General Information of the Protein
Protein ID
PT01006
Protein Name
Cathepsin S
Gene Name
CTSS
Sequence
MKRLVCVLLVCSSAVAQLHKDPTLDHHWHLWKKTYGKQYKEKNEEAVRRLIWEKNLKFVMLHNLEHSMGMHSYDLGMNHLGDMTSEEVMSLMSSLRVPSQWQRNITYKSNPNRILPDSVDWREKGCVTEVKYQGSCGACWAFSAVGALEAQLKLKTGKLVSLSAQNLVDCSTEKYGNKGCNGGFMTTAFQYIIDNKGIDSDASYPYKAMDQKCQYDSKYRAATCSKYTELPYGREDVLKEAVANKGPVSVGVDARHPSFFLYRSGVYYEPSCTQNVNHGVLVVGYGDLNGKEYWLVKNSWGHNFGEEGYIRMARNKGNHCGIASFPSYPEI
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Protease
>
Cysteine protease
>
Cysteine protease CA clan
>
Cysteine protease C1A family
Function
Thiol protease. Key protease responsible for the removal of the invariant chain from MHC class II molecules and MHC class II antigen presentation (PubMed:30612035). The bond-specificity of this proteinase is in part similar to the specificities of cathepsin L.
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Uniprot ID
Primary ID:
P25774

Secondarily ID:
B4DWC9
D3DV05
Q5T5I0
Q6FHS5
Q9BUG3
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Ensembl ID
ENSG00000163131
HGNC ID
HGNC:2545
Subcellular Location
Lysosome
Secreted
Cytoplasmic vesicle
Phagosome
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0157175
 Compound Info 
N-[5-[6-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]-3-piperidin-1-ylpyridin-2-yl]oxy-2-methylphenyl]prop-2-enamide
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C32H40N6O3
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0167818
 Compound Info 
N-[5-[6-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]-3-pyrrolidin-1-ylpyridin-2-yl]oxy-2-methylphenyl]prop-2-enamide
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C31H38N6O3
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0240119
 Compound Info 
N-[5-[6-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]-3-morpholin-4-ylpyridin-2-yl]oxy-2-methylphenyl]prop-2-enamide
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C31H38N6O4
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000147 , JY
 Cell Line Info 
Cell Line ID: CL000174 , Raji
 Cell Line Info 
Cell Line ID: CL000003 , Ramos
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0190970
 Compound Info 
N-[(2S)-3-(1-methylcyclohexyl)-1-[[(4S,7R)-7-methyl-3-oxo-1-pyridin-2-ylsulfonylazepan-4-yl]amino]-1-oxopropan-2-yl]morpholine-4-carboxamide
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C27H41N5O6S
  1
1 IC50 < 0.4 nM
CP0197279
 Compound Info 
N-[(2S)-3-(1-methylcyclohexyl)-1-[[(4S,7R)-7-methyl-3-oxo-1-pyridin-2-ylsulfonylazepan-4-yl]amino]-1-oxopropan-2-yl]furan-2-carboxamide
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C27H36N4O6S
  1
1 IC50 < 0.4 nM
CP0197278
 Compound Info 
N-[(2S)-3-cyclohexyl-1-[[(4S,7R)-7-methyl-3-oxo-1-pyridin-2-ylsulfonylazepan-4-yl]amino]-1-oxopropan-2-yl]furan-2-carboxamide
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C26H34N4O6S
  1
1 IC50 = 0.5 nM
CP0055364
 Compound Info 
N-(1-amino-1,2-dioxopentan-3-yl)-2-chloro-4-(pyridin-2-ylmethoxy)-3-(trifluoromethyl)benzamide
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C19H17ClF3N3O4
  1
1 IC50 = 1.1 nM
CP0055367
 Compound Info 
2-chloro-N-(1-(1-methyl-1H-pyrazol-3-ylamino)-1,2-dioxopentan-3-yl)-4-(pyridin-2-ylmethoxy)-3-(trifluoromethyl)benzamide
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C23H21ClF3N5O4
  1
1 IC50 = 1.1 nM
CP0233764
 Compound Info 
N-[(2S)-4,4-dimethyl-1-[[(4S,7R)-7-methyl-3-oxo-1-pyridin-2-ylsulfonylazepan-4-yl]amino]-1-oxopentan-2-yl]furan-2-carboxamide
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C24H32N4O6S
  1
1 IC50 = 1.3 nM
CP0281337
 Compound Info 
N-[(2S)-3-(1-methylcyclohexyl)-1-[[(4S,7R)-7-methyl-3-oxo-1-(pyridine-2-carbonyl)azepan-4-yl]amino]-1-oxopropan-2-yl]furan-2-carboxamide
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C28H36N4O5
  1
1 IC50 = 1.5 nM
CP0192328
 Compound Info 
2-chloro-N-[1,2-dioxo-1-(1H-pyrazol-5-ylamino)pentan-3-yl]-3-(trifluoromethyl)benzamide
