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Cathepsin K Inhibitors (IC50, Ki)

Structure
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Compound Name
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Standard Type
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Standard Values (in nM)
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OdanacatibIC500.2 [1]
OdanacatibKi0.18 [1]
3-(Benzyloxycarbonylamino)pyrrolidine-1-carbonitrileIC5050.0 [1]
3-(Benzyloxycarbonylamino)pyrrolidine-1-carbonitrileKi140.0 [1]
Pyrrolidine-1-carbonitrileIC502100.0 [1]
Pyrrolidine-1-carbonitrileKi2100.0 [1]
1,3-Dihydro-pyrrolo[3,4-b]quinoline-2-carbonitrileIC50360.0 [1]
1,3-Dihydro-pyrrolo[3,4-b]quinoline-2-carbonitrileKi380.0 [1]
L-873724IC500.2 [1]
BalicatibIC500.6 [1], 1.4 [2], 5.0 [3]
BalicatibKi1.4 [1]
N-[(2S)-4-Methyl-1-oxo-1-[[(4S)-3-oxo-1-pyridin-2-ylsulfonylazepan-4-yl]amino]pentan-2-yl]-1-benzofuran-2-carboxamideIC5070.0 [1], 80.0 [2]
N-[(2S)-4-Methyl-1-oxo-1-[[(4S)-3-oxo-1-pyridin-2-ylsulfonylazepan-4-yl]amino]pentan-2-yl]-1-benzofuran-2-carboxamideKi0.16 [1]
3-[(Cyclohexylcarbonylamino)methyl]azetidine-1-carbonitrileIC5016.0 [1]
4-Propyl-6-(3-(trifluoromethyl)phenyl)pyrimidine-2-carbonitrileIC5033.0 [1]
(S)-Tert-butyl 1-oxohexan-2-ylcarbamateIC5051.0 [1]
Benzyl N-[(2S)-4-methyl-1-[3-[[(2S)-4-methyl-2-(phenylmethoxycarbonylamino)pentanoyl]amino]-4-oxopyrrolidin-1-yl]-1-oxopentan-2-yl]carbamateKi2.0 [1], 2.3 [2]
(2R)-N-(Cyanomethyl)-4-methyl-2-[3-(4-piperazin-1-ylphenyl)phenyl]pentanamideIC503.0 [1], 7.8 [2], 11.0 [3]
(2R)-N-(Cyanomethyl)-4-methyl-2-[3-(4-piperazin-1-ylphenyl)phenyl]pentanamideKi8.0 [1]
N-(1-Cyanopyrrolidin-3-yl)benzenesulfonamideIC5018.0 [1], 50.0 [2], 81.0 [3], 750.0 [4]
N-(1-Cyanopyrrolidin-3-yl)benzenesulfonamideKi90.0 [1]
Azetidine-1-carbonitrileIC50100.0 [1], 450.0 [2], 480.0 [3], 880.0 [4], 100000.0 [5]
2,4-Dimethylpentan-3-yl N-[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamateIC502.5 [1], 2.51 [2], 2.54 [3], 2500.0 [4]
N-[(2S)-1-[2-(4-Methoxyanilino)ethylamino]-4-methyl-1-oxopentan-2-yl]-3-methylbenzamideIC50372.0 [1]
N-[(2S)-1-[2-(4-Methoxyanilino)ethylamino]-4-methyl-1-oxopentan-2-yl]-3-methylbenzamideKi43.0 [1], 91.0 [2]
(S)-1-Cyclohexylpropan-2-yl (S)-1-oxohexan-2-ylcarbamateIC502.7 [1]
1,3-Bis[[n-[(phenylmethoxy)carbonyl]-l-leucyl]amino]-2-propanoneKi22.0 [1]
N-[(2S)-4-Methyl-1-oxo-1-[[(4S)-3-oxo-1-[2-(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl]amino]pentan-2-yl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamideIC5030.0 [1]
N-[(2S)-4-Methyl-1-oxo-1-[[(4S)-3-oxo-1-[2-(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl]amino]pentan-2-yl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamideKi0.0 [1], 0.1 [2]
RelacatibIC500.5 [1]
RelacatibKi0.04 [1]
(2S)-N-(Cyanomethyl)-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-piperazin-1-ylphenyl)phenyl]ethyl]amino]pentanamideIC500.01 [1]
