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Literature summary for 3.4.22.27 extracted from

  • Liu, H.; Tully, D.C.; Epple, R.; Bursulaya, B.; Li, J.; Harris, J.L.; Williams, J.A.; Russo, R.; Tumanut, C.; Roberts, M.J.; Alper, P.B.; He, Y.; Karanewsky, D.S.
    Design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 1 (2005), Bioorg. Med. Chem. Lett., 15, 4979-4984.
    View publication on PubMed
Search for more literature for 3.4.22.27

Inhibitors

Inhibitors Comment Organism Structure
2,3,4,5,6-pentafluoro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide IC50: 0.020 mM Homo sapiens
2-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide IC50: 35 nM Homo sapiens
3-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide IC50: 33 nM Homo sapiens
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-(naphthalen-2-ylacetyl)-L-alaninamide IC50: 5.0 nM Homo sapiens
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-([5-[3-(trifluoromethyl)phenyl]furan-2-yl]acetyl)-L-alaninamide IC50: 3.3 nM Homo sapiens
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(3-phenoxyphenyl)acetyl]-L-alaninamide IC50: 8.0 nM Homo sapiens
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(4-morpholin-4-ylphenyl)acetyl]-L-alaninamide IC50: 4.0 nM Homo sapiens
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(4-phenoxyphenyl)acetyl]-L-alaninamide IC50: 17 nM Homo sapiens
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(5-methyl-1-phenyl-1H-pyrazol-4-yl)acetyl]-L-alaninamide IC50: 34 nM Homo sapiens
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[[4-(1H-1,2,4-triazol-1-yl)phenyl]acetyl]-L-alaninamide IC50: 26 nM Homo sapiens
3-cyclohexyl-N2-([4-[(4,6-dimethylpyrimidin-2-yl)amino]phenyl]acetyl)-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide IC50: 2.0 nM Homo sapiens
4-(acetylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide IC50: 123 nM Homo sapiens
4-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide IC50: 16 nM Homo sapiens
additional information analysis of inhibition mechanisms and binding to the active site; design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S, overview Homo sapiens
N-[(1S)-1-(1H-indol-2-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide IC50: 29 nM Homo sapiens
N-[(1S)-1-(biphenyl-4-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide IC50: 34 nM Homo sapiens
N-[(1S)-1-(cyclohexylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide IC50: 62 nM Homo sapiens
N-[(1S)-1-(furan-2-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide IC50: 0.020 mM Homo sapiens
N-[(1S)-1-cyclohexyl-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide IC50: 23 nM Homo sapiens
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-1-(naphthalen-2-ylmethyl)-2-oxoethyl]-3-methylbenzamide IC50: 16 nM Homo sapiens
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(1,3-thiazol-5-ylmethyl)ethyl]-3-methylbenzamide IC50: 0.065 mM Homo sapiens
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(pyridin-3-ylmethyl)ethyl]-3-methylbenzamide IC50: 3707 nM Homo sapiens
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(pyridin-4-ylmethyl)ethyl]-3-methylbenzamide IC50: 6769 nM Homo sapiens
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-phenylethyl]-3-methylbenzamide IC50: 285 nM Homo sapiens
N-[(1S)-3-cyclohexyl-1-([2-[(4-methoxyphenyl)amino]ethyl]carbamoyl)propyl]-3-methylbenzamide IC50: 38 nM Homo sapiens
N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-N2-[(3-methylphenyl)carbonyl]-L-leucinamide IC50: 46 nM Homo sapiens
N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide IC50: 27 nM Homo sapiens
N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(3-methylphenyl)carbonyl]-L-leucinamide IC50: 62 nM Homo sapiens
N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-4-(trifluoromethyl)-L-phenylalaninamide IC50: 19 nM Homo sapiens
N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide IC50: 29 nM Homo sapiens
N-[2-[(4-methoxyphenyl)amino]ethyl]-O-methyl-Na-[(3-methylphenyl)carbonyl]-L-tyrosinamide IC50: 66 nM Homo sapiens
N2-(biphenyl-3-ylacetyl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide IC50: 2.9 nM Homo sapiens
N2-(biphenyl-4-ylacetyl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide IC50: 9.1 nM Homo sapiens
N2-[(3'-chlorobiphenyl-4-yl)acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide IC50: 7.4 nM Homo sapiens
N2-[(5-chloro-1-benzofuran-2-yl)acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide IC50: 9.4 nM Homo sapiens
N2-[[1-(5-bromopyrimidin-2-yl)piperidin-3-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide IC50: 49 nM Homo sapiens
N2-[[1-(5-bromopyrimidin-2-yl)piperidin-4-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide IC50: 107 nM Homo sapiens
N2-[[5-(4-chlorophenyl)furan-2-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide IC50: 7.1 nM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000002
-
 IC50: 2.0 nM Homo sapiens 3-cyclohexyl-N2-([4-[(4,6-dimethylpyrimidin-2-yl)amino]phenyl]acetyl)-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
0.0000029
-
 IC50: 2.9 nM Homo sapiens N2-(biphenyl-3-ylacetyl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
0.0000033
-
 IC50: 3.3 nM Homo sapiens 3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-([5-[3-(trifluoromethyl)phenyl]furan-2-yl]acetyl)-L-alaninamide
0.000004
-
 IC50: 4.0 nM Homo sapiens 3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(4-morpholin-4-ylphenyl)acetyl]-L-alaninamide
0.000005
-
 IC50: 5.0 nM Homo sapiens 3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-(naphthalen-2-ylacetyl)-L-alaninamide
0.0000071
-
 IC50: 7.1 nM Homo sapiens N2-[[5-(4-chlorophenyl)furan-2-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
0.0000074
-
 IC50: 7.4 nM Homo sapiens N2-[(3'-chlorobiphenyl-4-yl)acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
0.000008
-
 IC50: 8.0 nM Homo sapiens 3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(3-phenoxyphenyl)acetyl]-L-alaninamide
0.0000091
-
 IC50: 9.1 nM Homo sapiens N2-(biphenyl-4-ylacetyl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
0.0000094
-
 IC50: 9.4 nM Homo sapiens N2-[(5-chloro-1-benzofuran-2-yl)acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
0.000016
-
 IC50: 16 nM Homo sapiens 4-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
0.000016
-
 IC50: 16 nM Homo sapiens N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-1-(naphthalen-2-ylmethyl)-2-oxoethyl]-3-methylbenzamide
0.000017
-
 IC50: 17 nM Homo sapiens 3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(4-phenoxyphenyl)acetyl]-L-alaninamide
0.000019
-
 IC50: 19 nM Homo sapiens N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-4-(trifluoromethyl)-L-phenylalaninamide
0.000023
-
 IC50: 23 nM Homo sapiens N-[(1S)-1-cyclohexyl-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
0.000026
-
 IC50: 26 nM Homo sapiens 3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[[4-(1H-1,2,4-triazol-1-yl)phenyl]acetyl]-L-alaninamide
0.000027
-
 IC50: 27 nM Homo sapiens N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
0.000029
-
 IC50: 29 nM Homo sapiens N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
0.000029
-
 IC50: 29 nM Homo sapiens N-[(1S)-1-(1H-indol-2-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
0.000033
-
 IC50: 33 nM Homo sapiens 3-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
0.000034
-
 IC50: 34 nM Homo sapiens N-[(1S)-1-(biphenyl-4-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
0.000034
-
 IC50: 34 nM Homo sapiens 3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(5-methyl-1-phenyl-1H-pyrazol-4-yl)acetyl]-L-alaninamide
0.000035
-
 IC50: 35 nM Homo sapiens 2-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
0.000038
-
 IC50: 38 nM Homo sapiens N-[(1S)-3-cyclohexyl-1-([2-[(4-methoxyphenyl)amino]ethyl]carbamoyl)propyl]-3-methylbenzamide
0.000046
-
 IC50: 46 nM Homo sapiens N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-N2-[(3-methylphenyl)carbonyl]-L-leucinamide
0.000049
-
 IC50: 49 nM Homo sapiens N2-[[1-(5-bromopyrimidin-2-yl)piperidin-3-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
0.000062
-
 IC50: 62 nM Homo sapiens N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(3-methylphenyl)carbonyl]-L-leucinamide
0.000062
-
 IC50: 62 nM Homo sapiens N-[(1S)-1-(cyclohexylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
0.000066
-
 IC50: 66 nM Homo sapiens N-[2-[(4-methoxyphenyl)amino]ethyl]-O-methyl-Na-[(3-methylphenyl)carbonyl]-L-tyrosinamide
0.000107
-
 IC50: 107 nM Homo sapiens N2-[[1-(5-bromopyrimidin-2-yl)piperidin-4-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
0.000123
-
 IC50: 123 nM Homo sapiens 4-(acetylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
0.000285
-
 IC50: 285 nM Homo sapiens N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-phenylethyl]-3-methylbenzamide
0.003707
-
 IC50: 3707 nM Homo sapiens N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(pyridin-3-ylmethyl)ethyl]-3-methylbenzamide
0.006769
-
 IC50: 6769 nM Homo sapiens N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(pyridin-4-ylmethyl)ethyl]-3-methylbenzamide
0.02
-
 IC50: 0.020 mM Homo sapiens N-[(1S)-1-(furan-2-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
0.02
-
 IC50: 0.020 mM Homo sapiens 2,3,4,5,6-pentafluoro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
0.065
-
 IC50: 0.065 mM Homo sapiens N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(1,3-thiazol-5-ylmethyl)ethyl]-3-methylbenzamide