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C16H14ClF3N4O3
  1
1 IC50 = 2.3 nM
CP0261638
 Compound Info 
6-(4-(2-(1-((3,5-dimethylisoxazol-4-yl)methyl)piperidin-4-yl)ethoxy)-3-(trifluoromethyl)phenyl)-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
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C28H29F3N6O2
  1
1 IC50 = 3.3 nM
CP0043425
 Compound Info 
2-(4-ethoxy-3-(trifluoromethyl)phenyl)-9H-purine-6-carbonitrile
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C15H10F3N5O
  1
1 IC50 = 3.9 nM
CP0125936
 Compound Info 
2-(4-ethoxy-3-(trifluoromethyl)phenyl)-9-(2-hydroxyethyl)-9H-purine-6-carbonitrile
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C17H14F3N5O2
  1
1 IC50 = 4.5 nM
CP0146153
 Compound Info 
(2S)-N-(cyanomethyl)-3-cyclohexyl-2-(phenylformamido)propanamide
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C18H23N3O2
  1
1 IC50 = 5.3 nM
CP0233777
 Compound Info 
9-(3-(dimethylamino)propyl)-2-(4-ethoxy-3-(trifluoromethyl)phenyl)-9H-purine-6-carbonitrile
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C20H21F3N6O
  1
1 IC50 = 6.9 nM
CP0054137
 Compound Info 
6-(4-(3-(4-ethylpiperazin-1-yl)propoxy)-3-(trifluoromethyl)phenyl)-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
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C24H27F3N6O
  1
1 IC50 = 7.2 nM
CP0099327
 Compound Info 
1-methyl-6-(4-(2-(2-oxopyrrolidin-1-yl)ethoxy)-3-(trifluoromethyl)phenyl)-1H-imidazo[4,5-c]pyridine-4-carbonitrile
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C21H18F3N5O2
  1
1 IC50 = 7.8 nM
CP0101971
 Compound Info 
1-methyl-6-(4-(2-(1-methylpiperidin-4-yl)ethoxy)-3-(trifluoromethyl)phenyl)-1H-imidazo[4,5-c]pyridine-4-carbonitrile
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C23H24F3N5O
  1
1 IC50 = 7.9 nM
CP0227274
 Compound Info 
1-methyl-6-(4-(2-(1-(oxazol-2-ylmethyl)piperidin-4-yl)ethoxy)-3-(trifluoromethyl)phenyl)-1H-imidazo[4,5-c]pyridine-4-carbonitrile
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C26H25F3N6O2
  1
1 IC50 = 7.9 nM
CP0054142
 Compound Info 
1-methyl-6-(4-(2-(piperidin-4-yl)ethoxy)-3-(trifluoromethyl)phenyl)-1H-imidazo[4,5-c]pyridine-4-carbonitrile
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C22H22F3N5O
  2
1 IC50 = 8 nM
2 IC50 = 8.3 nM
CP0290727
 Compound Info 
2-(4-(2-(4-(4-cyano-1-methyl-1H-imidazo[4,5-c]pyridin-6-yl)-2-(trifluoromethyl)phenoxy)ethyl)piperidin-1-yl)-N,N-dimethylacetamide
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C26H29F3N6O2
  1
1 IC50 = 8.3 nM
CP0060769
 Compound Info 
5-(2-MORPHOLIN-4-YLETHOXY)BENZOFURAN-2-CARBOXYLIC ACID ((S)-3-METHYL-1-{(S)-3-OXO-1-[2-(3-PYRIDIN-2-YLPHENYL)ACETYL]AZEPAN-4-YLCARBAMOYL}BUTYL)AMIDE
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C40H47N5O7
  3
1 IC50 = 8.3 nM
2 Ki = 8.3 nM
3 Ki = 14 nM
CP0089713
 Compound Info 
1-methyl-6-(4-(3-(4-methylpiperazin-1-yl)propoxy)-3-(trifluoromethyl)phenyl)-1H-imidazo[4,5-c]pyridine-4-carbonitrile
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C23H25F3N6O
  1
1 IC50 = 9.5 nM
CP0168866
 Compound Info 
1-(1-(3-(3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydropyrazolo[4,3-c]pyridin-1-yl)propyl)piperidin-4-yl)-3-methyl-1H-benzo[d]imidazol-2(3H)-one
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C29H34Cl2N6O3S
  2
1 IC50 = 10 nM
2 IC50 = 50 nM
CP0179285
 Compound Info 
3-(5-carbamoyl-3-(4-iodophenyl)-4,5,6,7-tetrahydropyrazolo[4,3-c]pyridin-1-yl)-1-(4-(2-cyanophenyl)piperazin-1-yl)propan-2-yl carbamate
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C28H31IN8O3
  2
1 IC50 = 10 nM
2 IC50 = 20 nM
CP0200185
 Compound Info 
4-(1-(2-hydroxy-3-(5-(methylsulfonyl)-3-(4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydropyrazolo[4,3-c]pyridin-1-yl)propyl)piperidin-4-yl)-2H-benzo[b][1,4]oxazin-3(4H)-one
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C30H34F3N5O5S
  2
1 IC50 = 10 nM
2 IC50 = 28 nM
CP0095325
 Compound Info 
(+/-)-2-(1-(2-hydroxy-3-(5-(methylsulfonyl)-3-(3-(2-(piperidin-1-yl)ethylthio)-4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)propyl)piperidin-4-yl)benzonitrile
