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Literature summary for 3.4.22.27 extracted from

  • Grice, C.A.; Tays, K.; Khatuya, H.; Gustin, D.J.; Butler, C.R.; Wei, J.; Sehon, C.A.; Sun, S.; Gu, Y.; Jiang, W.; Thurmond, R.L.; Karlsson, L.; Edwards, J.P.
    The SAR of 4-substituted (6,6-bicyclic) piperidine cathepsin S inhibitors (2006), Bioorg. Med. Chem. Lett., 16, 2209-2212.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
4-[1-(2-hydroxy-3-[3-[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
4-[1-(3-[3-[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
4-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
Homo sapiens
4-[1-(3-[5-acetyl-3-[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
4-[1-(3-[5-tert-butoxy-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
Homo sapiens
4-[1-(3-[5-tert-butoxy-3-[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
methyl 1-[2-hydroxy-3-(4-quinolin-4-ylpiperazin-1-yl)propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 1-[2-hydroxy-3-[4-(2-oxo-2,3-dihydro-4,1-benzoxazepin-1(5H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 1-[2-hydroxy-3-[4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 1-[3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 1-[3-[4-(5-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 1-[3-[4-(6-chloro-2,2-dioxido-3,4-dihydro-1H-2,1,3-benzothiadiazin-1-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 3-(4-bromophenyl)-1-[3-[4-(3,4-dihydroisoquinolin-2(1H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 3-(4-bromophenyl)-1-[3-[4-(3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 3-(4-bromophenyl)-1-[3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 3-(4-bromophenyl)-1-[3-[4-(5-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2,2-dioxido-3,4-dihydro-1H-2,1,3-benzothiadiazin-1-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
CatS
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000013
-
-
Homo sapiens methyl 1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.000016
-
-
Homo sapiens methyl 1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.000018
-
-
Homo sapiens methyl 1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.000018
-
-
Homo sapiens methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.000023
-
-
Homo sapiens methyl 1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.000023
-
-
Homo sapiens methyl 1-[3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.000028
-
-
Homo sapiens methyl 1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.00003
-
-
Homo sapiens methyl 1-[3-[4-(6-chloro-2,2-dioxido-3,4-dihydro-1H-2,1,3-benzothiadiazin-1-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.000032
-
-
Homo sapiens methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.000033
-
-
Homo sapiens methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.000033
-
-
Homo sapiens methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.000048
-
-
Homo sapiens methyl 1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.000048
-
-
Homo sapiens methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.00006
-
-
Homo sapiens methyl 3-(4-bromophenyl)-1-[3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.000065
-
-
Homo sapiens methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.000068
-
-
Homo sapiens methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.000075
-
-
Homo sapiens methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2,2-dioxido-3,4-dihydro-1H-2,1,3-benzothiadiazin-1-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.00008
-
-
Homo sapiens methyl 1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.000088
-
-
Homo sapiens methyl 1-[2-hydroxy-3-[4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.0001
-
-
Homo sapiens 4-[1-(3-[5-acetyl-3-[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
0.00012
-
-
Homo sapiens 4-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
0.00013
-
-
Homo sapiens methyl 1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.00013
-
-
Homo sapiens methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.000133
-
-
Homo sapiens methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.000145
-
-
Homo sapiens methyl 1-[3-[4-(5-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.000163
-
-
Homo sapiens methyl 1-[2-hydroxy-3-[4-(2-oxo-2,3-dihydro-4,1-benzoxazepin-1(5H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.000322
-
-
Homo sapiens methyl 3-(4-bromophenyl)-1-[3-[4-(3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.000826
-
-
Homo sapiens 4-[1-(3-[5-tert-butoxy-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
0.0009
-
-
Homo sapiens 4-[1-(3-[5-tert-butoxy-3-[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
0.0017
-
-
Homo sapiens methyl 1-[2-hydroxy-3-(4-quinolin-4-ylpiperazin-1-yl)propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.0017
-
-
Homo sapiens methyl 3-(4-bromophenyl)-1-[3-[4-(5-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.001775
-
-
Homo sapiens methyl 3-(4-bromophenyl)-1-[3-[4-(3,4-dihydroisoquinolin-2(1H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
0.0018
-
-
Homo sapiens 4-[1-(3-[3-[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
0.001925
-
-
Homo sapiens 4-[1-(2-hydroxy-3-[3-[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