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Imatinib

Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

In Vitro Substrates

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter
Transporter Synonyms Km (μM) Cell System Reference
ABCG2 BCRP, MXR ND Intracellular accumulation in BCRP-expressing HEK293 cells inhbited with Ko-143 Burger, 2004

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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
SLC22A1 OCT1 Imatinib 107 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Wittwer, 2013
SLC22A3 OCT3 Imatinib 25.5 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT3 Wittwer, 2013
SLC22A2 OCT2 Imatinib 4.2 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT2 Wittwer, 2013
SLC47A1 MATE1 Imatinib 0.35 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-MATE1 Wittwer, 2013
SLC47A2 MATE2K Imatinib 0.35 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-MATE2K Wittwer, 2013
SLC47A2 MATE2K Imatinib 2.9 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-MATE2K Wittwer, 2013
SLC22A1 OCT1 Imatinib 5 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Schmidt-Lauber, 2012
SLC22A4 OCTN1 Imatinib 31 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-hOCTN1 Schmidt-Lauber, 2012
SLC22A8 OAT3 Imatinib 14.5 6-carboxyfluorescein HEK293-OAT3 Zou, 2021
SLC22A6 OAT1 Imatinib 29.2 6-carboxyfluorescein HEK293-OAT1 Zou, 2021
ABCB1 MDR1, P-gp Imatinib 7.2 Calcein AM MDR1 expressing A2780/ADR cells Muller, 2007
SLC22A2 OCT2 Imatinib 6.7 Creatinine HEK293-OCT2 Tanihara, 2009
ABCC2 MRP2, cMOAT Imatinib >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC3 MRP3 Imatinib >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC4 MRP4 Imatinib >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCB1 MDR1, P-gp Imatinib 7.2 Hoechst 33342 MDR1 expressing A2780/ADR cells Pick, 2008
SLC22A1 OCT1 Imatinib 1.47 Metformin HEK293-OCT1 Minematsu, 2011
SLC47A1 MATE1 Imatinib 0.04 Metformin MDCK2- MATE1 Wittwer, 2013
SLC47A1 MATE1 Imatinib 0.05 Metformin HEK293-MATE1 Wittwer, 2013
SLC22A1 OCT1 Imatinib 10.2 Serotonin HEK293-OCT1 Boxberger, 2014
ABCB11 BSEP Imatinib 25.1 Taurocholate Sf9 cell membrane vesicles Morgan, 2013

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Clinical Drug-Drug Interactions

No drug-drug interaction information.


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