Application | Comment | Organism |
---|---|---|
medicine | treatment of hyperaldosteronism, congestive heart failure, and myocardial fibrosis by lowering the elevated plasma aldosterone levels via blockade of aldosterone synthase, CYP11B2, the key enzyme of mineralocorticoid biosynthesis | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
expression of CYP11B1 and CYP11B2 in V79 cells | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
6,6-dimethyl-8-(pyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-(1H-imidazol-1-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-(2,3'-bipyridin-5-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-(5-ethoxypyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-(5-fluoropyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-(5-hydroxypyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-(5-methoxypyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-(5-phenylpyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]-quinolin-4-one | - |
Homo sapiens | |
8-(isoquinolin-4-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-(pyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-(pyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinoline-4-thione | - |
Homo sapiens | |
8-(pyrimidin-5-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-[5-(2,5-difluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-[5-(2-fluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-[5-(2-methoxyphenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-[5-(3,4-difluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-[5-(3,5-difluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-[5-(3-fluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-[5-(3-hydroxyphenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-[5-(3-methoxyphenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-[5-(4-fluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-[5-(4-methoxyphenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-[5-(propan-2-yloxy)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-[5-(trifluoromethyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-[5-[3-(trifluoromethoxy)phenyl]pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
8-[5-[3-(trifluoromethyl)phenyl]pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | - |
Homo sapiens | |
9-(5-methoxypyridin-3-yl)-2,3,6,7-tetrahydro-1H,5H-pyrido[3,2,1-ij]quinolin-5-one | - |
Homo sapiens | |
9-(pyridin-3-yl)-1,2,6,7-tetrahydro-5H-pyrido[ 3,2,1-ij]quinolin-3-one | - |
Homo sapiens | |
9-[6-(isoquinolin-4-yl)pyridin-3-yl]-2,3,6,7-tetrahydro-1H,5H-pyrido[3,2,1-ij]quinolin-5-one | - |
Homo sapiens | |
additional information | development of 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-ones and structurally related aldosterone synthase inhibitors, molecular modelling, overview. No inhibition of both isozymes by 32 and 15 | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
mitochondrion | CYP11B2 | Homo sapiens | 5739 | - |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
adrenal gland | CYP11B2 | Homo sapiens | - |
zona glomerulosa | CYP11B2 | Homo sapiens | - |
Synonyms | Comment | Organism |
---|---|---|
11beta-hydroxylase | - |
Homo sapiens |
Aldosterone synthase | - |
Homo sapiens |
CYP11B1 | - |
Homo sapiens |
CYP11B2 | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000002 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-(isoquinolin-4-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.0000002 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 9-[6-(isoquinolin-4-yl)pyridin-3-yl]-2,3,6,7-tetrahydro-1H,5H-pyrido[3,2,1-ij]quinolin-5-one | |
0.0000006 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-(5-methoxypyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.0000007 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(2-fluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.0000009 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 9-(5-methoxypyridin-3-yl)-2,3,6,7-tetrahydro-1H,5H-pyrido[3,2,1-ij]quinolin-5-one | |
0.0000009 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(4-fluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.000001 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-(5-ethoxypyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.0000011 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-(pyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.0000012 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(3-hydroxyphenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.0000012 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-(pyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinoline-4-thione | |
0.0000013 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-(5-phenylpyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]-quinolin-4-one | |
0.0000014 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(3-fluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.0000014 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(4-methoxyphenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.0000022 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(propan-2-yloxy)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.0000023 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(3,4-difluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.0000024 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 9-(pyridin-3-yl)-1,2,6,7-tetrahydro-5H-pyrido[ 3,2,1-ij]quinolin-3-one | |
0.0000024 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(2-methoxyphenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.0000036 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(2,5-difluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.0000043 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-(5-hydroxypyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.0000044 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-(5-fluoropyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.0000046 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(3-methoxyphenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.0000059 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(trifluoromethyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.000013 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-(isoquinolin-4-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.000016 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-[3-(trifluoromethoxy)phenyl]pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.000018 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(3,5-difluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.000021 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(4-methoxyphenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.000033 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-[3-(trifluoromethyl)phenyl]pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.000034 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 9-[6-(isoquinolin-4-yl)pyridin-3-yl]-2,3,6,7-tetrahydro-1H,5H-pyrido[3,2,1-ij]quinolin-5-one | |
0.00004 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(4-fluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.000043 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(2-fluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.000044 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(3-hydroxyphenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.000056 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-(pyrimidin-5-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.000058 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-(5-phenylpyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]-quinolin-4-one | |
0.000089 | - |
inhibition of CYP11B1, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-(1H-imidazol-1-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.000103 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(propan-2-yloxy)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.000128 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(2-methoxyphenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.000141 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(trifluoromethyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.000158 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-(5-ethoxypyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.000183 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(2,5-difluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.000247 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-(5-methoxypyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.000333 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-(pyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinoline-4-thione | |
0.00049 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(3-fluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.000496 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(3,4-difluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.000545 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 9-(5-methoxypyridin-3-yl)-2,3,6,7-tetrahydro-1H,5H-pyrido[3,2,1-ij]quinolin-5-one | |
0.000715 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-(pyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.001288 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-(5-fluoropyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.001374 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(3-methoxyphenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.001748 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-(3,5-difluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.002045 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-(5-hydroxypyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.002058 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-[3-(trifluoromethoxy)phenyl]pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.002077 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-(1H-imidazol-1-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.002296 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 9-(pyridin-3-yl)-1,2,6,7-tetrahydro-5H-pyrido[ 3,2,1-ij]quinolin-3-one | |
0.004646 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-[5-[3-(trifluoromethyl)phenyl]pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one | |
0.02855 | - |
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 8-(pyrimidin-5-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one |
General Information | Comment | Organism |
---|---|---|
metabolism | aldosterone synthase, CYP11B2, is the key enzyme of mineralocorticoid biosynthesis and its malfunction is involved in hyperaldosteronism, congestive heart failure, and myocardial fibrosis | Homo sapiens |