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Tamoxifen

Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

In Vitro Substrates

No substrate information.


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In Vitro Inhibitors

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter
Transporter Synonyms Inhibitor IC50 (μM) Ki (μM) Substrate used Cell System Reference
ABCB1 MDR1, P-gp Tamoxifen 6.4 Daunorubicin NIH-3T3-G185 cells Wang, 2001
ABCC2 MRP2, cMOAT Tamoxifen >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC3 MRP3 Tamoxifen >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC4 MRP4 Tamoxifen >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
SLC22A5 OCTN2 Tamoxifen 20 L-carnitine MDCKII-hOCTN2 Diao, 2009
ABCB1 MDR1, P-gp Tamoxifen 12.1 LDS-751 NIH-3T3-G185 cells Wang, 2001
SLC22A2 OCT2 Tamoxifen 87 N-methylpyridinium HEK293-OCT2 Zolk, 2009
ABCB1 MDR1, P-gp Tamoxifen 7.1 Rhodamine 123 MDR1 transfected NIH3T3-G185 Wang, 2001
ABCB1 MDR1, P-gp Tamoxifen 31.4 Rhodamine 123 NIH-3T3-G185 cells Wang, 2001
ABCB11 BSEP Tamoxifen >133 Taurocholate Sf9 cell membrane vesicles Morgan, 2013

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Clinical Drug-Drug Interactions

No drug-drug interaction information.


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