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Literature summary for 3.4.22.27 extracted from

  • Lee-Dutra, A.; Wiener, D.K.; Arienti, K.L.; Liu, J.; Mani, N.; Ameriks, M.K.; Axe, F.U.; Gebauer, D.; Desai, P.J.; Nguyen, S.; Randal, M.; Thurmond, R.L.; Sun, S.; Karlsson, L.; Edwards, J.P.; Jones, T.K.; Grice, C.A.
    Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors: part 1 (2010), Bioorg. Med. Chem. Lett., 20, 2370-2374.
    View publication on PubMed
Search for more literature for 3.4.22.27

Inhibitors

Inhibitors Comment Organism Structure
1-(1-[3-[3-[3-[(2-hydroxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)pyrrolidin-2-one
-
 Homo sapiens
1-(1-[3-[5-(methylsulfonyl)-3-[3-[(2-phenoxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)pyrrolidin-2-one
-
 Homo sapiens
1-[1-(3-[3-[3-([2-[benzyl(methyl)amino]ethyl]sulfanyl)-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
 Homo sapiens
1-[1-(3-[3-[3-[[2-(4-hydroxypiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
 Homo sapiens
1-[1-(3-[3-[3-[[2-(4-methylpiperazin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
 Homo sapiens
1-[1-(3-[3-[3-[[2-(4-methylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
 Homo sapiens
1-[1-(3-[3-[3-[[2-(4-tert-butylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
 Homo sapiens
1-[1-(3-[3-[3-[[2-(benzylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
 Homo sapiens
1-[1-(3-[3-[3-[[2-(dimethylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
 Homo sapiens
1-[1-(3-[3-[3-[[2-(methylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
 Homo sapiens
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(4-phenylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
 Homo sapiens
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
 Homo sapiens
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(octahydroisoquinolin-2(1H)-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
 Homo sapiens
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
 Homo sapiens
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
 Homo sapiens
2-[(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)sulfanyl]ethanol
-
 Homo sapiens
3-[3-(benzylsulfanyl)-4-chlorophenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
 Homo sapiens
3-[4-chloro-3-(propylsulfanyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
 Homo sapiens
3-[4-chloro-3-[(2-phenoxyethyl)sulfanyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
 Homo sapiens
3-[4-chloro-3-[(2-phenylethyl)sulfanyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
 Homo sapiens
4-(dimethylamino)-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
-
 Homo sapiens
4-fluoro-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
-
 Homo sapiens
4-hydroxy-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
-
 Homo sapiens
4-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
 Homo sapiens
5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-3-[3-[(2-phenoxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
 Homo sapiens
5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
 Homo sapiens
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-(piperidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
 Homo sapiens
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-(pyrrolidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
 Homo sapiens
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-[4-(pyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
 Homo sapiens
N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]-2-phenylacetamide
-
 Homo sapiens
N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
-
 Homo sapiens
N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]piperidine-3-carboxamide
-
 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
0.00003
-
-
 Homo sapiens 4-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
0.000055
-
-
 Homo sapiens 1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(octahydroisoquinolin-2(1H)-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
0.00011
-
-
 Homo sapiens 1-[1-(3-[3-[3-[[2-(4-methylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
0.00013
-
-
 Homo sapiens N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]-2-phenylacetamide
0.00016
-
-
 Homo sapiens 1-[1-(3-[3-[3-[[2-(4-tert-butylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
0.00017
-
-
 Homo sapiens 1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
0.0002
-
-
 Homo sapiens 1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(4-phenylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
0.0002
-
-
 Homo sapiens 1-(1-[3-[3-[3-[(2-hydroxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)pyrrolidin-2-one
0.00022
-
-
 Homo sapiens 1-(1-[3-[5-(methylsulfonyl)-3-[3-[(2-phenoxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)pyrrolidin-2-one
0.00027
-
-
 Homo sapiens 1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
0.00034
-
-
 Homo sapiens 1-[1-(3-[3-[3-[[2-(4-hydroxypiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
0.00036
-
-
 Homo sapiens 4-fluoro-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
0.00038
-
-
 Homo sapiens N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
0.00038
-
-
 Homo sapiens 5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-(piperidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.00039
-
-
 Homo sapiens 4-hydroxy-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
0.00041
-
-
 Homo sapiens 1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
0.00042
-
-
 Homo sapiens N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]piperidine-3-carboxamide
0.00052
-
-
 Homo sapiens 5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-(pyrrolidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.00053
-
-
 Homo sapiens 4-(dimethylamino)-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
0.00056
-
-
 Homo sapiens 5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-[4-(pyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.0006
-
-
 Homo sapiens 3-[4-chloro-3-[(2-phenoxyethyl)sulfanyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.0007
-
-
 Homo sapiens 1-[1-(3-[3-[3-[[2-(benzylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
0.00074
-
-
 Homo sapiens 5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-3-[3-[(2-phenoxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.0008
-
-
 Homo sapiens 1-[1-(3-[3-[3-[[2-(methylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
0.00081
-
-
 Homo sapiens 5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.00096
-
-
 Homo sapiens 2-[(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)sulfanyl]ethanol
0.00106
-
-
 Homo sapiens 1-[1-(3-[3-[3-[[2-(4-methylpiperazin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
0.00128
-
-
 Homo sapiens 1-[1-(3-[3-[3-[[2-(dimethylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
0.00147
-
-
 Homo sapiens 3-[4-chloro-3-[(2-phenylethyl)sulfanyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.00165
-
-
 Homo sapiens 3-[3-(benzylsulfanyl)-4-chlorophenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.00201
-
-
 Homo sapiens 1-[1-(3-[3-[3-([2-[benzyl(methyl)amino]ethyl]sulfanyl)-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
0.0036
-
-
 Homo sapiens 3-[4-chloro-3-(propylsulfanyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine