Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T27265 | Target Info | |||
Target Name | Oxo-5-alpha-steroid 4-dehydrogenase (SRD5A) | ||||
Synonyms |
Steroid 5-alpha-reductase; SR; S5AR; 3-oxo-5-alpha-steroid 4-dehydrogenase
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Target Type | Successful Target | ||||
Gene Name | SRD5A1; SRD5A2; SRD5A3 | ||||
Biochemical Class | CH-CH donor oxidoreductase | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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Co-Target Name | Steroid 5-alpha-reductase 2 (SRD5A2) | Successful Target | ||||
UniProt ID | S5A2_HUMAN | |||||
Gene Name | SRD5A2 | |||||
Synonyms |
Type 2 steroid 5alpha-reductase (5alpha-R); SRD5A2; SR type 2; 5-alpha reductase 2; 5 alpha-SR2
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Representative Drug(s) | Dutasteride | Drug Info | IC50 < 0.1 nM | Click to Show More | [1] | |
2 | Finasteride | Drug Info | IC50 < 0.1 nM | [2] | ||
3 | Epristeride | Drug Info | IC50 = 0.18 nM | [3] | ||
4 | FK-143 | Drug Info | IC50 = 11 nM | [4] | ||
5 | Turosteride | Drug Info | IC50 = 55 nM | [5] | ||
Co-Target Name | Strychnine-binding glycine receptor (GLRA1) | Successful Target | ||||
UniProt ID | GLRA1_HUMAN | |||||
Gene Name | GLRA1 | |||||
Synonyms |
Strychnine-insensitive glycine receptor; Strychnine binding subunit; Glycine receptor 48 kDa subunit; GLRA1
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Representative Drug(s) | Dutasteride | Drug Info | EC50 = 330 nM | [6] | ||
Co-Target Name | Steroid 5-alpha-reductase 1 (SRD5A1) | Clinical trial Target | ||||
UniProt ID | S5A1_HUMAN | |||||
Gene Name | SRD5A1 | |||||
Synonyms |
SRD5A1; SR type 1; 5-alpha reductase 1
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Representative Drug(s) | FK-143 | Drug Info | IC50 = 3 nM | Click to Show More | [4] | |
2 | Dutasteride | Drug Info | IC50 = 4 nM | [1] | ||
3 | Finasteride | Drug Info | IC50 = 19.8 ug.mL-1 | [7] | ||
4 | Epristeride | Drug Info | Ki = 410 nM | [8] |
References | Top | ||||
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REF 1 | Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design. J Med Chem. 2018 Jul 26;61(14):5822-5880. | ||||
REF 2 | 4-Aza-3-oxo-5 alpha-androst-1-ene-17 beta-N-aryl-carboxamides as dual inhibitors of human type 1 and type 2 steroid 5 alpha-reductases. Dramatic effect of N-aryl substituents on type 1 and type 2 5 alpha-reductase inhibitory potency. J Med Chem. 1995 Aug 18;38(17):3189-92. | ||||
REF 3 | 6-Azasteroids: structure-activity relationships for inhibition of type 1 and 2 human 5 alpha-reductase and human adrenal 3 beta-hydroxy-delta 5-steroid dehydrogenase/3-keto-delta 5-steroid isomerase. J Med Chem. 1994 Jul 22;37(15):2352-60. | ||||
REF 4 | Synthesis and 5 alpha-reductase inhibitory activities of benzofuran derivatives with a carbamoyl group. Bioorg Med Chem Lett. 1998 Mar 17;8(6):561-6. | ||||
REF 5 | Pharmacological options in the treatment of benign prostatic hyperplasia. J Med Chem. 1997 Apr 25;40(9):1293-315. | ||||
REF 6 | Ensemble-based virtual screening for cannabinoid-like potentiators of the human glycine receptor alpha1 for the treatment of pain. J Med Chem. 2015 Apr 9;58(7):2958-66. | ||||
REF 7 | A novel class of inhibitors for steroid 5alpha-reductase: synthesis and evaluation of umbelliferone derivatives. Bioorg Med Chem Lett. 2001 Sep 3;11(17):2361-3. | ||||
REF 8 | A non-steroidal diene acid inhibitor of human type 2 stereoid 5alpha-reductase. Bioorg Med Chem Lett. 1994 Oct 6;4(19):2327-30. |
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