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Ondansetron

Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

In Vitro Substrates

No substrate information.

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	Ondansetron	63		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT1	Tzvetkov, 2012
SLC47A1	MATE1	Ondansetron	0.15		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-MATE1	Kido, 2011
SLC47A2	MATE2K	Ondansetron	6.9		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-MATE2K	Kido, 2011
SLC22A1	OCT1	Ondansetron	>300		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT1	Wittwer, 2013
SLC22A3	OCT3	Ondansetron	17.4		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT3	Wittwer, 2013
SLC22A2	OCT2	Ondansetron	1.7		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT2	Wittwer, 2013
SLC47A1	MATE1	Ondansetron	0.16		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-MATE1	Wittwer, 2013
SLC47A2	MATE2K	Ondansetron	0.16		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-MATE2K	Wittwer, 2013
SLC47A2	MATE2K	Ondansetron	0.3		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-MATE2K	Wittwer, 2013
ABCC2	MRP2, cMOAT	Ondansetron	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Ondansetron	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Ondansetron	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLC47A1	MATE1	Ondansetron	0.01		Metformin	MDCK2- MATE1	Wittwer, 2013
SLC47A1	MATE1	Ondansetron	0.03		Metformin	HEK293-MATE1	Wittwer, 2013
SLC22A2	OCT2	Ondansetron		85	Metformin	HEK293-OCT2	Li, 2013
SLC22A1	OCT1	Ondansetron	1.2		Morphine	HEK293-OCT1	Tzvetkov, 2013
SLC22A1	OCT1	Ondansetron	0.3		Morphine	HEK293-OCT1	Zhu, 2018
ABCB11	BSEP	Ondansetron	>133		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013

Clinical Drug-Drug Interactions

No drug-drug interaction information.