| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T70309 | ||||
| Target Name | 3-oxo-5-alpha-steroid 4-dehydrogenase 1 | ||||
| Target Type | Clinical Trial |
||||
| Drug Potency against Target | 4-Methyl-5,6-dihydro-pyrido[1,2-a]quinolin-3-one | Drug Info | IC50 = 1400 nM | [1] | |
| 3,4,5,6-Tetrahydrobenzo[c]quinolizin-3-(4aH)-one | Drug Info | IC50 = 5130 nM | [1] | ||
| 1,2,5,6-tetrahydro pyrido[1,2-a]quinolin-3-one | Drug Info | IC50 = 298 nM | [1] | ||
| 4,4'-dihydroxyoctafluoroazobenzene | Drug Info | IC50 = 790 nM | [2] | ||
| ONO-3805 | Drug Info | IC50 = 2.6 nM | [3] | ||
| FK-143 | Drug Info | IC50 = 4.2 nM | [3] | ||
| 5-(4-Chloro-phenyl)-1-methyl-piperidine-2-thione | Drug Info | IC50 = 3360 nM | [4] | ||
| LY-266111 | Drug Info | IC50 = 17 nM | [4] | ||
| 2,3,5,6-Tetrafluoro-4-pentafluorophenylazo-phenol | Drug Info | IC50 = 2000 nM | [2] | ||
| 5-(4-Chloro-phenyl)-1-methyl-piperidin-2-one | Drug Info | IC50 = 1690 nM | [4] | ||
| (3-methyl-4-(4-phenoxybenzoyl)phenyl)acetic acid | Drug Info | IC50 = 1450 nM | [5] | ||
| Bexlosteride | Drug Info | IC50 = 8 nM | [6] | ||
| 1-Methyl-5-(4-phenylazo-phenyl)-piperidin-2-one | Drug Info | IC50 = 302 nM | [4] | ||
| MK-386 | Drug Info | IC50 = 0.5 nM | [6] | ||
| 1-Methyl-5-phenyl-piperidin-2-one | Drug Info | IC50 = 2477 nM | [4] | ||
| References | |||||
| REF 1 | J Med Chem. 2000 Oct 5;43(20):3718-35.Benzo[c]quinolizin-3-ones: a novel class of potent and selective nonsteroidal inhibitors of human steroid 5alpha-reductase 1. | ||||
| REF 2 | J Med Chem. 1990 Sep;33(9):2452-5.Hydroxyperfluoroazobenzenes: novel inhibitors of enzymes of androgen biosynthesis. | ||||
| REF 3 | Bioorg Med Chem Lett. 1999 Jun 7;9(11):1553-8.Dual-acting agents with alpha1-adrenoceptor antagonistic and steroid 5alpha-reductase inhibitory activities. Synthesis and evaluation of arylpiperazine derivatives. | ||||
| REF 4 | Bioorg Med Chem Lett. 2000 Sep 4;10(17):1909-11.Simple bi- and tricyclic inhibitors of human steroid 5alpha-reductase. | ||||
| REF 5 | J Med Chem. 2006 Jan 26;49(2):748-59.Novel 5alpha-reductase inhibitors: synthesis, structure-activity studies, and pharmacokinetic profile of phenoxybenzoylphenyl acetic acids. | ||||
| REF 6 | Bioorg Med Chem Lett. 2000 Feb 21;10(4):353-6.Synthesis of 8-chloro-benzo[c]quinolizin-3-ones as potent and selective inhibitors of human steroid 5alpha-reductase 1. | ||||
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