Target Validation Information
TTD ID T70309
Target Name Steroid 5-alpha-reductase 1 (SRD5A1)
Type of Target
Clinical trial
Drug Potency against Target (3-methyl-4-(4-phenoxybenzoyl)phenyl)acetic acid Drug Info IC50 = 1450 nM [5]
1,2,5,6-tetrahydro pyrido[1,2-a]quinolin-3-one Drug Info IC50 = 298 nM [4]
1-Methyl-5-(4-phenylazo-phenyl)-piperidin-2-one Drug Info IC50 = 302 nM [3]
1-Methyl-5-phenyl-piperidin-2-one Drug Info IC50 = 2477 nM [3]
2,3,5,6-Tetrafluoro-4-pentafluorophenylazo-phenol Drug Info IC50 = 2000 nM [6]
3,4,5,6-Tetrahydrobenzo[c]quinolizin-3-(4aH)-one Drug Info IC50 = 5130 nM [4]
4,4'-dihydroxyoctafluoroazobenzene Drug Info IC50 = 790 nM [6]
4-Methyl-5,6-dihydro-pyrido[1,2-a]quinolin-3-one Drug Info IC50 = 1400 nM [4]
5-(4-Chloro-phenyl)-1-methyl-piperidin-2-one Drug Info IC50 = 1690 nM [3]
5-(4-Chloro-phenyl)-1-methyl-piperidine-2-thione Drug Info IC50 = 3360 nM [3]
Bexlosteride Drug Info IC50 = 8 nM [2]
FK-143 Drug Info IC50 = 4.2 nM [1]
LY-266111 Drug Info IC50 = 17 nM [3]
MK-386 Drug Info IC50 = 0.5 nM [2]
ONO-3805 Drug Info IC50 = 2.6 nM [1]
References
REF 1 Dual-acting agents with alpha1-adrenoceptor antagonistic and steroid 5alpha-reductase inhibitory activities. Synthesis and evaluation of arylpipera... Bioorg Med Chem Lett. 1999 Jun 7;9(11):1553-8.
REF 2 Synthesis of 8-chloro-benzo[c]quinolizin-3-ones as potent and selective inhibitors of human steroid 5alpha-reductase 1. Bioorg Med Chem Lett. 2000 Feb 21;10(4):353-6.
REF 3 Simple bi- and tricyclic inhibitors of human steroid 5alpha-reductase. Bioorg Med Chem Lett. 2000 Sep 4;10(17):1909-11.
REF 4 Benzo[c]quinolizin-3-ones: a novel class of potent and selective nonsteroidal inhibitors of human steroid 5alpha-reductase 1. J Med Chem. 2000 Oct 5;43(20):3718-35.
REF 5 Novel 5alpha-reductase inhibitors: synthesis, structure-activity studies, and pharmacokinetic profile of phenoxybenzoylphenyl acetic acids. J Med Chem. 2006 Jan 26;49(2):748-59.
REF 6 Hydroxyperfluoroazobenzenes: novel inhibitors of enzymes of androgen biosynthesis. J Med Chem. 1990 Sep;33(9):2452-5.

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