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Literature summary for 3.4.22.27 extracted from

  • Ameriks, M.K.; Axe, F.U.; Bembenek, S.D.; Edwards, J.P.; Gu, Y.; Karlsson, L.; Randal, M.; Sun, S.; Thurmond, R.L.; Zhu, J.
    Pyrazole-based cathepsin S inhibitors with arylalkynes as P1 binding elements (2009), Bioorg. Med. Chem. Lett., 19, 6131-6134.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(furan-2-yl)methanone
-
Homo sapiens
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(pyridin-2-yl)methanone
-
Homo sapiens
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(tetrahydrofuran-2-yl)methanone
-
Homo sapiens
1-(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)-2-hydroxyethanone
-
Homo sapiens
2-(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)-2-oxoethyl acetate
-
Homo sapiens
3-(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)prop-2-yn-1-ol
-
Homo sapiens
3-(4-chloro-3-ethynylphenyl)-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-(trifluoromethyl)phenyl]ethynyl]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-[[3-(trifluoromethyl)phenyl]ethynyl]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-[[4-(trifluoromethyl)phenyl]ethynyl]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-(4-methylpent-1-yn-1-yl)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-(cyclohexylethynyl)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-(hept-1-yn-1-yl)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-(phenylethynyl)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-(thiophen-2-ylethynyl)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-(thiophen-3-ylethynyl)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-chlorophenyl)ethynyl]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-methoxyphenyl)ethynyl]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-methylphenyl)ethynyl]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-[(3,4-dichlorophenyl)ethynyl]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-[(3-chlorophenyl)ethynyl]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-[(4-chlorophenyl)ethynyl]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-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
Mus musculus
3-[4-chloro-3-[(4-methoxyphenyl)ethynyl]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-[(4-methylphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
Homo sapiens
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]aniline
-
Homo sapiens
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]benzoic acid
-
Homo sapiens
methyl (3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(oxo)acetate
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
-
-

Synonyms

Synonyms Comment Organism
cathepsin S
-
Mus musculus
cathepsin S
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00004
-
-
Homo sapiens methyl (3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(oxo)acetate
0.00014
-
-
Homo sapiens (3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(pyridin-2-yl)methanone
0.0002
-
-
Homo sapiens 3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.00022
-
-
Homo sapiens 1-(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)-2-hydroxyethanone
0.00028
-
-
Homo sapiens 3-[4-chloro-3-[(4-methylphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.00028
-
-
Homo sapiens 3-(4-chloro-3-[[4-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.00028
-
-
Homo sapiens 2-(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)-2-oxoethyl acetate
0.00031
-
-
Homo sapiens (3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(tetrahydrofuran-2-yl)methanone
0.00032
-
-
Homo sapiens 3-[4-chloro-3-[(3,4-dichlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.00033
-
-
Homo sapiens (3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(furan-2-yl)methanone
0.00043
-
-
Homo sapiens 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]aniline
0.00048
-
-
Homo sapiens 3-[4-chloro-3-[(4-methoxyphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.00051
-
-
Homo sapiens 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]benzoic acid
0.00055
-
-
Homo sapiens 3-[4-chloro-3-[(2-methoxyphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.00061
-
-
Homo sapiens 3-[4-chloro-3-(phenylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.00069
-
-
Mus musculus 3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.0007
-
-
Homo sapiens 3-[4-chloro-3-[(3-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.00072
-
-
Homo sapiens 3-[4-chloro-3-[(2-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.00079
-
-
Homo sapiens 3-[4-chloro-3-(thiophen-2-ylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.00087
-
-
Homo sapiens 3-(4-chloro-3-[[2-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.0011
-
-
Homo sapiens 3-[4-chloro-3-[(2-methylphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.0015
-
-
Homo sapiens 3-(4-chloro-3-[[3-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.0015
-
-
Homo sapiens 3-[4-chloro-3-(thiophen-3-ylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.0067
-
-
Homo sapiens 3-[4-chloro-3-(cyclohexylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.0074
-
-
Homo sapiens 3-(4-chloro-3-ethynylphenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.0079
-
-
Homo sapiens 3-(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)prop-2-yn-1-ol
0.0083
-
-
Homo sapiens 3-[4-chloro-3-(4-methylpent-1-yn-1-yl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.011
-
-
Homo sapiens 3-[4-chloro-3-(hept-1-yn-1-yl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine