Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T92521 | ||||
Target Name | Cytochrome P450 1B1 (CYP1B1) | ||||
Type of Target |
Clinical trial |
||||
Drug Potency against Target | 2-[2-(3,5-Dimethoxy-phenyl)-vinyl]-thiophene | Drug Info | IC50 = 2 nM | [1] | |
3-[2-(3,5-Dimethoxy-phenyl)-vinyl]-furan | Drug Info | IC50 = 2100 nM | [1] | ||
4-[2-(3,5-Dimethoxy-phenyl)-vinyl]-pyridine | Drug Info | IC50 = 460 nM | [1] | ||
ACACETIN | Drug Info | IC50 = 12 nM | [2] | ||
APIGENIN | Drug Info | IC50 = 25 nM | [2] | ||
Chrysin | Drug Info | IC50 = 24 nM | [2] | ||
CHRYSOERIOL | Drug Info | IC50 = 20 nM | [2] | ||
DIOSMETIN | Drug Info | IC50 = 29 nM | [2] | ||
ERIODICTYOL | Drug Info | IC50 = 1284 nM | [2] | ||
Galangin | Drug Info | IC50 = 25 nM | [2] | ||
HOMOERIODICTYOL | Drug Info | IC50 = 1716 nM | [2] | ||
ISORHAMNETIN | Drug Info | IC50 = 17 nM | [2] | ||
ISOSAKUTANETIN | Drug Info | IC50 = 1024 nM | [2] | ||
KAEMPFERIDE | Drug Info | IC50 = 25 nM | [2] | ||
KAEMPFEROL | Drug Info | IC50 = 47 nM | [2] | ||
N-(2,4-Dimethoxy-phenyl)-3,5-dimethoxy-benzamide | Drug Info | IC50 = 670 nM | [1] | ||
NARINGENIN | Drug Info | IC50 = 3656 nM | [2] | ||
PINOCEMBRIN | Drug Info | IC50 = 1679 nM | [2] | ||
TAMARIXETIN | Drug Info | IC50 = 20 nM | [2] | ||
TRISMETHOXYRESVERATROL | Drug Info | IC50 = 790 nM | [1] | ||
References | |||||
REF 1 | Design, synthesis, and discovery of novel trans-stilbene analogues as potent and selective human cytochrome P450 1B1 inhibitors. J Med Chem. 2002 Jan 3;45(1):160-4. | ||||
REF 2 | Selective inhibition of methoxyflavonoids on human CYP1B1 activity. Bioorg Med Chem. 2010 Sep 1;18(17):6310-5. | ||||
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