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]benzonitrile
-
-
2-[3-(4-chloro-3-[4-[(4-chloro-benzylamino)-methyl]-phenylethynyl]-phenyl)-1-[3-(3-methyl-morpholin-4-yl)-propyl]-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-oxo-acetamide
-
-
2-[3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
-
-
2-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-oxoacetamide
-
-
2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9-(2-hydroxyethyl)-9H-purine-6-carbonitrile
-
-
2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9-ethyl-9H-purine-6-carbonitrile
-
-
2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
-
-
2-[4-methoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
-
-
2-[5-carbamoyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-1-[[4-(2-cyanophenyl)piperazin-1-yl]methyl]ethyl carbamate
-
IC50: 20 nM
2-[N-(3-chlorophenyl)-L-leucyl]tetrahydropyridazine-1(2H)-carbonitrile
-
-
2-[N-(4-cyanophenyl)-L-leucyl]pyrazolidine-1-carbonitrile
-
-
2-[N-(4-cyanophenyl)-L-phenylalanyl]pyrazolidine-1-carbonitrile
-
-
2-[N-(4-fluorophenyl)-L-valyl]tetrahydropyridazine-1(2H)-carbonitrile
-
-
2-[N-[3-(trifluoromethyl)phenyl]-L-isoleucyl]tetrahydropyridazine-1(2H)-carbonitrile
-
-
2-[[5-(1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(morpholin-4-yl)ethanone
-
-
2-[[5-(1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
-
-
2-[[5-(1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(morpholin-4-yl)ethanone
-
-
2-[[5-(1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
-
-
2-[[5-(5-acetyl-1-[2-hydroxy-3-[4-(2-hydroxypropan-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
-
-
2-[[5-(5-acetyl-1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(morpholin-4-yl)ethanone
-
-
2-[[5-(5-ethyl-1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
-
-
2-[[5-[5-acetyl-1-[2-hydroxy-3-(4-methylpiperidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
-
-
2-{[3-(4-chloro-5-hydroxy-2-methoxyphenyl)-4-oxo-3,4-dihydroquinazolin-2-yl]sulfanyl}-N-[(1S)-1-cyano-1,2-dimethylpropyl]acetamide
-
-
3'-[1-[[(cyanomethy)amino]carbonyl]-3-methylbutyl]-1,1'biphenyl-4-carboxamide
-
IC50: 1373 nM
-
3-(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)prop-2-yn-1-ol
-
-
3-(4-chloro-3-ethynylphenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-(4-chloro-3-[[2-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-(4-chloro-3-[[3-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-(4-chloro-3-[[4-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 33 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-(naphthalen-2-ylacetyl)-L-alaninamide
-
IC50: 5.0 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-([5-[3-(trifluoromethyl)phenyl]furan-2-yl]acetyl)-L-alaninamide
-
IC50: 3.3 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(3-phenoxyphenyl)acetyl]-L-alaninamide
-
IC50: 8.0 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(4-morpholin-4-ylphenyl)acetyl]-L-alaninamide
-
IC50: 4.0 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(4-phenoxyphenyl)acetyl]-L-alaninamide
-
IC50: 17 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(5-methyl-1-phenyl-1H-pyrazol-4-yl)acetyl]-L-alaninamide
-
IC50: 34 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[[4-(1H-1,2,4-triazol-1-yl)phenyl]acetyl]-L-alaninamide
-
IC50: 26 nM
3-cyclohexyl-N2-(5-fluoro-1,3-benzoxazol-2-yl)-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
-
IC50: 197 nM
3-cyclohexyl-N2-(6-fluoro-1,3-benzoxazol-2-yl)-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
-
IC50: 43 nM
3-cyclohexyl-N2-([4-[(4,6-dimethylpyrimidin-2-yl)amino]phenyl]acetyl)-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 2.0 nM
3-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,5-dimethyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 30 nM
3-[3-(benzylsulfanyl)-4-chlorophenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide
-
-
3-[4-chloro-3-(4-methylpent-1-yn-1-yl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(cyclohexylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(hept-1-yn-1-yl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(phenylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(propylsulfanyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(thiophen-2-ylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(thiophen-3-ylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(2-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(2-methoxyphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(2-methylphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(2-phenoxyethyl)sulfanyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(2-phenylethyl)sulfanyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(3,4-dichlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(3-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
3-[4-chloro-3-[(4-methoxyphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(4-methylphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
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]pyrimidine-6-yl]methoxy]benzamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
4-(3-acetylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-bromophenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-chlorophenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-cyclobutylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-cyclopentylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-cyclopropylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-ethylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-methylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-tert-butylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(acetylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 123 nM
4-(dimethylamino)-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
-
-
4-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 16 nM
4-fluoro-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
-
-
4-hydroxy-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
-
-
4-methyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-N2-(morpholin-4-ylcarbonyl)-L-leucinamide
-
-
4-methyl-N2-(morpholin-4-ylcarbonyl)-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-L-leucinamide
-
-
4-morpholinecarbonyl-Phe-(S-benzyl)Cys-PSI(CHO)
-
-
4-morpholinecarboxamide, N-[(1R)-2-[[(1S)-1-(2-benzoxazolylcarbonyl) propyl] amino]-1-[[(cyclopropylmethyl)-sulfonyl]methyl]-2-oxoethyl]
-
previously reported as 05141, ihbitor-dosed mice are protected against ozone-induced airway hyperresponsiveness
4-phenyl-6-propylpyrimidine-2-carbonitrile
-
-
4-propyl-6-(3-propylphenyl)pyrimidine-2-carbonitrile
-
-
4-propyl-6-[2-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-propyl-6-[3-(trifluoromethoxy)phenyl]pyrimidine-2-carbonitrile
-
-
4-propyl-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-propyl-6-[4-(trifluoromethoxy)-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-propyl-6-[4-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[(1-acetylpiperidin-4-yl)methoxy]-2-cyano-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
brain-penetrating cathepsin S inhibitors
4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]aniline
-
-
4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzoic acid
-
-
4-[(4-[(E)-[(cyanoacetyl)hydrazono]methyl]phenoxy)methyl]benzoic acid
-
-
4-[1-(2-hydroxy-3-[3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[5-tert-butoxy-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[5-tert-butoxy-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
-
-
4-[2-chloro-5-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[3,5-bis(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[3-(2-methylpropyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[3-(methylsulfonyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[3-(propan-2-yl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[4-(propan-2-yloxy)-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-chloro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-ethoxy-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-fluoro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-methoxy-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-methyl-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]benzamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]benzoic acid
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-3-[3-[(2-phenoxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-(methylsulfonyl)-1-[3-[4-(1H-pyrrolo[3,2-c]pyridin-3-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-(piperidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-(pyrrolidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-[4-(pyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-bromo-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
-
-
5-chloro-3-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 150 nM
5-chloro-3-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 80 nM
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
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-(2-cyclooctylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-(2-piperidine-1-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
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-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-[2-(3-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-chloro-1-(1-[3-[3-(4-chloro-3-methylphenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
6-chloro-1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 60 nM
6-chloro-1-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 30 nM
6-[3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
-
-
6-[4-(2-hydroxyethoxy)-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-(2-hydroxyethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
-
-
6-[4-(3-oxopropyl)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-(ethylamino)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-[2-(morpholin-4-yl)ethyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-[3-(morpholin-4-yl)propyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-ethoxy-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
-
-
6-[4-methoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-phenoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-[2-(2-oxopyrrolidin-1-yl)ethoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
-
-
6-[4-[2-(dimethylamino)ethoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-[3-(2-ethyl-1H-imidazol-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
-
-
6-[4-[3-(4-ethylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
-
-
6-[4-[3-(dimethylamino)propoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[[4-(1-acetyl-1,2,3,6-tetrahydropyridine-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
-
-
6-[[4-(1-acetylpiperidine-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-[[4-(4-acetylpiperazine-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
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-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2-cyclohexylethyl)-6-(naphthalen-1-ylmethyl)-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
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2-cyclohexylethyl)-6-[(pyridine-2-yloxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[(pyridine-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
7-tert-butyl-6-(4-chlorobenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
9-[3-(dimethylamino)propyl]-2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
-
-
APC-2848
-
irreversible vinyl-sulfone inhibitor
benzoyl-Phe-Phe-CHN2
-
0.006 mM, 39% inhibition
benzyl [(2S)-1-(2-cyanotetrahydropyridazin-1(2H)-yl)-3-methyl-1-oxopentan-2-yl]carbamate
-
-
benzyloxycarbonyl Phe-Ala-CH2F
-
very potent time-dependent inhibitor, inhibits proteinase 30times more efficiently than it does cathepsin L and about 300times better than it does cathepsin B
benzyloxycarbonyl-((CH3)3C-CH(NH2)-COOH)-Tyr-CHN2
-
t1/2 at 0.1 mM is 1.6 min
benzyloxycarbonyl-((CH3)3C-CH2-CH(NH2)-COOH)-Leu-Tyr-CHN2
-
t1/2 at 0.0004 mM is 3.85 min
benzyloxycarbonyl-Ala-Leu-COCHO
-
-
benzyloxycarbonyl-Ile-Met-CHN2
-
t1/2 at 0.001 mM is 5.4 min
benzyloxycarbonyl-Ile-Trp-CHN2
-
t1/2 at 0.004 mM is 3.45 min
benzyloxycarbonyl-Leu-Ala-CHN2
-
t1/2 at 0.0001 mM is 5.5 min
benzyloxycarbonyl-Leu-Leu-CHN2
-
t1/2 at 0.00002 mM is 8.6 min
benzyloxycarbonyl-Leu-Leu-Nle-CHN2
-
t1/2 at 0.000001 mM is 1.25 min
benzyloxycarbonyl-Leu-Leu-Tyr-CHN2
-
t1/2 at 0.000001 mM is 5.5 min
benzyloxycarbonyl-Leu-Nle-CHN2
-
t1/2 at 0.00001 mM is 3.4 min
benzyloxycarbonyl-Leu-Nva-CHN2
-
t1/2 at 0.00001 mM is 4.5 min
benzyloxycarbonyl-Leu-Thr(tert-butyl)-CHN2
-
t1/2 at 0.001 mM is 3.5 min
benzyloxycarbonyl-Leu-Trp-CHN2
-
t1/2 at 0.0002 mM is 2.6 min
benzyloxycarbonyl-Phe-Ala-CH2F
-
-
Benzyloxycarbonyl-Phe-Ala-CHN2
-
-
benzyloxycarbonyl-Phe-Ala-COCHO
-
-
-
Benzyloxycarbonyl-Phe-Arg
-
-
benzyloxycarbonyl-Phe-Arg-COCHO
-
-
-
benzyloxycarbonyl-Phe-Leu-COCHO
-
potent, reversible cathepsin S inhibitor, the inhibitor is 400fold more selective for cathepsin S than for cathepsin B
-
benzyloxycarbonyl-Phe-Lys(benzyloxycarbonyl)-CH3
-
; inhibition in the micromolar range, competitive
-
Benzyloxycarbonyl-Phe-Phe-CHN2
benzyloxycarbonyl-Phe-Tyr(OBut)-COCHO
-
-
-
benzyloxycarbonyl-Phe-Tyr(tert-butyl)CHN2
-
t1/2 at 0.02 mM is 19.25 min, about 10000times more effective against cathepsin L than against cathepsin S
-
benzyloxycarbonyl-Trp-Met-CHN2
-
t1/2 at 0.00001 mM is 3.0 min
benzyloxycarbonyl-Tyr-Ala-CHN2
-
0.001 mM, 88% inhibition
benzyloxycarbonyl-Tyr-Tyr(o-butyl)-CHN2
-
1 mM, 78% inhibition
-
benzyloxycarbonyl-Val-Met-CHN2
-
t1/2 at 0.0001 mM is 3.5 min
-
benzyloxycarbonyl-Val-Nle-CHN2
-
t1/2 at 0.00003 mM is 5.8 min
-
benzyloxycarbonyl-Val-Trp-Nle-CHN2
-
t1/2 at 0.00001 mM is 5.7 min
-
benzyloxycarbonyl-Val-Val-CHN2
-
t1/2 at 0.0001 mM is 47.0 min
-
benzyloxycarbonyl-Val-Val-Lys-NHO-4-nitrobenzoyl
-
-
-
benzyloxycarbonyl-Val-Val-Nle-CHN2
-
t1/2 at 0.000001 is 2.5 min, 300times more effective in inactivating cathepsin S than cathepsin L
-
benzyloxycarbonyl-Val-Val-Phe-CH3
-
; inhibition in the micromolar range, competitive
-
benzyloxycarbonyl-Val-Val-Tyr-CHN2
-
t1/2 at 0.000005 mM is 6.75 min
-
butyloxycarbonyl-Lys-Leu-Tyr-CHN2
-
t1/2 at 0.0001 mM is 2.9 min
carbobishydrazide
-
irreversible cathepsin S inhibitor
cathepsin K propeptide
-
-
-
cathepsin L propeptide
-
-
-
cathepsin S propeptide
-
0.0002 mM, blocks gelatinase, collagenase and elastinase activities of mature cathepsin S
-
cathespin S propeptide
chimeric propeptide of cathepsin S and cathepsin L S1-54/L44-86
-
-
-
Chlorella powder
-
-
-
CLIK-060
CLIK-066
-
0.01 mM, 28% inhibition
CLIK-088
-
0.01 mM, 64% inhibition
CLIK-112
-
0.01 mM, 77% inhibition
CLIK-121
-
0.01 mM, complete inhibition
CLIK-148
-
0.01 mM, complete inhibition
CLIK-164
-
-
CLIK-181
-
0.01 mM, 80% inhibition
CLIK-195
-
0.01 mM, complete inhibition
CLIK60
-
selective CatS inhibitor, CatS inhibition increases macrophage cholesterol accumulation and efflux
Cystatin
cystatin A
-
inhibition in the subnanomolar range
-
cystatin B
-
inhibition in the subnanomolar range
-
cystatin C
cystatin F
-
-
-
dipeptide-vinyl sulfone LHVS
-
irreversible cathepsin S inhibitor
egg white cystatin
Ep-475
-
0.01 mM, complete inhibition
epoxysuccinyl-Ala benzyl ester
-
-
epoxysuccinyl-Arg benzyl ester
-
-
epoxysuccinyl-D-Phe benzyl amide
-
-
epoxysuccinyl-D-Phe benzyl ester
-
-
epoxysuccinyl-Ile benzyl ester
-
-
epoxysuccinyl-Leu benzyl amide
-
-
epoxysuccinyl-Leu benzyl ester
-
-
epoxysuccinyl-Phe benzyl amide
-
-
epoxysuccinyl-Phe benzyl ester
-
-
epoxysuccinyl-Val benzyl ester
-
-
ethyl (3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoate
-
IC50: 71 nM
GM6001
-
-
iodoacetic acid
-
1 mM, 92% inhibition
JNJ 10329670
kininogen domain 3
-
-
-
L-873724
Leupeptin
methyl (2R)-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)(phenyl)ethanoate
-
-
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-4-[(1S)-1-[(1R)-2-[(1-cyanocyclopropyl)amino]-1-(methoxysulfinyl)methyl]-2-oxoethyl]amino)-2,2,2-trifluoroethyl]-4'-fluorobiphenyl
-
-
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfenate
-
-
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(3-fluorophenyl)ethyl]amino]propane-1-sulfinate
-
-
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propane-1-sulfinate
-
-
methyl (2S)-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)(phenyl)ethanoate
-
-
methyl (2Z)-4-[4-(dimethylamino)phenyl]-4-oxo-2-[(phenylcarbonyl)hydrazono]butanoate
-
-
methyl (3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(oxo)acetate
-
-
methyl (3R)-3-[[(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanoyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate
-
-
methyl (3S)-3-[[(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanoyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate
-
-
methyl (3S)-3-[[3-cyclohexyl-N-(morpholin-4-ylcarbonyl)-L-alanyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate
-
-
methyl 1-[2-hydroxy-3-(4-quinolin-4-ylpiperazin-1-yl)propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(2-oxo-2,3-dihydro-4,1-benzoxazepin-1(5H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidine-4-carboxylate
-
-
methyl 1-[3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(5-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(6-chloro-2,2-dioxido-3,4-dihydro-1H-2,1,3-benzothiadiazin-1-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 2-amino-4-([(1S)-2-(1-[(benzyloxy)methyl]-3-[(2-ethoxy-2-oxoethyl)amino]-2,3-dioxopropylamino)-1-(cyclohexylmethyl)-2-oxoethyl]aminocarbonyl)benzoate
-
-
methyl 2-[[(1S)-1-(cyclohexylmethyl)-2-([2-[(4-fluorophenyl)amino]ethyl]amino)-2-oxoethyl]amino]-1,3-benzoxazole-6-carboxylate
-
IC50: 43 nM
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(3,4-dihydroisoquinolin-2(1H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(5-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2,2-dioxido-3,4-dihydro-1H-2,1,3-benzothiadiazin-1-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 4'-[(1S)-1-([(1S)-1-[(1-cyanocyclopropyl)carbamoyl]pentyl]amino)-2,2,2-trifluoroethyl]biphenyl-4-sulfinate