[(2S)-3,3-Dimethyl-1-[3-[4-(trifluoromethyl)phenyl]pyrazol-1-yl]butan-2-yl] N-[(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamateIC500.07 [1], 72.0 [2]
{1-[2-(4-Methoxy-phenylamino)-ethylcarbamoyl]-3-methyl-butyl}-carbamic acid benzyl esterIC5060.0 [1], 70.0 [2], 90.0 [3]
Benzyl N-[(2S)-1-[[(2S)-4-methoxy-3-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamateKi60.0 [1]
[(3R)-4,4-Dimethyl-1-phenylpentan-3-yl] N-[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamateIC501.1 [1]
Tert-butyl N-[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamateIC501200.0 [1], 1202.26 [2]
Benzyl N-[(2S)-4-methyl-1-[2-[2-[(1S)-3-methyl-1-(phenylmethoxycarbonylamino)butyl]-1,3-thiazole-4-carbonyl]hydrazinyl]-1-oxopentan-2-yl]carbamateKi10.0 [1]
(1r,2r)-N-(1-Cyanocyclopropyl)-2-{[4-(4-Fluorophenyl)piperazin-1-Yl]carbonyl}cyclohexanecarboxamideIC5015.0 [1], 15.85 [2]
N-[(2S)-1-[2-(4-Methoxyanilino)ethylamino]-4-methyl-1-oxopentan-2-yl]-4-phenylmethoxybenzamideIC503.0 [1], 6.0 [2]
N-[(2S)-1-[2-(4-Methoxyanilino)ethylamino]-4-methyl-1-oxopentan-2-yl]-4-phenylmethoxybenzamideKi15.0 [1]
1-(2,3-Dichlorophenyl)-N-[(2S)-1-[2-(4-methoxyanilino)ethylamino]-4-methyl-1-oxopentan-2-yl]-1,2,4-triazole-3-carboxamideIC503.0 [1], 9.0 [2]
1-(2,3-Dichlorophenyl)-N-[(2S)-1-[2-(4-methoxyanilino)ethylamino]-4-methyl-1-oxopentan-2-yl]-1,2,4-triazole-3-carboxamideKi11.0 [1]
3-[(Phenylsulfonylamino)methyl]azetidine-1-carbonitrileIC5017.0 [1], 20.0 [2]
3-[(Phenylsulfonylamino)methyl]azetidine-1-carbonitrileKi20.0 [1]
N-[(2S)-1-[(3As,6R,6aR)-6-ethynyl-3-oxo-3a,5,6,6a-tetrahydrofuro[3,2-b]pyrrol-4-yl]-4-methyl-1-oxopentan-2-yl]-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamideKi1.6 [1], 50.0 [2]
N-[(2S)-1-[(3As,6R,6aR)-6-ethynyl-3-oxo-3a,5,6,6a-tetrahydrofuro[3,2-b]pyrrol-4-yl]-4-methyl-1-oxopentan-2-yl]-4-[5-fluoro-2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamideKi1.1 [1], 50.0 [2]
CalpeptinIC500.11 [1]
N-(1-((Cyanomethyl)carbamoyl)cyclohexyl)-4-(2-(4-methylpiperazin-1-yl)thiazol-4-yl)benzamideIC500.25 [1], 0.6 [2]
Morpholine-4-carboxylic acid (1-(3-benzenesulfonyl-1-phenethylallylcarbamoyl)-3-methylbutyl)-amideIC504.0 [1], 6.2 [2]
Grassystatin AIC5010000.0 [1]
Cathepsin inhibitor 1IC503162.28 [1]
7-(2,2-Dimethylpropyl)-6-[(1,3-dioxo-2,8-diazaspiro[4.5]decan-2-yl)methyl]pyrrolo[2,3-d]pyrimidine-2-carbonitrileIC501.0 [1]
N-[1-(Cyanomethylcarbamoyl)cyclohexyl]-4-(4-piperazin-1-ylphenyl)benzamideIC500.4 [1]
N-[(2S)-3-Cyclohexyl-1-[2-(4-methoxyanilino)ethylamino]-1-oxopropan-2-yl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamideKi65000.0 [1]
(2S)-N-[(1S)-1-Cyano-2-phenylethyl]-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-methylsulfonylphenyl)phenyl]ethyl]amino]pentanamideIC500.6 [1]
(1R,2R)-N-(1-Cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexane-1-carboxamideIC501.0 [1]
5-Tert-butyl-N-[(2S)-1-(cyanomethylamino)-3-(3-methylphenyl)-1-oxopropan-2-yl]-2-methylpyrazole-3-carboxamideIC502511.89 [1]
(2S)-1-Phenylpropan-2-yl [(2S)-1-oxohexan-2-yl]carbamateIC501.8 [1]
[(3S)-4,4-Dimethyl-2-oxooxolan-3-yl] N-[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamateIC503.0 [1]
(2S)-N-(Cyanomethyl)-4-methyl-2-[[4-(4-piperazin-1-ylphenyl)thiophen-3-yl]amino]pentanamideIC500.2 [1], 1.0 [2]
(1R)-2-Methyl-1-(phenylmethyl)propyl[(1S)-1-formylpentyl]carbamateIC500.5 [1]
1-(Phenylmethyl)cyclopentyl[(1S)-1-formylpentyl]carbamateIC500.35 [1]
[(2R)-1-[5-(4-Fluorophenyl)-1,3,4-oxadiazol-2-yl]-3,3-dimethylbutan-2-yl] N-[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamateIC500.37 [1], 370.0 [2]
(1-Benzylcyclobutyl)methyl N-[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamateIC508.5 [1], 8.51 [2]
N-[1-[[(2S)-1-Oxo-1-(5-phenyl-1,3,4-oxadiazol-2-yl)pentan-2-yl]carbamoyl]cyclohexyl]-4-(trifluoromethoxy)benzamideKi29.0 [1]
N-[1-[[(2S)-1-(5-Ethyl-1,3,4-oxadiazol-2-yl)-1-oxopentan-2-yl]carbamoyl]cyclohexyl]-4-(trifluoromethoxy)benzamideKi7.9 [1]
[(2R)-3,3-Dimethyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)butan-2-yl] N-[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamateIC500.24 [1], 240.0 [2]
[(2S)-3,3-Dimethyl-1-[4-[4-(trifluoromethyl)phenyl]pyrazol-1-yl]butan-2-yl] N-[(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamateIC500.03 [1], 32.0 [2]
N-[1-[[(2S)-1-[5-(4-Methoxyphenyl)-1,3,4-oxadiazol-2-yl]-1-oxopentan-2-yl]carbamoyl]cyclohexyl]-4-(trifluoromethoxy)benzamideKi22.0 [1]
[1-(3-Phenylpropyl)cyclobutyl]methyl N-[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamateIC5016.98 [1], 17.0 [2]
[(2S)-3,3-Dimethyl-1-[4-[4-(trifluoromethyl)phenyl]imidazol-1-yl]butan-2-yl] N-[(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamateIC500.03 [1], 26.0 [2]
[(2R)-3,3-Dimethyl-1-[5-[4-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]butan-2-yl] N-[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamateIC500.41 [1], 410.0 [2]
N-[1-[[(2S)-1-Oxo-1-[5-[3-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]pentan-2-yl]carbamoyl]cyclohexyl]-4-(trifluoromethoxy)benzamideKi54.0 [1]
[(2S)-3,3-Dimethyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)butan-2-yl] N-[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamateIC50457.09 [1], 460000.0 [2]
[(2R)-3,3-Dimethyl-1-[5-[4-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]butan-2-yl] N-[(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamateIC500.03 [1], 29.0 [2]
[1-(2-Phenylethyl)cyclobutyl]methyl N-[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamateIC5023.99 [1], 24.0 [2]
[(2S)-3,3-Dimethyl-1-[4-[4-(trifluoromethyl)phenyl]imidazol-1-yl]butan-2-yl] N-[(3S)-1,2-dioxo-1-(1,3-thiazol-2-ylamino)heptan-3-yl]carbamateIC505.75 [1], 5800.0 [2]
Benzyl N-[(2S)-4-methyl-1-oxo-1-[[3-oxo-1-(4-phenoxyphenyl)sulfonylpiperidin-4-yl]amino]pentan-2-yl]carbamateKi0.5 [1]
N-[(2S)-4-Methyl-1-oxo-1-[(4-oxooxolan-3-yl)amino]pentan-2-yl]quinoline-2-carboxamideKi44.0 [1]
Benzyl N-[(1S)-3-methyl-1-[(4-oxooxolan-3-yl)carbamoyl]butyl]carbamateKi140.0 [1]
N-[(2S)-4-Methyl-1-oxo-1-[[(2S)-3-oxo-4-(pyridin-2-ylsulfonylamino)butan-2-yl]amino]pentan-2-yl]-1-benzofuran-2-carboxamideIC507.5 [1]
N-[(2S)-4-Methyl-1-oxo-1-[[(2S)-3-oxo-4-(pyridin-2-ylsulfonylamino)butan-2-yl]amino]pentan-2-yl]-1-benzofuran-2-carboxamideKi7.5 [1]
Benzyl N-[(2S)-4-methyl-1-[4-[[(2S)-4-methyl-2-(phenylmethoxycarbonylamino)pentanoyl]amino]-3-oxopiperidin-1-yl]-1-oxopentan-2-yl]carbamateKi2.6 [1]
N-[(2S)-4-Methyl-1-oxo-1-[[(4R)-3-oxo-1-pyridin-2-ylsulfonylazepan-4-yl]amino]pentan-2-yl]-1-benzofuran-2-carboxamideKi0.16 [1], 980.0 [2]
4-Methoxy-N-{1-[2-(4-methoxy-phenylamino)-ethylcarbamoyl]-3-methyl-butyl}-benzamideIC509.0 [1], 14.0 [2]
N-[(2S)-1-[(3Ar,6aS)-4-benzoyl-6-oxo-3,3a,5,6a-tetrahydro-2H-pyrrolo[3,2-b]pyrrol-1-yl]-4-methyl-1-oxopentan-2-yl]-4-tert-butylbenzamideKi10.1 [1]
(2S)-N-(1-Cyanocyclopropyl)-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-methylsulfonylphenyl)phenyl]ethyl]amino]pentanamideIC500.3 [1]
N-(Cyanomethyl)-5,5-difluoro-2-[2-(4-methylsulfanylphenyl)phenyl]cyclohexane-1-carboxamideIC500.46 [1], 0.5 [2]
4-(3-Piperidin-1-Ylpropyl)-6-[3-(Trifluoromethyl)phenyl]pyrimidine-2-CarbonitrileIC504.0 [1]
Ethyl 2-((S)-2-(((S)-1-cyclohexylpropan-2-yloxy)carbonyl)hexanoyl)thiazole-4-carboxylateIC50230.0 [1]
4-Cycloheptyl-6-(3-Piperidin-1-Ylpropyl)pyrimidine-2-CarbonitrileIC50100.0 [1]
N-[(2S)-3-Naphthalen-2-yl-1-oxo-1-[[(4S)-3-oxo-1-pyridin-2-ylsulfonylazepan-4-yl]amino]propan-2-yl]naphthalene-1-carboxamideKi10000.0 [1]
4-(3-(Pentan-3-ylamino)propyl)-6-(3-(trifluoromethyl)phenyl)pyrimidine-2-carbonitrileIC504.0 [1]
N-[1-[[(2S)-1-[5-(Furan-2-yl)-1,3,4-oxadiazol-2-yl]-1-oxopentan-2-yl]carbamoyl]cyclohexyl]-4-(trifluoromethoxy)benzamideKi1.7 [1]
CID 16108900IC500.01 [1], 10.0 [2]
N-[(2S)-4-Methyl-1-oxo-1-[(3-oxooxan-4-yl)amino]pentan-2-yl]-1-benzothiophene-2-carboxamideKi8.0 [1], 11.0 [2]
6-[[4-(4-Acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)pyrrolo[2,3-d]pyrimidine-2-carbonitrileIC501500.0 [1], 1650.0 [2]
6-[4-[3-(4-Ethylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1-methylimidazo[4,5-c]pyridine-4-carbonitrileIC50331.0 [1]
5-Amino-4-(isobutylamino)-6-morpholinopyrimidine-2-carbonitrileIC5018.0 [1]
Items per page: 1 - 10 of 100
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References

This online tool may be cited as follows

MLA

"Quest Database™ Cathepsin K Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Feb. 2025, https://www.aatbio.com/data-sets/cathepsin-k-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2025, February 21). Quest Database™ Cathepsin K Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/cathepsin-k-inhibitors-ic50-ki.
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