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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