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Literature summary for 3.4.22.27 extracted from

  • Ameriks, M.K.; Cai, H.; Edwards, J.P.; Gebauer, D.; Gleason, E.; Gu, Y.; Karlsson, L.; Nguyen, S.; Sun, S.; Thurmond, R.L.; Zhu, J.
    Pyrazole-based arylalkyne cathepsin S inhibitors. Part II: optimization of cellular potency (2009), Bioorg. Med. Chem. Lett., 19, 6135-6139.
    View publication on PubMed
Search for more literature for 3.4.22.27

Inhibitors

Inhibitors Comment Organism Structure
(2R)-2-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)-2-phenylethanol
-
 Homo sapiens
(2S)-1-(4,4'-bipiperidin-1-yl)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
-
 Homo sapiens
(2S)-1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(1'-methyl-4,4'-bipiperidin-1-yl)propan-2-ol
-
 Homo sapiens
1-(1'-[(2S)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]-4,4'-bipiperidin-1-yl)ethanone
-
 Homo sapiens
1-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidine-4-carboxamide
-
 Homo sapiens
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(morpholin-4-yl)propan-2-ol
-
 Homo sapiens
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperazin-1-yl)propan-2-ol
-
 Homo sapiens
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
 Homo sapiens
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(3,4-dichlorobenzyl)methanamine
-
 Homo sapiens
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(4-methoxybenzyl)methanamine
-
 Homo sapiens
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(4-methylbenzyl)methanamine
-
 Homo sapiens
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-methylmethanamine
-
 Homo sapiens
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
-
 Homo sapiens
methyl (2R)-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)(phenyl)ethanoate
-
 Homo sapiens
methyl (2S)-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)(phenyl)ethanoate
-
 Homo sapiens
methyl 1-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidine-4-carboxylate
-
 Homo sapiens
N-(4-chlorobenzyl)-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
-
 Homo sapiens
N-benzyl-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-methylmethanamine
-
 Homo sapiens
N-benzyl-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
-
 Homo sapiens
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]-1-phenylethanamine
-
 Homo sapiens
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]-2-phenylethanamine
-
 Homo sapiens
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]benzamide
-
 Homo sapiens
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]benzenesulfonamide
-
 Homo sapiens
tert-butyl 1'-[(2S)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]-4,4'-bipiperidine-1-carboxylate
-
 Homo sapiens
tert-butyl 4-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperazine-1-carboxylate
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
cathepsin S
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00001
-
-
 Homo sapiens tert-butyl 1'-[(2S)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]-4,4'-bipiperidine-1-carboxylate
0.00001
-
-
 Homo sapiens (2S)-1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(1'-methyl-4,4'-bipiperidin-1-yl)propan-2-ol
0.00001
-
-
 Homo sapiens 1-(1'-[(2S)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]-4,4'-bipiperidin-1-yl)ethanone
0.00002
-
-
 Homo sapiens methyl 1-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidine-4-carboxylate
0.00003
-
-
 Homo sapiens (2S)-1-(4,4'-bipiperidin-1-yl)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
0.00008
-
-
 Homo sapiens 1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(3,4-dichlorobenzyl)methanamine
0.00008
-
-
 Homo sapiens 1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
0.0001
-
-
 Homo sapiens methyl (2R)-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)(phenyl)ethanoate
0.0001
-
-
 Homo sapiens (2R)-2-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)-2-phenylethanol
0.00011
-
-
 Homo sapiens 1-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidine-4-carboxamide
0.00012
-
-
 Homo sapiens methyl (2S)-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)(phenyl)ethanoate
0.00014
-
-
 Homo sapiens N-(4-chlorobenzyl)-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
0.00014
-
-
 Homo sapiens 1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(morpholin-4-yl)propan-2-ol
0.00015
-
-
 Homo sapiens tert-butyl 4-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperazine-1-carboxylate
0.00016
-
-
 Homo sapiens N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]benzenesulfonamide
0.00019
-
-
 Homo sapiens N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]-1-phenylethanamine
0.00023
-
-
 Homo sapiens 1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(4-methoxybenzyl)methanamine
0.00035
-
-
 Homo sapiens N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]benzamide
0.00035
-
-
 Homo sapiens 1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(4-methylbenzyl)methanamine
0.00038
-
-
 Homo sapiens 1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperazin-1-yl)propan-2-ol
0.00042
-
-
 Homo sapiens N-benzyl-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
0.00049
-
-
 Homo sapiens 1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
0.00058
-
-
 Homo sapiens N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]-2-phenylethanamine
0.0006
-
-
 Homo sapiens N-benzyl-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-methylmethanamine
0.0013
-
-
 Homo sapiens 1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-methylmethanamine