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Literature summary for 3.4.22.38 extracted from

  • Shinozuka, T.; Shimada, K.; Matsui, S.; Yamane, T.; Ama, M.; Fukuda, T.; Taki, M.; Naito, S.
    4-Aminophenoxyacetic acids as a novel class of reversible cathepsin K inhibitors (2006), Bioorg. Med. Chem. Lett., 16, 1502-1505.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
DTT
-
Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2S)-2-(biphenyl-2-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
-
Homo sapiens
(2S)-2-(biphenyl-3-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
-
Homo sapiens
(2S)-2-(biphenyl-4-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
-
Homo sapiens
(2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-(3-phenoxyphenoxy)pentanamide
-
Homo sapiens
(2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-(4-phenoxyphenoxy)pentanamide
-
Homo sapiens
(2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-phenoxypentanamide
-
Homo sapiens
1-(4-cyclohexylphenoxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
Homo sapiens
1-(4-ethylphenoxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
Homo sapiens
1-(biphenyl-2-ylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
Homo sapiens
1-(biphenyl-3-ylamino)-N-[(1R)-2-[(4-methoxyphenyl)amino]-1-methylethyl]cyclohexanecarboxamide
-
Homo sapiens
1-(biphenyl-3-ylamino)-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]butyl]cyclohexanecarboxamide
-
Homo sapiens
1-(biphenyl-3-ylamino)-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]pentyl]cyclohexanecarboxamide
-
Homo sapiens
1-(biphenyl-3-ylamino)-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]propyl]cyclohexanecarboxamide
-
Homo sapiens
1-(biphenyl-3-ylamino)-N-[(1S)-2-[(4-methoxyphenyl)amino]-1-methylethyl]cyclohexanecarboxamide
-
Homo sapiens
1-(biphenyl-3-ylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
Homo sapiens
1-(biphenyl-3-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
Homo sapiens
1-(biphenyl-4-ylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
Homo sapiens
1-(biphenyl-4-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
Homo sapiens
3-(4-[[(2S)-2-([[1-(biphenyl-3-ylamino)cyclohexyl]carbonyl]amino)butyl]amino]phenoxy)propanoic acid
-
Homo sapiens
3-[4-([(2S)-2-[(N-biphenyl-3-yl-L-leucyl)amino]butyl]amino)phenoxy]propanoic acid
-
Homo sapiens
N-[2-[(4-methoxyphenyl)amino]ethyl]-1-(phenylamino)cyclohexanecarboxamide
-
Homo sapiens
N-[2-[(4-methoxyphenyl)amino]ethyl]-1-phenoxycyclohexanecarboxamide
-
Homo sapiens
N-[2-[(4-methoxyphenyl)amino]ethyl]-1-[4-(1-methylethyl)phenoxy]cyclohexanecarboxamide
-
Homo sapiens
N2-(3-cyclohexylphenyl)-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-leucinamide
-
Homo sapiens
N2-biphenyl-3-yl-N-[(1S)-1-[([4-[2-(1H-tetrazol-5-yl)ethoxy]phenyl]amino)methyl]propyl]-L-leucinamide
-
Homo sapiens
N2-biphenyl-3-yl-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]propyl]-L-leucinamide
-
Homo sapiens
N2-biphenyl-3-yl-N-[(1S)-2-[(4-methoxyphenyl)amino]-1-methylethyl]-L-leucinamide
-
Homo sapiens
N2-biphenyl-3-yl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-leucinamide
-
Homo sapiens
N2-[(benzyloxy)carbonyl]-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-leucinamide
-
Homo sapiens
tert-butyl 3-(4-[[(2S)-2-([[1-(biphenyl-3-ylamino)cyclohexyl]carbonyl]amino)butyl]amino]phenoxy)propanoate
-
Homo sapiens
tert-butyl 3-[4-([(2S)-2-[(N-biphenyl-3-yl-L-leucyl)amino]butyl]amino)phenoxy]propanoate
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
cathepsin K
-
Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
3.8
-
assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000027
-
-
Homo sapiens 1-(biphenyl-3-ylamino)-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]propyl]cyclohexanecarboxamide
0.0000038
-
-
Homo sapiens N2-biphenyl-3-yl-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]propyl]-L-leucinamide
0.0000039
-
-
Homo sapiens 1-(biphenyl-3-ylamino)-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]butyl]cyclohexanecarboxamide
0.0000045
-
-
Homo sapiens 3-[4-([(2S)-2-[(N-biphenyl-3-yl-L-leucyl)amino]butyl]amino)phenoxy]propanoic acid
0.0000048
-
-
Homo sapiens 3-(4-[[(2S)-2-([[1-(biphenyl-3-ylamino)cyclohexyl]carbonyl]amino)butyl]amino]phenoxy)propanoic acid
0.0000048
-
-
Homo sapiens tert-butyl 3-(4-[[(2S)-2-([[1-(biphenyl-3-ylamino)cyclohexyl]carbonyl]amino)butyl]amino]phenoxy)propanoate
0.0000056
-
-
Homo sapiens 1-(biphenyl-3-ylamino)-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]pentyl]cyclohexanecarboxamide
0.0000064
-
-
Homo sapiens tert-butyl 3-[4-([(2S)-2-[(N-biphenyl-3-yl-L-leucyl)amino]butyl]amino)phenoxy]propanoate
0.00001
-
-
Homo sapiens N2-biphenyl-3-yl-N-[(1S)-2-[(4-methoxyphenyl)amino]-1-methylethyl]-L-leucinamide
0.000011
-
-
Homo sapiens N2-biphenyl-3-yl-N-[(1S)-1-[([4-[2-(1H-tetrazol-5-yl)ethoxy]phenyl]amino)methyl]propyl]-L-leucinamide
0.000019
-
-
Homo sapiens 1-(biphenyl-3-ylamino)-N-[(1S)-2-[(4-methoxyphenyl)amino]-1-methylethyl]cyclohexanecarboxamide
0.00004
-
-
Homo sapiens N2-biphenyl-3-yl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-leucinamide
0.00006
-
-
Homo sapiens N2-(3-cyclohexylphenyl)-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-leucinamide
0.000069
-
-
Homo sapiens (2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-(3-phenoxyphenoxy)pentanamide
0.000082
-
-
Homo sapiens 1-(biphenyl-3-ylamino)-N-[(1R)-2-[(4-methoxyphenyl)amino]-1-methylethyl]cyclohexanecarboxamide
0.000083
-
-
Homo sapiens 1-(biphenyl-3-ylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
0.00009
-
-
Homo sapiens (2S)-2-(biphenyl-3-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
0.00009
-
-
Homo sapiens N2-[(benzyloxy)carbonyl]-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-leucinamide
0.000099
-
-
Homo sapiens 1-(4-cyclohexylphenoxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
0.0001
-
-
Homo sapiens (2S)-2-(biphenyl-4-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
0.0001
-
-
Homo sapiens 1-(biphenyl-4-ylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
0.00013
-
-
Homo sapiens 1-(4-ethylphenoxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
0.00019
-
-
Homo sapiens 1-(biphenyl-4-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
0.0002
-
-
Homo sapiens N-[2-[(4-methoxyphenyl)amino]ethyl]-1-[4-(1-methylethyl)phenoxy]cyclohexanecarboxamide
0.00032
-
-
Homo sapiens 1-(biphenyl-3-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
0.0006
-
-
Homo sapiens (2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-(4-phenoxyphenoxy)pentanamide
0.0012
-
-
Homo sapiens (2S)-2-(biphenyl-2-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
0.003
-
-
Homo sapiens (2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-phenoxypentanamide
0.003
-
-
Homo sapiens N-[2-[(4-methoxyphenyl)amino]ethyl]-1-phenoxycyclohexanecarboxamide
0.011
-
-
Homo sapiens N-[2-[(4-methoxyphenyl)amino]ethyl]-1-(phenylamino)cyclohexanecarboxamide
0.02
-
value above 20 mM Homo sapiens 1-(biphenyl-2-ylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide