Cloned (Comment) | Organism |
---|---|
stable expression of human CYP11B2 or CYP11B1 enzymes in V79 Chinese hamster cells | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2,3-dichloro-N-(pyridin-3-yl)benzamide | 51% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B22 | Homo sapiens | |
2,4,5-trifluoro-N-(pyridin-3-yl)benzamide | 70% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B23 | Homo sapiens | |
2-fluoro-N-(pyridin-3-yl)benzamide | 34% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B19 | Homo sapiens | |
3,4-difluoro-N-(pyridin-3-yl)benzamide | 83% inhibition of CYP11B2 at 0.5 mM, 6% inhibition of CYP11B20 | Homo sapiens | |
3,4-dimethoxy-N-(pyridin-3-yl)benzamide | - |
Homo sapiens | |
3-chloro-N-(pyridin-3-yl)benzamide | 26% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B18 | Homo sapiens | |
3-fluoro-N-(pyridin-3-yl)benzamide | 47% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B17 | Homo sapiens | |
4-bromo-N-(pyridin-3-yl)benzamide | 64% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B9 | Homo sapiens | |
4-chloro-N-(pyridin-3-yl)benzamide | 88% inhibition of CYP11B2 at 0.5 mM, 5% inhibition of CYP11B8 | Homo sapiens | |
4-cyano-N-(pyridin-3-yl)benzamide | 81% inhibition of CYP11B2 at 0.5 mM, 9% inhibition of CYP11B15 | Homo sapiens | |
4-fluoro-N-(pyridin-3-yl)benzamide | 86% inhibition of CYP11B2 at 0.5 mM, 7% inhibition of CYP11B7 | Homo sapiens | |
4-methoxy-N-(pyridin-3-yl)benzamide | 19% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B10 | Homo sapiens | |
4-methyl-N-(pyridin-3-yl)benzamide | 25% inhibition of CYP11B2 at 0.5 mM, no% inhibition of CYP11B13 | Homo sapiens | |
4-nitro-N-(pyridin-3-yl)benzamide | 64% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B16 | Homo sapiens | |
5-bromo-N-(pyridin-3-yl)pyridine-3-carboxamide | 29% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B5 | Homo sapiens | |
6-(5,8-dihydroisoquinolin-4-yl)-3,4-dihydroquinolin-2(1H)-one | 94% inhibition of CYP11B2 at 0.5 mM, 91% inhibition of CYP11B1 | Homo sapiens | |
Metyrapone | 79% inhibition of CYP11B2 at 0.5 mM, 94% inhibition of CYP11B2 | Homo sapiens | |
additional information | synthesis of 23 N-(pyridin-3-yl)benzamides and evaluation for their potential to inhibit steroid-11beta-hydroxylase CYP11B1 and aldosterone synthase CYP11B2, overview. N-(Pyridin-3-yl)benzamides are a highly selective class of CYP11B2 inhibitors in vitro. No or poor inhibition of both isozymes by 3i, 3j, 3l, and 3s | Homo sapiens | |
N-(pyridin-3-yl)-4-(trifluoromethoxy)benzamide | - |
Homo sapiens | |
N-(pyridin-3-yl)-4-(trifluoromethyl)benzamide | - |
Homo sapiens | |
N-(pyridin-3-yl)benzamide | 30% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B6 | Homo sapiens | |
N-(pyridin-3-yl)biphenyl-4-carboxamide | - |
Homo sapiens | |
N-(pyridin-3-yl)pyridine-3-carboxamide | 8% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B3 | Homo sapiens | |
N-(pyridin-3-yl)pyridine-4-carboxamide | 39% inhibition of CYP11B2 at 0.5 mM, 4% inhibition of CYP11B4 | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Synonyms | Comment | Organism |
---|---|---|
Aldosterone synthase | - |
Homo sapiens |
CYP11B1 | - |
Homo sapiens |
CYP11B2 | - |
Homo sapiens |
steroid-11beta-hydroxylase | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000002 | - |
inhibition of CYP11B2, substrate 11-deoxycorticosterone, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 6-(5,8-dihydroisoquinolin-4-yl)-3,4-dihydroquinolin-2(1H)-one | |
0.0000059 | - |
inhibition of CYP11B1, substrate 11-deoxycorticosterone, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 3,4-difluoro-N-(pyridin-3-yl)benzamide | |
0.0000075 | - |
inhibition of CYP11B1, substrate 11-deoxycorticosterone, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 4-cyano-N-(pyridin-3-yl)benzamide | |
0.0000102 | - |
inhibition of CYP11B1, substrate 11-deoxycorticosterone, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 4-chloro-N-(pyridin-3-yl)benzamide | |
0.0000143 | - |
inhibition of CYP11B1, substrate 11-deoxycorticosterone, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 4-fluoro-N-(pyridin-3-yl)benzamide | |
0.0000146 | - |
inhibition of CYP11B1, substrate 11-deoxycorticosterone, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | Metyrapone | |
0.0000161 | - |
inhibition of CYP11B1, substrate 11-deoxycorticosterone, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 2,4,5-trifluoro-N-(pyridin-3-yl)benzamide | |
0.0000248 | - |
inhibition of CYP11B1, substrate 11-deoxycorticosterone, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 4-nitro-N-(pyridin-3-yl)benzamide | |
0.000033 | - |
inhibition of CYP11B1, substrate 11-deoxycorticosterone, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 6-(5,8-dihydroisoquinolin-4-yl)-3,4-dihydroquinolin-2(1H)-one | |
0.0000535 | - |
inhibition of CYP11B2, substrate 11-deoxycorticosterone, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 3,4-difluoro-N-(pyridin-3-yl)benzamide | |
0.000065 | - |
inhibition of CYP11B2, substrate 11-deoxycorticosterone, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 4-chloro-N-(pyridin-3-yl)benzamide | |
0.000072 | - |
inhibition of CYP11B2, substrate 11-deoxycorticosterone, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | Metyrapone | |
0.000078 | - |
inhibition of CYP11B2, substrate 11-deoxycorticosterone, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 4-cyano-N-(pyridin-3-yl)benzamide | |
0.000082 | - |
inhibition of CYP11B2, substrate 11-deoxycorticosterone, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 4-fluoro-N-(pyridin-3-yl)benzamide | |
0.000104 | - |
inhibition of CYP11B2, substrate 11-deoxycorticosterone, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 4-bromo-N-(pyridin-3-yl)benzamide | |
0.000145 | - |
inhibition of CYP11B2, substrate 11-deoxycorticosterone, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 4-nitro-N-(pyridin-3-yl)benzamide | |
0.000166 | - |
inhibition of CYP11B2, substrate 11-deoxycorticosterone, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 2,4,5-trifluoro-N-(pyridin-3-yl)benzamide | |
0.000167 | - |
inhibition of CYP11B1, substrate 11-deoxycorticosterone, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 4-bromo-N-(pyridin-3-yl)benzamide |