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Literature summary for 3.4.22.27 extracted from

  • Gustin, D.J.; Sehon, C.A.; Wei, J.; Cai, H.; Meduna, S.P.; Khatuya, H.; Sun, S.; Gu, Y.; Jiang, W.; Thurmond, R.L.; Karlsson, L.; Edwards, J.P.
    Discovery and SAR studies of a novel series of noncovalent cathepsin S inhibitors (2005), Bioorg. Med. Chem. Lett., 15, 1687-1691.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1-(1-[(2R)-3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one IC50: 350 nM Homo sapiens
1-(1-[(2S)-3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one IC50: 190 nM Homo sapiens
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one IC50: 10 nM Homo sapiens
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one IC50: 50 nM Homo sapiens
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one IC50: 50 nM Homo sapiens
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one IC50: 50 nM Homo sapiens
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one IC50: 140 nM Homo sapiens
1-(1-[3-[3-(4-chloro-3-methylphenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one IC50: 60 nM Homo sapiens
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one IC50: 80 nM Homo sapiens
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5,6-dichloro-1,3-dihydro-2H-benzimidazol-2-one IC50: 110 nM Homo sapiens
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methoxy-1,3-dihydro-2H-benzimidazol-2-one IC50: 140 nM Homo sapiens
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methyl-1,3-dihydro-2H-benzimidazol-2-one IC50: 90 nM Homo sapiens
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one IC50: 120 nM Homo sapiens
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-7-methyl-1,3-dihydro-2H-benzimidazol-2-one IC50: 210 nM Homo sapiens
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one IC50: 130 nM Homo sapiens
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-(2,2,2-trifluoroethyl)-1,3-dihydro-2H-benzimidazol-2-one IC50: 90 nM Homo sapiens
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-butyl-1,3-dihydro-2H-benzimidazol-2-one IC50: 140 nM Homo sapiens
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one IC50: 310 nM Homo sapiens
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one IC50: 500 nM Homo sapiens
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-tert-butyl-1,3-dihydro-2H-benzimidazol-2-one IC50: 100 nM Homo sapiens
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methyl-1,3-dihydro-2H-benzimidazol-2-one IC50: 100 nM Homo sapiens
1-(1-[3-[5-acetyl-3-(4-chlorophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one IC50: 460 nM Homo sapiens
1-(1-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one IC50: 120 nM Homo sapiens
1-(1-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-fluoro-1,3-dihydro-2H-benzimidazol-2-one IC50: 230 nM Homo sapiens
1-(ethenylideneamino)-3-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one IC50: 100 nM Homo sapiens
1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one IC50: 50 nM Homo sapiens
1-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one IC50: 50 nM Homo sapiens
1-[1-(3-[5-acetyl-3-[4-(trifluoromethoxy)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one IC50: 130 nM Homo sapiens
1-[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]-1,3-dihydro-2H-benzimidazol-2-one IC50: 100 nM Homo sapiens
1-[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]-3-methyl-1,3-dihydro-2H-benzimidazol-2-one IC50: 110 nM Homo sapiens
1-[1-[(2R)-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]-6-chloro-1,3-dihydro-2H-benzimidazol-2-one IC50: 180 nM Homo sapiens
1-[1-[(2S)-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]-6-chloro-1,3-dihydro-2H-benzimidazol-2-one IC50: 200 nM Homo sapiens
1-[3-[4-(2-cyanophenyl)piperazin-1-yl]-2-hydroxypropyl]-3-(4-iodophenyl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide IC50: 50 nM Homo sapiens
2-(4-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperazin-1-yl)benzonitrile IC50: 120 nM Homo sapiens
2-[5-carbamoyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-1-[[4-(2-cyanophenyl)piperazin-1-yl]methyl]ethyl carbamate IC50: 20 nM Homo sapiens
3-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,5-dimethyl-1,3-dihydro-2H-benzimidazol-2-one IC50: 30 nM Homo sapiens
5-chloro-3-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1-methyl-1,3-dihydro-2H-benzimidazol-2-one IC50: 150 nM Homo sapiens
5-chloro-3-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1-methyl-1,3-dihydro-2H-benzimidazol-2-one IC50: 80 nM Homo sapiens
6-chloro-1-(1-[3-[3-(4-chloro-3-methylphenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one IC50: 50 nM Homo sapiens
6-chloro-1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one IC50: 60 nM Homo sapiens
6-chloro-1-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one IC50: 30 nM Homo sapiens
JNJ 10329670 competitive, reversible inhibition, 4-(2-keto-1-benzimidazolinyl)-piperidin-1-yl derivative, IC50: 100 nM Homo sapiens
additional information inhibitory potential in vivo on Ii degradation in JY cells Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
Ii protein + H2O Homo sapiens degradation Ii fragments
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
JY cell
-
Homo sapiens
-
T-cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Ii protein + H2O
-
Homo sapiens Ii fragments
-
?
Ii protein + H2O degradation Homo sapiens Ii fragments
-
?

