Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T25258 | ||||
Target Name | Multidrug resistance protein 1 (ABCB1) | ||||
Type of Target |
Clinical trial |
||||
Drug Potency against Target | 4,3'',5''-trimethoxy-[1,1':2',1'']-terphenyl | Drug Info | IC50 = 16000 nM | [1] | |
6-(3,5-dimethoxy-phenyl)-naphthalen-2-ol | Drug Info | IC50 = 16000 nM | [1] | ||
Elacridar | Drug Info | IC50 = 2000 nM | [3] | ||
TRISMETHOXYRESVERATROL | Drug Info | IC50 = 8000 nM | [1] | ||
XR-9456 | Drug Info | IC50 = 300 nM | [2] | ||
XR-9504 | Drug Info | IC50 = 260 nM | [2] | ||
XR-9544 | Drug Info | IC50 = 50 nM | [2] | ||
XR-9577 | Drug Info | IC50 = 320 nM | [2] | ||
[1,1':2',1'']-terphenyl-4,3'',5''-triol | Drug Info | IC50 = 12000 nM | [1] | ||
References | |||||
REF 1 | Identification of a terphenyl derivative that blocks the cell cycle in the G0-G1 phase and induces differentiation in leukemia cells. J Med Chem. 2006 May 18;49(10):3012-8. | ||||
REF 2 | Functional assay and structure-activity relationships of new third-generation P-glycoprotein inhibitors. Bioorg Med Chem. 2008 Mar 1;16(5):2448-62. | ||||
REF 3 | 2-[(3-Methoxyphenylethyl)phenoxy]-based ABCB1 inhibitors: effect of different basic side-chains on their biological properties. J Med Chem. 2008 Dec 11;51(23):7602-13. | ||||
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