-
-
methyl 4-([(1S)-2-((1S)-1-[(benzyloxy)methyl]-3-[(2-ethoxy-2-oxoethyl)amino]-2,3-dioxopropyl amino)-1-(cyclohexylmethyl)-2-oxoethyl]aminocarbonyl)-2-[(tert-butoxycarbonyl)amino]benzoate
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-
methyl 4-[(E)-[[(3-[2-[(2-chlorobenzyl)oxy]phenyl]-1H-pyrazol-5-yl)carbonyl]hydrazono]methyl]benzoate
-
-
morpholine-4-carboxylic acid [1-[1S-(N-benzoyl-hydrazinomethyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
IC50: 565 mM
morpholine-4-carboxylic acid [1R-(1S-cyano-3-phenyl-propylcarbamoyl)-1,3-dimethyl-butyl]-amide
-
-
morpholine-4-carboxylic acid [1R-(1S-cyano-3-phenyl-propylcarbamoyl)-3-methylbutyl]amide
-
IC50: 0.011 mM
morpholine-4-carboxylic acid [1S-(1R-cyano-3-phenylpropylcarbamoyl)-3-methylbutyl]amide
-
IC50: 387 nM
morpholine-4-carboxylic acid [1S-(1S-cyano-2,2-dimethylpropylcarbamoyl)-3-methylbutyl]amide
-
IC50: 0.107 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-2-methyl-propylcarbamoyl)-3-methylbutyl]amide
-
IC50: 1400 nM
morpholine-4-carboxylic acid [1S-(1S-cyano-2-phenylethylcarbamoyl)-3-methylbutyl]amide
-
IC50: 130 nM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenyl-propylcarbamoyl)-1,3-dimethyl-butyl]-amide
-
IC50: 0.076 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-cyclohexyl-ethyl]-amide
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IC50: 5 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-methyl-propyl]-amide
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IC50: 0.006 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-phenyl-ethyl]-amide
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IC50: 173 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-3,3-dimethyl-butyl]-amide
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IC50: 23 nM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-cyclohexyl-R-methyl]-amide
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IC50: 84 nM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-ethyl]-amide
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IC50: 0.134 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-pentyl]-amide
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IC50: 41 nM
morpholine-4-carboxylic acid [1S-(1S-cyanobutylcarbamoyl)-3-methylbutyl]amide
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IC50: 82 nM
morpholine-4-carboxylic acid [1S-(1S-cyanobutylcarbamoyl)-3-methylpentyl]amide
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IC50: 56 nM
morpholine-4-carboxylic acid [1S-(1S-cyanomethylcarbamoyl)-3-methylbutyl]amide
-
IC50: 142 nM
morpholine-4-carboxylic acid [1S-(2-benzyloxy-1R-cyano-ethylcarbamoyl)-3-methylbutyl]amide
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IC50: 19 nM
morpholine-4-carboxylic acid [1S-(cyanomethylcarbamoyl)-3-methylbutyl]amide
-
IC50: 124 nM
morpholine-4-carboxylic acid [1S-[(1-cyano-1-methyl)ethylcarbamoyl]-3-methylbutyl]amide
-
IC50: 114 nM
morpholine-4-carboxylic acid [1S-[(cyano-phenyl-S-methyl)carbamoyl]-3-methylbutyl]amide
-
IC50: 51 nM
morpholine-4-carboxylic acid [1S-[1S-(benzoyl-hydrazonomethyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
IC50: 11 nM
morpholine-4-carboxylic acid [1S-[1S-cyano-2-(3,4-dichlorophenyl)ethylcarbamoyl]-3-methylbutyl]amide
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IC50: 56 nM
morpholine-4-carboxylic acid [1S-[1S-[(2-hydroxy-benzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
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IC50: 7 nM
morpholine-4-carboxylic acid [1S-[1S-[(4-hydroxybenzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
IC50: 35 nM
morpholine-4-carboxylic acid [1S-[2-(2-chlorobenzyloxy)-1R-cyanoethylcarbamoyl]-3-methylbutyl]amide
-
9 nM
morpholine-4-carboxylic acid [1S-[2-(3-chlorobenzyloxy)-1R-cyanoethylcarbamoyl]-3-methylbutyl]amide
-
9 nM
morpholine-4-carboxylic acid [1S-[2-(4-chlorobenzyloxy)-1R-cyanoethylcarbamoyl]-3-methylbutyl]amide
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27 nM
morpholine-4-carboxylic acid [3-methyl-1S-(1-prop-2-ynylcarbamoyl)butyl]amide
-
IC50: 0.097 m
morpholine-4-carboxylic acid [3-methyl-1S-(1R-methyl-3-phenylpropylcarbamoyl)butyl]amide
-
IC50 above 0.339 mM
morpholine-4-carboxylic acid [3-methyl-1S-(3-phenyl-propylcarbamoyl)butyl]amide
-
IC50 above 0.028 mM
morpholineurea-leucyl-homophenylalanine-vinylsulfone phenyl
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LHVS, CatS-specific inhibitor at a concentration of 10 nM, other cathepsins are not inhibited
morpholinurea-leucine-homophenylalanine-vinyl sulfone-phenyl
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irreversible inhibitor
morpholinurea-leucinehomophenylalanine-vinyl phenyl sulfone
-
irreversible CatS inhibitor
N,N-dimethyl-2-([5-[5-(methylsulfonyl)-1-[3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)acetamide
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-
N-(1-cyanocyclopropyl)-3-(methylsulfinyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
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-
N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-(4'-fluorobiphenyl-4-yl)ethyl]-L-alaninamide
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-
N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
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-
N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-phenylethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-[(3,4-dichlorophenyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-[(4-fluorobenzyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-phenylethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-[(4-fluorophenyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-[[2-(4-fluorophenyl)propan-2-yl]sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(4-benzyl-1-methylpiperidin-4-yl)-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
-
N-(4-chlorobenzyl)-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
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-
N-(4-cyano-1-phenyl-1H-pyrazol-5-yl)-2-[(4-ethyl-5-thiophen-2-yl-4H-1,2,4-triazol-3-yl)sulfanyl]acetamide
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-
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetamide
-
-
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-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]pyrimidine-6-yl]methoxy]phenyl)propanamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
N-(cyanomethyl)-2-[3-(1H-indol-5-yl)phenyl]-4-methylpentanamide
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IC50: 922 nM
N-(cyanomethyl)-2-[3-(1H-indol-6-yl)phenyl]-4-methylpentanamide
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IC50: 1257 nM
N-(cyanomethyl)-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]-3-phenylpropanamide
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IC50 above 0.01 mM
N-(cyanomethyl)-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]acetamide
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IC50 above 0.01 mM
N-(cyanomethyl)-3-cyclobutyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]propanamide
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IC50: 2310 nM
N-(cyanomethyl)-3-cyclopropyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]propanamide
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IC50: 6597 nM
N-(cyanomethyl)-4-methyl-2-(2-phenyl-1,3-thiazol-4-yl)pentanamide
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IC50 above 0.01 mM
N-(cyanomethyl)-4-methyl-2-(3'-piperazin-1-yl-1,1'-biphenyl-3-yl)pentanamide methanesulfonate
-
IC50 above 0.01 mM
N-(cyanomethyl)-4-methyl-2-(3-pyridin-3-ylphenyl)-pentanamide
-
IC50 above 0.01 nM
N-(cyanomethyl)-4-methyl-2-(3-pyridin-4-ylphenyl)-pentanamide trifluoroacetate
-
IC50: 1748 nM
N-(cyanomethyl)-4-methyl-2-(3-pyrimidin-5-ylphenyl)pentanamide
-
IC50 above 0.01 mM
N-(cyanomethyl)-4-methyl-2-(5-phenylpyridin-3-yl)-pentanamide trifluoroacetate
-
IC50 above 0.01 mM
N-(cyanomethyl)-4-methyl-2-[2'-(1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
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IC50: 521 nM
N-(cyanomethyl)-4-methyl-2-[2'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide
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IC50: 3368 nM
N-(cyanomethyl)-4-methyl-2-[3'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide
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IC50 above 0.01 mM
N-(cyanomethyl)-4-methyl-2-[4'-(1,2,3,6-tetrahydro-4-pyridinyl)[1,1'-biphenyl]-3-yl]pentanamide
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IC50: 652 nM
N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
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IC50: 1245 nM
N-(cyanomethyl)-4-methyl-2-[4'-(4-methyl-1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
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IC50: 1695 nM