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Literature summary for 1.14.15.4 extracted from

  • Adams, C.M.; Hu, C.W.; Jeng, A.Y.; Karki, R.; Ksander, G.; Lasala, D.; Leung-Chu, J.; Liang, G.; Liu, Q.; Meredith, E.; Rao, C.; Rigel, D.F.; Shi, J.; Smith, S.; Springer, C.; Zhang, C.
    The discovery of potent inhibitors of aldosterone synthase that exhibit selectivity over 11-beta-hydroxylase (2010), Bioorg. Med. Chem. Lett., 20, 4324-4327.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(1R)-2-[2-[(1S)-1-(4-chlorophenyl)ethyl]-3,3-dioxido-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazin-4-yl]-1-phenylethanol
-
Homo sapiens
(1S)-2-[2-[(1S)-1-(4-chlorophenyl)ethyl]-3,3-dioxido-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazin-4-yl]-1-phenylethanol
-
Homo sapiens
2-(4-chlorobenzyl)-4-(2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
Homo sapiens
2-(4-fluorobenzyl)-4-(2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
Homo sapiens
2-benzyl-4-(2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
Homo sapiens
2-[(1R)-1-(4-chlorophenyl)ethyl]-4-(2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
Homo sapiens
2-[(1S)-1-(4-chlorophenyl)ethyl]-4-(2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
Homo sapiens
2-[(1S)-1-(4-chlorophenyl)ethyl]-4-(3-methoxy-2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
Homo sapiens
2-[(1S)-1-(4-chlorophenyl)ethyl]-4-(cyclopropylmethyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
Homo sapiens
2-[(1S)-1-(4-chlorophenyl)ethyl]-4-[(3-methyloxetan-3-yl)methyl]-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
Homo sapiens
2-[(1S)-1-(4-chlorophenyl)ethyl]-4-[(propan-2-yloxy)methyl]-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
Homo sapiens
3-[2-[(1S)-1-(4-chlorophenyl)ethyl]-3,3-dioxido-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazin-4-yl]-2-methylpropan-1-ol
-
Homo sapiens
4-(2-methylpropyl)-2-(thiophen-2-ylmethyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
Homo sapiens
4-(2-methylpropyl)-2-[4-(trifluoromethoxy)benzyl]-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
Homo sapiens
4-(2-methylpropyl)-2-[4-(trifluoromethyl)benzyl]-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
Homo sapiens
4-(7-benzyl-6-oxo-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazin-5-yl)benzonitrile
-
Homo sapiens
FAD286 inhibitor of 11-beta-hydroxylase CYP11B1 Homo sapiens
fadrozole inhibitor of CYP11B2 Homo sapiens
additional information a sulfonamide-imidazole scaffold is a potent inhibitor of CYP11B2, the scaffold can achieve high levels of selectivity for CYP11B2 over CYP11B1, overview. Evaluation of a lactam series of derivatives of the R-enantiomer of fadrozole, FAD286, homology modelling, overview Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
zona glomerulosa cells of the adrenal gland express CYP11B2 Homo sapiens
-

Synonyms

Synonyms Comment Organism
11-beta-hydroxylase
-
Homo sapiens
Aldosterone synthase
-
Homo sapiens
CYP11B1
-
Homo sapiens
CYP11B2
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000003
-
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication Homo sapiens (1S)-2-[2-[(1S)-1-(4-chlorophenyl)ethyl]-3,3-dioxido-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazin-4-yl]-1-phenylethanol
0.0000007
-
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[(1S)-1-(4-chlorophenyl)ethyl]-4-(3-methoxy-2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
0.0000008
-
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[(1S)-1-(4-chlorophenyl)ethyl]-4-[(propan-2-yloxy)methyl]-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
0.0000013
-
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[(1S)-1-(4-chlorophenyl)ethyl]-4-(cyclopropylmethyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
0.0000024
-
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication Homo sapiens (1R)-2-[2-[(1S)-1-(4-chlorophenyl)ethyl]-3,3-dioxido-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazin-4-yl]-1-phenylethanol
0.0000052
-
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-(4-chlorobenzyl)-4-(2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
0.0000078
-
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[(1S)-1-(4-chlorophenyl)ethyl]-4-[(3-methyloxetan-3-yl)methyl]-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
0.0000094
-
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[(1R)-1-(4-chlorophenyl)ethyl]-4-(2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
0.0000114
-
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication Homo sapiens 3-[2-[(1S)-1-(4-chlorophenyl)ethyl]-3,3-dioxido-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazin-4-yl]-2-methylpropan-1-ol
0.0000186
-
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-benzyl-4-(2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
0.0000617
-
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[(1S)-1-(4-chlorophenyl)ethyl]-4-(2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
0.000104
-
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication Homo sapiens 4-(2-methylpropyl)-2-[4-(trifluoromethoxy)benzyl]-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
0.000117
-
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication Homo sapiens 4-(2-methylpropyl)-2-(thiophen-2-ylmethyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
0.000121
-
inhibition of CYP11B2, pH not specified in the publication, temperature not specified in the publication Homo sapiens 4-(2-methylpropyl)-2-[4-(trifluoromethyl)benzyl]-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide

General Information

General Information Comment Organism
metabolism CYP11B1 is a key enzyme in the biosynthesis of cortisol. CYP11B2 catalyzes the last three steps of aldosterone biosynthesis Homo sapiens