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C36H45F3N6O3S2
  1
1 IC50 = 10 nM
CP0095635
 Compound Info 
(+/-)-1-(5-(methylsulfonyl)-3-(3-(2-(piperidin-1-yl)ethylthio)-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
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C34H45F3N6O3S2
  1
1 IC50 = 10 nM
CP0188325
 Compound Info 
2-[3-[4-chloro-3-[2-[4-[[(4-chlorophenyl)methylamino]methyl]phenyl]ethynyl]phenyl]-1-[3-(4-phenylpiperazin-1-yl)propyl]-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-5-yl]-2-oxoacetamide
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C43H43Cl2N7O2
  1
1 IC50 = 10 nM
CP0035631
 Compound Info 
1-methyl-6-(4-(2-(6-methylpyridin-2-yl)ethoxy)-3-(trifluoromethyl)phenyl)-1H-imidazo[4,5-c]pyridine-4-carbonitrile
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C23H18F3N5O
  1
1 IC50 = 11 nM
CP0224911
 Compound Info 
6-(4-(2-(1-acetylpiperidin-4-yl)ethoxy)-3-(trifluoromethyl)phenyl)-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
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C24H24F3N5O2
  1
1 IC50 = 13 nM
CP0054150
 Compound Info 
1-methyl-6-(4-(2-(1-((5-methyl-1,3,4-oxadiazol-2-yl)methyl)piperidin-4-yl)ethoxy)-3-(trifluoromethyl)phenyl)-1H-imidazo[4,5-c]pyridine-4-carbonitrile
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C26H26F3N7O2
  1
1 IC50 = 14.1 nM
CP0283409
 Compound Info 
1-methyl-6-(4-(2-(1-((3-methyl-1,2,4-oxadiazol-5-yl)methyl)piperidin-4-yl)ethoxy)-3-(trifluoromethyl)phenyl)-1H-imidazo[4,5-c]pyridine-4-carbonitrile
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C26H26F3N7O2
  1
1 IC50 = 18.6 nM
CP0066962
 Compound Info 
1-methyl-6-(4-(pyridin-2-ylmethoxy)-3-(trifluoromethyl)phenyl)-1H-imidazo[4,5-c]pyridine-4-carbonitrile
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C21H14F3N5O
  1
1 IC50 = 20 nM
CP0286273
 Compound Info 
ethyl 3-[1-[2-hydroxy-3-[5-methylsulfonyl-3-[4-(trifluoromethyl)phenyl]-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl]-1H-indole-5-carboxylate
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C33H38F3N5O5S
  1
1 IC50 = 27 nM
CP0331268
 Compound Info 
1-(4-(1H-pyrrolo[2,3-b]pyridin-3-yl)piperidin-1-yl)-3-(5-(methylsulfonyl)-3-(4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydropyrazolo[4,3-c]pyridin-1-yl)propan-2-ol
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C29H33F3N6O3S
  1
1 IC50 = 27 nM
CP0043424
 Compound Info 
1-(3-(dimethylamino)propyl)-6-(4-ethoxy-3-(trifluoromethyl)phenyl)-1H-imidazo[4,5-c]pyridine-4-carbonitrile
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C21H22F3N5O
  1
1 IC50 = 27 nM
CP0054139
 Compound Info 
1-methyl-6-(4-(2-(1-(methylsulfonyl)piperidin-4-yl)ethoxy)-3-(trifluoromethyl)phenyl)-1H-imidazo[4,5-c]pyridine-4-carbonitrile
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C23H24F3N5O3S
  1
1 IC50 = 27 nM
CP0043426
 Compound Info 
1-methyl-6-(4-(3-(pyrrolidin-1-yl)propoxy)-3-(trifluoromethyl)phenyl)-1H-imidazo[4,5-c]pyridine-4-carbonitrile
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C22H22F3N5O
  1
1 IC50 = 28 nM
CP0178423
 Compound Info 
1-(4-(1H-pyrrolo[2,3-c]pyridin-3-yl)piperidin-1-yl)-3-(5-(methylsulfonyl)-3-(4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydropyrazolo[4,3-c]pyridin-1-yl)propan-2-ol
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C29H33F3N6O3S
  1
1 IC50 = 30 nM
CP0136628
 Compound Info 
4-(1-(3-(5-(methylsulfonyl)-3-(3-(2-(piperidin-1-yl)ethylthio)-4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)propyl)piperidin-4-yl)-2H-benzo[b][1,4]oxazin-3(4H)-one
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C37H47F3N6O4S2
  1
1 IC50 = 30 nM
CP0228427
 Compound Info 
3-[4-chloro-3-[2-[4-chloro-3-(piperidin-3-ylmethylcarbamoyl)phenyl]ethynyl]phenyl]-1-(3-thiomorpholin-4-ylpropyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide
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C35H41Cl2N7O2S
  1
