Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.22.38 extracted from

  • Palmer, J.T.; Bryant, C.; Wang, D.X.; Davis, D.E.; Setti, E.L.; Rydzewski, R.M.; Venkatraman, S.; Tian, Z.Q.; Burrill, L.C.; Mendonca, R.V.; Springman, E.; McCarter, J.; Chung, T.; Cheung, H.; Janc, J.W.; McGrath, M.; Somoza, J.R.; Enriquez, P.; Yu, Z.W.; Strickley, R.M.; Liu, L.; Venuti, M.C.; Percival, M.D.; et al
    Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K (2005), J. Med. Chem., 48, 7520-7534.
    View publication on PubMed
Search for more literature for 3.4.22.38

Inhibitors

Inhibitors Comment Organism Structure
3-(4-([4'-((1-[(cyanomethyl)carbamoyl]cyclohexyl)carbamoyl)biphenyl-4-yl]oxy)piperidin-1-yl)propanoic acid
-
 Homo sapiens
3-bromo-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
 Homo sapiens
4'-(4-tert-butylpiperazin-1-yl)-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-4-carboxamide
-
 Homo sapiens
4'-[4-(tert-butylamino)piperidin-1-yl]-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-4-carboxamide
-
 Homo sapiens
4-(2-[(3R)-3-aminopyrrolidin-1-yl]-1,3-thiazol-4-yl)-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
 Homo sapiens
4-amino-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
 Homo sapiens
4-bromo-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
 Homo sapiens
4-[2-(1,4'-bipiperidin-1'-yl)-1,3-thiazol-4-yl]-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
 Homo sapiens
4-[2-(4-tert-butylpiperazin-1-yl)-1,3-thiazol-4-yl]-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
 Homo sapiens
5-bromo-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)thiophene-2-carboxamide
-
 Homo sapiens
benzyl (1-[(cyanomethyl)carbamoyl]-2-hydroxypropyl)carbamate
-
 Homo sapiens
benzyl [(1S)-2-[(cyanomethyl)amino]-1-(naphthalen-2-ylmethyl)-2-oxoethyl]carbamate
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-2-pyridin-4-yl-1,3-thiazole-4-carboxamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-(4-fluoropiperidin-4-yl)biphenyl-4-carboxamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-(dimethylamino)biphenyl-4-carboxamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-(piperazin-1-ylsulfonyl)biphenyl-4-carboxamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-([(2S)-1-methylpyrrolidin-2-yl]methoxy)biphenyl-4-carboxamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-([1-(2-hydroxyethyl)piperidin-4-yl]oxy)biphenyl-4-carboxamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-([4-(2,2,2-trifluoroethyl)piperazin-1-yl]sulfonyl)biphenyl-4-carboxamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-isoxazol-5-ylbiphenyl-4-carboxamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-piperazin-1-ylbiphenyl-4-carboxamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-[(1-methylpiperidin-3-yl)oxy]biphenyl-4-carboxamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-[(1-methylpiperidin-4-yl)oxy]biphenyl-4-carboxamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-[methyl(1-methylpyrrolidin-3-yl)amino]biphenyl-4-carboxamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-(4-[(1-methylethyl)amino]piperidin-1-yl)-1,3-thiazol-4-yl)benzamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-(4-[methyl(1-methylethyl)amino]piperidin-1-yl)-1,3-thiazol-4-yl)benzamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-morpholin-4-yl-1,3-thiazol-4-yl)benzamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[(4-methylpiperazin-1-yl)amino]-1,3-thiazol-4-yl)benzamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[(4-methylpiperazin-1-yl)methyl]-1,3-thiazol-4-yl)benzamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[3-(dimethylamino)pyrrolidin-1-yl]-1,3-thiazol-4-yl)benzamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[4-(2-methoxyethyl)piperazin-1-yl]-1,3-thiazol-4-yl)benzamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[4-(tetrahydro-2H-pyran-4-yl)piperazin-1-yl]-1,3-thiazol-4-yl)benzamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(4-methylpiperazin-1-yl)benzamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(4-propylpiperazin-1-yl)benzamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(dimethylamino)benzamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-ethynylbenzamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-morpholin-4-ylbenzamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[(4-methylpiperazin-1-yl)carbonyl]benzamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[(4-methylpiperazin-1-yl)sulfonyl]benzamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(1,4-dimethylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(1-methylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(4-morpholin-4-ylpiperidin-1-yl)-1,3-thiazol-4-yl]benzamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(morpholin-4-ylmethyl)-1,3-thiazol-4-yl]benzamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(piperidin-4-yloxy)-1,3-thiazol-4-yl]benzamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-3-carboxamide
-
 Homo sapiens
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-4-carboxamide
-
 Homo sapiens
N-(cyanomethyl)-1-[(3-phenylpropanoyl)amino]cyclohexanecarboxamide
-
 Homo sapiens
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-5,5,5-trifluoro-D-leucinamide
-
 Homo sapiens
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-D-leucinamide
-
 Homo sapiens
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-L-isoleucinamide
-
 Homo sapiens
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-L-leucinamide
-
 Homo sapiens
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-L-norleucinamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens ?
-
 ?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000025
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[(4-methylpiperazin-1-yl)amino]-1,3-thiazol-4-yl)benzamide
-
 Homo sapiens
0.00000029
-
 4-[2-(4-tert-butylpiperazin-1-yl)-1,3-thiazol-4-yl]-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
 Homo sapiens
0.00000045
-
 4-[2-(1,4'-bipiperidin-1'-yl)-1,3-thiazol-4-yl]-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
 Homo sapiens
0.00000047
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[4-(tetrahydro-2H-pyran-4-yl)piperazin-1-yl]-1,3-thiazol-4-yl)benzamide
-
 Homo sapiens
0.00000048
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[4-(2-methoxyethyl)piperazin-1-yl]-1,3-thiazol-4-yl)benzamide
-
 Homo sapiens
0.00000057
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(piperidin-4-yloxy)-1,3-thiazol-4-yl]benzamide
-
 Homo sapiens
0.00000059
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-(4-[(1-methylethyl)amino]piperidin-1-yl)-1,3-thiazol-4-yl)benzamide
-
 Homo sapiens
0.00000067
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-[(1-methylpiperidin-3-yl)oxy]biphenyl-4-carboxamide
-
 Homo sapiens
0.00000079
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[3-(dimethylamino)pyrrolidin-1-yl]-1,3-thiazol-4-yl)benzamide
-
 Homo sapiens
0.00000094
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(1-methylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
-
 Homo sapiens
0.00000095
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(1,4-dimethylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
-
 Homo sapiens
0.0000014
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(4-propylpiperazin-1-yl)benzamide
-
 Homo sapiens
0.0000014
-
 4-(2-[(3R)-3-aminopyrrolidin-1-yl]-1,3-thiazol-4-yl)-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
 Homo sapiens
0.0000015
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(4-methylpiperazin-1-yl)benzamide
-
 Homo sapiens
0.0000016
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[(4-methylpiperazin-1-yl)methyl]-1,3-thiazol-4-yl)benzamide
-
 Homo sapiens
0.0000016
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-(4-[methyl(1-methylethyl)amino]piperidin-1-yl)-1,3-thiazol-4-yl)benzamide
-
 Homo sapiens
0.000002
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-(dimethylamino)biphenyl-4-carboxamide
-
 Homo sapiens
0.0000023
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-morpholin-4-yl-1,3-thiazol-4-yl)benzamide
-
 Homo sapiens
0.0000025
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-piperazin-1-ylbiphenyl-4-carboxamide Ki-value is below 0.0000025 mM Homo sapiens
0.0000025
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-([1-(2-hydroxyethyl)piperidin-4-yl]oxy)biphenyl-4-carboxamide Ki-value is below 0.0000025 mM Homo sapiens
0.0000025
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-[methyl(1-methylpyrrolidin-3-yl)amino]biphenyl-4-carboxamide Ki-value is below 0.0000025 mM Homo sapiens
0.0000025
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-[(1-methylpiperidin-4-yl)oxy]biphenyl-4-carboxamide Ki-value is below 0.0000025 mM Homo sapiens
0.0000025
-
 4'-(4-tert-butylpiperazin-1-yl)-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-4-carboxamide Ki-value is below 0.0000025 mM Homo sapiens
0.0000025
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-(piperazin-1-ylsulfonyl)biphenyl-4-carboxamide Ki-value is below 0.0000025 mM Homo sapiens
0.0000025
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-(4-fluoropiperidin-4-yl)biphenyl-4-carboxamide Ki-value is below 0.0000025 mM Homo sapiens
0.0000025
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-([(2S)-1-methylpyrrolidin-2-yl]methoxy)biphenyl-4-carboxamide Ki-value is below 0.0000025 mM Homo sapiens
0.0000025
-
 3-(4-([4'-((1-[(cyanomethyl)carbamoyl]cyclohexyl)carbamoyl)biphenyl-4-yl]oxy)piperidin-1-yl)propanoic acid Ki-value is below 0.0000025 mM Homo sapiens
0.0000025
-
 4'-[4-(tert-butylamino)piperidin-1-yl]-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-4-carboxamide Ki-value is below 0.0000025 mM Homo sapiens
0.0000025
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(4-morpholin-4-ylpiperidin-1-yl)-1,3-thiazol-4-yl]benzamide Ki-value is below 0.0000025 mM Homo sapiens
0.0000033
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(dimethylamino)benzamide
-
 Homo sapiens
0.0000054
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-isoxazol-5-ylbiphenyl-4-carboxamide
-
 Homo sapiens
0.0000061
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-([4-(2,2,2-trifluoroethyl)piperazin-1-yl]sulfonyl)biphenyl-4-carboxamide
-
 Homo sapiens
0.0000062
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-4-carboxamide
-
 Homo sapiens
0.0000087
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(morpholin-4-ylmethyl)-1,3-thiazol-4-yl]benzamide
-
 Homo sapiens
0.000013
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[(4-methylpiperazin-1-yl)sulfonyl]benzamide
-
 Homo sapiens
0.000013
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-ethynylbenzamide
-
 Homo sapiens
0.000014
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[(4-methylpiperazin-1-yl)carbonyl]benzamide
-
 Homo sapiens
0.000016
-
 5-bromo-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)thiophene-2-carboxamide
-
 Homo sapiens
0.000018
-
 4-bromo-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
 Homo sapiens
0.000019
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-morpholin-4-ylbenzamide
-
 Homo sapiens
0.000032
-
 4-amino-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
 Homo sapiens
0.0000347
-
 N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-L-leucinamide
-
 Homo sapiens
0.00015
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-2-pyridin-4-yl-1,3-thiazole-4-carboxamide
-
 Homo sapiens
0.00021
-
 N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-3-carboxamide
-
 Homo sapiens
0.00023
-
 3-bromo-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
 Homo sapiens
0.00035
-
 N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-5,5,5-trifluoro-D-leucinamide
-
 Homo sapiens
0.00041
-
 N-(cyanomethyl)-1-[(3-phenylpropanoyl)amino]cyclohexanecarboxamide
-
 Homo sapiens
0.00049
-
 N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-L-norleucinamide
-
 Homo sapiens
0.0015
-
 N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-L-isoleucinamide
-
 Homo sapiens
0.011
-
 benzyl (1-[(cyanomethyl)carbamoyl]-2-hydroxypropyl)carbamate
-
 Homo sapiens
0.013
-
 N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-D-leucinamide
-
 Homo sapiens
0.03
-
 benzyl [(1S)-2-[(cyanomethyl)amino]-1-(naphthalen-2-ylmethyl)-2-oxoethyl]carbamate
-
 Homo sapiens