Synonyms

Synonyms Comment Organism
CatS
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00001
-
IC50: 10 nM Homo sapiens 1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
0.00002
-
IC50: 20 nM Homo sapiens 2-[5-carbamoyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-1-[[4-(2-cyanophenyl)piperazin-1-yl]methyl]ethyl carbamate
0.00003
-
IC50: 30 nM Homo sapiens 3-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,5-dimethyl-1,3-dihydro-2H-benzimidazol-2-one
0.00003
-
IC50: 30 nM Homo sapiens 6-chloro-1-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
0.00005
-
IC50: 50 nM Homo sapiens 1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
0.00005
-
IC50: 50 nM Homo sapiens 1-[3-[4-(2-cyanophenyl)piperazin-1-yl]-2-hydroxypropyl]-3-(4-iodophenyl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide
0.00005
-
IC50: 50 nM Homo sapiens 6-chloro-1-(1-[3-[3-(4-chloro-3-methylphenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
0.00005
-
IC50: 50 nM Homo sapiens 1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
0.00005
-
IC50: 50 nM Homo sapiens 1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
0.00005
-
IC50: 50 nM Homo sapiens 1-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
0.00005
-
IC50: 50 nM Homo sapiens 1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
0.00006
-
IC50: 60 nM Homo sapiens 1-(1-[3-[3-(4-chloro-3-methylphenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
0.00006
-
IC50: 60 nM Homo sapiens 6-chloro-1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
0.00008
-
IC50: 80 nM Homo sapiens 1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
0.00008
-
IC50: 80 nM Homo sapiens 5-chloro-3-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
0.00009
-
IC50: 90 nM Homo sapiens 1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-(2,2,2-trifluoroethyl)-1,3-dihydro-2H-benzimidazol-2-one
0.00009
-
IC50: 90 nM Homo sapiens 1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methyl-1,3-dihydro-2H-benzimidazol-2-one
0.0001
-
IC50: 100 nM Homo sapiens 1-[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]-1,3-dihydro-2H-benzimidazol-2-one
0.0001
-
IC50: 100 nM Homo sapiens 1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-tert-butyl-1,3-dihydro-2H-benzimidazol-2-one
0.0001
-
IC50: 100 nM Homo sapiens 1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methyl-1,3-dihydro-2H-benzimidazol-2-one
0.0001
-
IC50: 100 nM Homo sapiens 1-(ethenylideneamino)-3-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
0.0001
-
competitive, reversible inhibition, 4-(2-keto-1-benzimidazolinyl)-piperidin-1-yl derivative, IC50: 100 nM Homo sapiens JNJ 10329670
0.00011
-
IC50: 110 nM Homo sapiens 1-[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]-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
0.00011
-
IC50: 110 nM Homo sapiens 1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5,6-dichloro-1,3-dihydro-2H-benzimidazol-2-one
0.00012
-
IC50: 120 nM Homo sapiens 2-(4-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperazin-1-yl)benzonitrile
0.00012
-
IC50: 120 nM Homo sapiens 1-(1-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
0.00012
-
IC50: 120 nM Homo sapiens 1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
0.00013
-
IC50: 130 nM Homo sapiens 1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
0.00013
-
IC50: 130 nM Homo sapiens 1-[1-(3-[5-acetyl-3-[4-(trifluoromethoxy)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
0.00014
-
IC50: 140 nM Homo sapiens 1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-butyl-1,3-dihydro-2H-benzimidazol-2-one
0.00014
-
IC50: 140 nM Homo sapiens 1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methoxy-1,3-dihydro-2H-benzimidazol-2-one
0.00014
-
IC50: 140 nM Homo sapiens 1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
0.00015
-
IC50: 150 nM Homo sapiens 5-chloro-3-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
0.00018
-
IC50: 180 nM Homo sapiens 1-[1-[(2R)-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]-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
0.00019
-
IC50: 190 nM Homo sapiens 1-(1-[(2S)-3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
0.0002
-
IC50: 200 nM Homo sapiens 1-[1-[(2S)-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]-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
0.00021
-
IC50: 210 nM Homo sapiens 1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-7-methyl-1,3-dihydro-2H-benzimidazol-2-one
0.00023
-
IC50: 230 nM Homo sapiens 1-(1-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-fluoro-1,3-dihydro-2H-benzimidazol-2-one
0.00031
-
IC50: 310 nM Homo sapiens 1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one
0.00035
-
IC50: 350 nM Homo sapiens 1-(1-[(2R)-3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
0.00046
-
IC50: 460 nM Homo sapiens 1-(1-[3-[5-acetyl-3-(4-chlorophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
0.0005
-
IC50: 500 nM Homo sapiens 1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one