1 IC50 = 30 nM
CP0228429
 Compound Info 
3-[4-chloro-3-[2-[4-chloro-3-[[(2S)-pyrrolidin-2-yl]methylcarbamoyl]phenyl]ethynyl]phenyl]-1-(3-thiomorpholin-4-ylpropyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide
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C34H39Cl2N7O2S
  1
1 IC50 = 30 nM
CP0239592
 Compound Info 
2-[3-[4-chloro-3-[2-[4-[[(4-chlorophenyl)methylamino]methyl]phenyl]ethynyl]phenyl]-1-(3-thiomorpholin-4-ylpropyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-5-yl]-2-oxoacetamide
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C37H38Cl2N6O2S
  1
1 IC50 = 30 nM
CP0066950
 Compound Info 
1-(2-(dimethylamino)ethyl)-6-(4-ethoxy-3-(trifluoromethyl)phenyl)-1H-imidazo[4,5-c]pyridine-4-carbonitrile
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C20H20F3N5O
  1
1 IC50 = 32 nM
CP0062587
 Compound Info 
6-(4-(3-(dimethylamino)propoxy)-3-(trifluoromethyl)phenyl)-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
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C20H20F3N5O
  2
1 IC50 = 32 nM
2 IC50 = 41 nM
CP0340860
 Compound Info 
N-ethyl-6-fluoro-3-[1-[3-[5-methylsulfonyl-3-[4-(trifluoromethyl)phenyl]-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl]-1-benzothiophene-2-carboxamide
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C33H37F4N5O3S2
  1
1 IC50 = 37 nM
CP0234034
 Compound Info 
6-(4-ethoxy-3-(trifluoromethyl)phenyl)-1-(2-morpholinoethyl)-1H-imidazo[4,5-c]pyridine-4-carbonitrile
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C22H22F3N5O2
  1
1 IC50 = 37 nM
CP0308788
 Compound Info 
6-fluoro-3-(1-(3-(5-(methylsulfonyl)-3-(4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydropyrazolo[4,3-c]pyridin-1-yl)propyl)piperidin-4-yl)-N-(2-morpholinoethyl)benzo[b]thiophene-2-carboxamide
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C37H44F4N6O4S2
  1
1 IC50 = 39 nM
CP0307757
 Compound Info 
(+/-)-1-(1-(2-hydroxy-3-(5-(methylsulfonyl)-3-(3-(2-(piperidin-1-yl)ethylthio)-4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)propyl)piperidin-4-yl)pyrrolidin-2-one
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C33H47F3N6O4S2
  1
1 IC50 = 40 nM
CP0151063
 Compound Info 
N-[[2-chloro-5-[1-[3-[4-(6-chloro-3-methyl-2-oxobenzimidazol-1-yl)piperidin-1-yl]propyl]-6-oxopyrimidin-5-yl]phenyl]methyl]-4-fluorobenzamide
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C34H33Cl2FN6O3
  1
1 IC50 = 40 nM
CP0145805
 Compound Info 
3-[4-chloro-3-[2-[4-[[(4-chlorophenyl)methylamino]methyl]phenyl]ethynyl]phenyl]-1-[3-(4-phenylpiperazin-1-yl)propyl]-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide
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C42H43Cl2N7O
  1
1 IC50 = 40 nM
CP0156115
 Compound Info 
3-[4-chloro-3-[2-[4-chloro-3-(2-morpholin-4-ylethylcarbamoyl)phenyl]ethynyl]phenyl]-1-(3-thiomorpholin-4-ylpropyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide
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C35H41Cl2N7O3S
  1
1 IC50 = 40 nM
CP0409174
 Compound Info 
N-(2-aminoethyl)-6-fluoro-3-[1-[3-[5-methylsulfonyl-3-[4-(trifluoromethyl)phenyl]-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl]-1-benzothiophene-2-carboxamide
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C33H38F4N6O3S2
  1
1 IC50 = 47 nM
CP0318812
 Compound Info 
2-[3-[4-chloro-3-[2-[4-[[(4-chlorophenyl)methylamino]methyl]phenyl]ethynyl]phenyl]-1-[3-[(3R)-3-methylmorpholin-4-yl]propyl]-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-5-yl]-2-oxoacetamide
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C38H40Cl2N6O3
  1
1 IC50 = 50 nM
CP0122579
 Compound Info 
1-(1-(3-(5-(methylsulfonyl)-3-(3-(2-(octahydroisoquinolin-2(1H)-yl)ethylthio)-4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)propyl)piperidin-4-yl)pyrrolidin-2-one
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C37H53F3N6O3S2
  1
1 IC50 = 55 nM
CP0214860
 Compound Info 
1-(4-(1H-pyrrolo[3,2-c]pyridin-3-yl)piperidin-1-yl)-3-(5-(methylsulfonyl)-3-(4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydropyrazolo[4,3-c]pyridin-1-yl)propan-2-ol
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C29H33F3N6O3S
  1
1 IC50 = 58 nM
CP0233538
 Compound Info 
(S)-1-(3-(3-(2-(4-fluoropiperidin-1-yl)ethylthio)-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
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C29H41F4N5O3S2
  1
1 IC50 = 58 nM
CP0039295
 Compound Info 
6-(4-(3-(4-methylpiperazin-1-yl)propoxy)-3-(trifluoromethyl)phenyl)picolinonitrile
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C21H23F3N4O
  1
1 IC50 = 58 nM
CP0148723
 Compound Info 
(2S)-N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-methylsulfonylphenyl)phenyl]ethyl]amino]pentanamide
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C25H27F4N3O3S
  3
1 IC50 = 60 nM
2 IC50 = 183 nM
3 IC50 < 500 nM
CP0094074
 Compound Info 
N-[[2-chloro-5-[2-[3-[4-(6-chloro-3-methyl-2-oxobenzimidazol-1-yl)piperidin-1-yl]propyl]-3-oxopyridazin-4-yl]phenyl]methyl]-4-fluorobenzamide
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C34H33Cl2FN6O3
  1
1 IC50 = 60 nM
CP0185713
 Compound Info 
2-[3-[4-chloro-3-[2-[4-[[(4-chlorophenyl)methylamino]methyl]phenyl]ethynyl]phenyl]-1-(3-morpholin-4-ylpropyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-5-yl]-2-oxoacetamide
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C37H38Cl2N6O3
  1
1 IC50 = 60 nM
CP0239593
 Compound Info 
3-[4-chloro-3-[2-[4-[[(4-chlorophenyl)methylamino]methyl]phenyl]ethynyl]phenyl]-1-[3-[4-(trifluoromethyl)piperidin-1-yl]propyl]-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide
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C38H39Cl2F3N6O
  1
1 IC50 = 60 nM
CP0270776
 Compound Info 
3-[4-chloro-3-[2-[4-[[(4-chlorophenyl)methylamino]methyl]phenyl]ethynyl]phenyl]-1-(3-piperidin-1-ylpropyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide
   Show/Hide
C37H40Cl2N6O
  1
1 IC50 = 60 nM
CP0270778
 Compound Info 
(S)-2-(3-(3-(2-(4-fluoropiperidin-1-yl)ethylthio)-4-(trifluoromethyl)phenyl)-1-(2-hydroxy-3-(piperidin-1-yl)propyl)-6,7-dihydro-1H-pyrazolo[4,3-c]pyridin-5(4H)-yl)-2-oxoacetamide
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C30H40F4N6O3S
  1
1 IC50 = 70 nM
CP0145803
 Compound Info 
3-[4-chloro-3-[2-[4-(pyridin-3-ylmethoxymethyl)phenyl]ethynyl]phenyl]-1-(3-thiomorpholin-4-ylpropyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide
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C35H37ClN6O2S
  1
1 IC50 = 70 nM
CP0145804
 Compound Info 
3-[4-chloro-3-[2-[4-[[(2S)-pyrrolidin-2-yl]methylcarbamoyl]phenyl]ethynyl]phenyl]-1-(3-thiomorpholin-4-ylpropyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide
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C34H40ClN7O2S
  1
1 IC50 = 70 nM
CP0185711
 Compound Info 
3-[4-chloro-3-[2-[4-[[(4-chlorophenyl)methylamino]methyl]phenyl]ethynyl]phenyl]-1-(3-thiomorpholin-4-ylpropyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide
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C36H38Cl2N6OS
  1
1 IC50 = 70 nM
CP0308787
 Compound Info 
1-(4-(1H-pyrrolo[3,2-c]pyridin-3-yl)piperidin-1-yl)-3-(3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydropyrazolo[4,3-c]pyridin-1-yl)propan-2-ol
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C28H33BrN6O3S
  1
1 IC50 = 77 nM
CP0260746
 Compound Info 
(+/-)-(1-(2-hydroxy-3-(5-(methylsulfonyl)-3-(3-(2-(piperidin-1-yl)ethylthio)-4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)propyl)piperidin-4-yl)(pyrrolidin-1-yl)methanone
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C34H49F3N6O4S2
  1
1 IC50 = 90 nM
CP0086359
 Compound Info 
3-[4-chloro-3-[2-[4-[[(4-chlorophenyl)methylamino]methyl]phenyl]ethynyl]phenyl]-1-(3-morpholin-4-ylpropyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide
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C36H38Cl2N6O2
  1
1 IC50 = 90 nM
CP0270775
 Compound Info 
3-[4-chloro-3-[2-[4-(pyridin-3-ylmethylcarbamoyl)phenyl]ethynyl]phenyl]-1-(3-thiomorpholin-4-ylpropyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide
   Show/Hide
C35H36ClN7O2S
  1
1 IC50 = 90 nM
CP0348865
 Compound Info 
6-fluoro-3-(1-(3-(5-(methylsulfonyl)-3-(4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydropyrazolo[4,3-c]pyridin-1-yl)propyl)piperidin-4-yl)benzo[b]thiophene-2-carboxylic acid
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C31H32F4N4O4S2
  1
1 IC50 = 100 nM
CP0128634
 Compound Info 
2-[3-[4-chloro-3-[2-[4-[[(4-chlorophenyl)methylamino]methyl]phenyl]ethynyl]phenyl]-1-[3-[4-(trifluoromethyl)piperidin-1-yl]propyl]-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-5-yl]-2-oxoacetamide
   Show/Hide
C39H39Cl2F3N6O2
  1
1 IC50 = 100 nM
CP0185712
 Compound Info 
2-[3-[4-chloro-3-[2-[4-[[(4-chlorophenyl)methylamino]methyl]phenyl]ethynyl]phenyl]-1-(3-piperidin-1-ylpropyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-5-yl]-2-oxoacetamide
   Show/Hide
C38H40Cl2N6O2
  1
1 IC50 = 100 nM
CP0095306
 Compound Info 
1-(1-(3-(3-(3-(2-(4-methylpiperidin-1-yl)ethylthio)-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
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C34H49F3N6O3S2
  1
1 IC50 = 110 nM
CP0294062
 Compound Info 
N-[[2-chloro-5-[4-[3-[4-(6-chloro-3-methyl-2-oxobenzimidazol-1-yl)piperidin-1-yl]propyl]-3-oxopyrazin-2-yl]phenyl]methyl]-4-fluorobenzamide
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C34H33Cl2FN6O3
  1
1 IC50 = 110 nM
CP0142405
 Compound Info 
2-[3-[4-chloro-3-[2-[4-[[(4-chlorophenyl)methylamino]methyl]phenyl]ethynyl]phenyl]-1-(3-morpholin-4-ylpropyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-5-yl]-N,N-dimethyl-2-oxoacetamide
   Show/Hide
C39H42Cl2N6O3
  1
1 IC50 = 110 nM
CP0262861
 Compound Info 
3-[4-chloro-3-[2-[4-[[(4-chlorophenyl)methylamino]methyl]phenyl]ethynyl]phenyl]-1-[3-[(3R)-3-methylmorpholin-4-yl]propyl]-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide
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C37H40Cl2N6O2
  1
1 IC50 = 110 nM
CP0159011
 Compound Info 
1-(4-(1H-pyrrolo[3,2-b]pyridin-3-yl)piperidin-1-yl)-3-(5-(methylsulfonyl)-3-(4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydropyrazolo[4,3-c]pyridin-1-yl)propan-2-ol
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C29H33F3N6O3S
  1
1 IC50 = 120 nM
CP0318809
 Compound Info 
3-[4-chloro-3-[2-[4-(morpholin-2-ylmethoxymethyl)phenyl]ethynyl]phenyl]-1-(3-thiomorpholin-4-ylpropyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide
   Show/Hide
C34H41ClN6O3S
  1
1 IC50 = 120 nM
CP0318810
 Compound Info 
3-[4-chloro-3-[2-[4-[(4-chlorophenyl)methylcarbamoyl]phenyl]ethynyl]phenyl]-1-(3-thiomorpholin-4-ylpropyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide
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C36H36Cl2N6O2S
  1
1 IC50 = 120 nM
CP0293053
 Compound Info 
methyl 6-fluoro-3-[1-[3-[5-methylsulfonyl-3-[4-(trifluoromethyl)phenyl]-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl]-1-benzothiophene-2-carboxylate
   Show/Hide
C32H34F4N4O4S2
  1
1 IC50 = 130 nM
CP0260743
 Compound Info 
N-[2-[5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-methylsulfonyl-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanylethyl]-2-phenylacetamide
   Show/Hide
C36H45F3N6O5S2
  1
1 IC50 = 130 nM
CP0188324
 Compound Info 
3-[4-chloro-3-[2-[4-chloro-3-(piperazine-1-carbonyl)phenyl]ethynyl]phenyl]-1-(3-thiomorpholin-4-ylpropyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide
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C33H37Cl2N7O2S
  1
1 IC50 = 130 nM
CP0318813
 Compound Info 
1-[4-[2-[2-chloro-5-[5-methylsulfonyl-1-(3-morpholin-4-ylpropyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-3-yl]phenyl]ethynyl]phenyl]-N-[(4-chlorophenyl)methyl]methanamine
   Show/Hide
C36H39Cl2N5O3S
  1
1 IC50 = 140 nM
CP0095636
 Compound Info 
(+/-)-1-(3-(3-(2-(4-fluoropiperidin-1-yl)ethylthio)-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
   Show/Hide
C29H41F4N5O3S2
  1
1 IC50 = 149 nM
CP0062143
 Compound Info 
1-(1-(3-(3-(3-(2-(4-tert-butylpiperidin-1-yl)ethylthio)-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
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C37H55F3N6O3S2
  1
1 IC50 = 160 nM
CP0262863
 Compound Info 
N-[2-[3-[4-chloro-3-[2-[4-[[(4-chlorophenyl)methylamino]methyl]phenyl]ethynyl]phenyl]-1-(3-morpholin-4-ylpropyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-5-yl]-2-oxoethyl]acetamide
   Show/Hide
C39H42Cl2N6O3
  1
1 IC50 = 160 nM
CP0302135
 Compound Info 
1-(1-(3-(5-(methylsulfonyl)-3-(3-(2-(piperidin-1-yl)ethylthio)-4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)propyl)piperidin-4-yl)pyrrolidin-2-one
   Show/Hide
C33H47F3N6O3S2
  1
1 IC50 = 170 nM
CP0059345
 Compound Info 
(2S)-N-(cyanomethyl)-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-methylsulfon
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C23H26F3N3O3S
  1
1 IC50 = 178 nM
CP0128637
 Compound Info 
3-[4-chloro-3-[2-[4-[[(4-chlorophenyl)methylamino]methyl]phenyl]ethynyl]phenyl]-N,N-dimethyl-1-(3-morpholin-4-ylpropyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-sulfonamide
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C37H42Cl2N6O3S
  1
1 IC50 = 180 nM
CP0370561
 Compound Info 
1-[5-methanesulfonyl-3-(4-trifluoromethyl-phenyl)-4,5,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-1-yl]-3-[4-(5-oxy-1H-pyrrolo[3,2-c]pyridin-3-yl)-piperidin-1-yl]-propan-2-ol
   Show/Hide
C29H33F3N6O4S
  1
1 IC50 = 200 nM
CP0095628
 Compound Info 
1-(1-(3-(5-(methylsulfonyl)-3-(3-(2-(4-phenylpiperidin-1-yl)ethylthio)-4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)propyl)piperidin-4-yl)pyrrolidin-2-one
   Show/Hide
C39H51F3N6O3S2
  1
1 IC50 = 200 nM
CP0307756
 Compound Info 
(+/-)-1-(5-(methylsulfonyl)-3-(3-(2-(piperidin-1-yl)ethylthio)-4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)-3-(piperidin-1-yl)propan-2-ol
   Show/Hide
C29H42F3N5O3S2
  1
1 IC50 = 204 nM
CP0297790
 Compound Info 
(S)-(3-(3-(2-(4-fluoropiperidin-1-yl)ethylthio)-4-(trifluoromethyl)phenyl)-1-(2-hydroxy-3-(piperidin-1-yl)propyl)-6,7-dihydro-1H-pyrazolo[4,3-c]pyridin-5(4H)-yl)(1H-1,2,4-triazol-3-yl)methanone
   Show/Hide
C31H40F4N8O2S
  1
1 IC50 = 205 nM
CP0364318
 Compound Info 
(+/-)-1-(4-cyclopentylpiperidin-1-yl)-3-(5-(methylsulfonyl)-3-(3-(2-(piperidin-1-yl)ethylthio)-4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)propan-2-ol
   Show/Hide
C34H50F3N5O3S2
  1
1 IC50 = 218 nM
CP0095305
 Compound Info 
1-(1-(3-(5-(methylsulfonyl)-3-(3-(2-morpholinoethylthio)-4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)propyl)piperidin-4-yl)pyrrolidin-2-one
   Show/Hide
C32H45F3N6O4S2
  1
1 IC50 = 270 nM
CP0293907
 Compound Info 
(+/-)-1-(4-cyclopropylpiperazin-1-yl)-3-(5-(methylsulfonyl)-3-(3-(2-(piperidin-1-yl)ethylthio)-4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)propan-2-ol
   Show/Hide
C31H45F3N6O3S2
  1
1 IC50 = 290 nM
CP0244589
 Compound Info 
(+/-)-1-(5-(methylsulfonyl)-3-(3-(2-(piperidin-1-yl)ethylthio)-4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)-3-morpholinopropan-2-ol
   Show/Hide
C28H40F3N5O4S2
  1
1 IC50 = 325 nM
CP0269813
 Compound Info 
(+/-)-1-(5-(methylsulfonyl)-3-(3-(2-(piperidin-1-yl)ethylthio)-4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)-3-(pyrrolidin-1-yl)propan-2-ol
   Show/Hide
C28H40F3N5O3S2
  1
1 IC50 = 335 nM
CP0260740
 Compound Info 
1-(1-(3-(3-(3-(2-(4-hydroxypiperidin-1-yl)ethylthio)-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
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C33H47F3N6O4S2
  1
1 IC50 = 340 nM
CP0254347
 Compound Info 
5-(methylsulfonyl)-3-(3-(2-(piperidin-1-yl)ethylthio)-4-(trifluoromethyl)phenyl)-1-(3-(piperidin-1-yl)propyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
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C29H42F3N5O2S2
  1
1 IC50 = 380 nM
CP0305743
 Compound Info 
(R)-1-(3-(3-(2-(4-fluoropiperidin-1-yl)ethylthio)-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
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C29H41F4N5O3S2
  1
1 IC50 = 395 nM
CP0302134
 Compound Info 
1-(1-(3-(5-(methylsulfonyl)-3-(3-(2-(pyrrolidin-1-yl)ethylthio)-4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)propyl)piperidin-4-yl)pyrrolidin-2-one
   Show/Hide
C32H45F3N6O3S2
  1
1 IC50 = 410 nM
CP0307758
 Compound Info 
(+/-)-1-(5-(methylsulfonyl)-3-(3-(2-morpholinoethylthio)-4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)-3-(piperidin-1-yl)propan-2-ol
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C28H40F3N5O4S2
  1
1 IC50 = 420 nM
CP0057881
 Compound Info 
(2S)-N-(cyanomethyl)-4-methyl-2-{[(1S)-2,2,2-trifluoro-1-{4-[4-(piperazin-1-yl)phenyl]phenyl}ethyl]amino}pentanamide
   Show/Hide
C26H32F3N5O
  1
1 IC50 = 451 nM
CP0095308
 Compound Info 
5-(methylsulfonyl)-3-(3-(2-(piperidin-1-yl)ethylthio)-4-(trifluoromethyl)phenyl)-1-(3-(pyrrolidin-1-yl)propyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
   Show/Hide
C28H40F3N5O2S2
  1
1 IC50 = 520 nM
CP0316229
 Compound Info 
5-(methylsulfonyl)-3-(3-(2-(piperidin-1-yl)ethylthio)-4-(trifluoromethyl)phenyl)-1-(3-(4-(pyrrolidin-1-yl)piperidin-1-yl)propyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
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C33H49F3N6O2S2
  1
1 IC50 = 560 nM
CP0283495
 Compound Info 
1-(1-(3-(3-(3-(2-(benzylamino)ethylthio)-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
   Show/Hide
C35H45F3N6O3S2
  1
1 IC50 = 700 nM
CP0233536
 Compound Info 
(+/-)-1-(5-(methylsulfonyl)-3-(3-(2-(pyrrolidin-1-yl)ethylthio)-4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)-3-(piperidin-1-yl)propan-2-ol
   Show/Hide
C28H40F3N5O3S2
  1
1 IC50 = 712 nM
CP0095630
 Compound Info 
4-(3-(5-(methylsulfonyl)-3-(3-(2-(piperidin-1-yl)ethylthio)-4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)propyl)morpholine
   Show/Hide
C28H40F3N5O3S2
  1
1 IC50 = 810 nM
CP0062141
 Compound Info 
1-(1-(3-(3-(3-(2-(4-methylpiperazin-1-yl)ethylthio)-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
   Show/Hide
C33H48F3N7O3S2
  1
1 IC50 = 1060 nM
CP0041940
 Compound Info 
(2R)-N-(cyanomethyl)-4-methyl-2-{3-[4-(piperazin-1-yl)phenyl]phenyl}pentanamide
   Show/Hide
C24H30N4O
  3
1 IC50 = 2010 nM
2 IC50 = 20000 nM
3 Ki = 1695 nM
CP0077258
 Compound Info 
N-{1-[(cyanomethyl)carbamoyl]cyclohexyl}-4-[2-(morpholin-4-yl)-1,3-thiazol-4-yl]benzamide
   Show/Hide
C23H27N5O3S
  2
1 IC50 = 27000 nM
2 Ki = 13000 nM
CP0134851
 Compound Info 
N-[1-(cyanomethylcarbamoyl)cyclohexyl]-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
   Show/Hide
C24H30N6O2S
  3
1 IC50 = 47000 nM
2 IC50 > 10000 nM
3 Ki = 47000 nM
CP0077259
 Compound Info 
N-{1-[(cyanomethyl)carbamoyl]cyclohexyl}-4-(morpholin-4-yl)benzamide
   Show/Hide
C20H26N4O3
  2
1 IC50 = 52000 nM
2 Ki = 42000 nM
CP0060236
 Compound Info 
Balicatib
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C23H33N5O2
  4
1 IC50 = 65000 nM
2 Ki = 28000 nM
3 Ki = 30100 nM
4 Ki = 65000 nM
CP0564248
 Compound Info 
N-[(2R)-1-[(1-cyanocyclopropyl)amino]-1-oxo-3-(4-pyridin-2-ylpiperazin-1-yl)sulfonylpropan-2-yl]-3,3-dimethylbutanamide
   Show/Hide
C22H32N6O4S
  1
1 Ki = 0.09 nM
CP0059908
 Compound Info 
(2S)-2-(1-benzofuran-2-ylformamido)-4-methyl-N-[(4S,7R)-7-methyl-3-oxo-1-(pyridine-2-sulfonyl)azepan-4-yl]pentanamide
   Show/Hide
C27H32N4O6S
  1
1 Ki = 1.6 nM
Clinical Information about the Protein
Target 1 ( Cathepsin S (CTSS) )
Target Type Clinical trial Target
Disease 4 Target-related Diseases  4
1 Abdominal aortic aneurysm [ICD-11: BD50.4]
2 Osteoarthritis [ICD-11: FA00-FA05]
3 Autoimmune diabetes [ICD-11: 5A10]
4 Asthma [ICD-11: CA23]
Investigative Drug(s) 2 Investigative Drugs  2
1 JNJ-10329670
 Drug Info 
Investigative
Autoimmune diabetes
2 L-873724
 Drug Info 
Investigative
Asthma
Patented Agent(s) 1 Patented Agent  1
1 PMID27998201-Compound-7
 Drug Info 
Patented
Abdominal aortic aneurysm
Preclinical Drug(s) 1 Preclinical Drug  1
1 L-006235-1
 Drug Info 
Preclinical
Osteoarthritis