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Chloroquine

In Vitro Substrates

No substrate information.

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter

Transporter	Synonyms	Inhibitor	IC50 (μM)	Substrate used	Cell System	Reference
SLC22A2	OCT2	Chloroquine	129	1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Belzer, 2013
SLC22A1	OCT1	Chloroquine	12.8	1-methyl-4-phenylpyridinium (MPP+)	HEK293-OCT1	Hubeny, 2016
ABCC4	MRP4	Chloroquine	103.9	Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC2	MRP2, cMOAT	Chloroquine	>133	Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Chloroquine	>133	Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLC47A1	MATE1	Chloroquine	1.5	Ipratropium	HEK293-MATE1	Chen, 2017
SLC47A2	MATE2K	Chloroquine	4	Ipratropium	HEK293-MATE2K	Chen, 2017
SLC47A1	MATE1	Chloroquine	2.5	Metformin	HEK293-MATE1	Muller, 2011
SLC22A2	OCT2	Chloroquine	9.6	Metformin	CHO-OCT2	Belzer, 2013
SLC22A1	OCT1	Chloroquine	10.7	Metformin	HEK293-OCT1	Yee, 2021
SLC22A2	OCT2	Chloroquine	1096	N-methylpyridinium	HEK293-OCT2	Zolk, 2009
SLC22A2	OCT2	Chloroquine	117	NBD-MTMA	CHO-OCT2	Belzer, 2013
ABCB11	BSEP	Chloroquine	>133	Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013

No drug-drug interaction information.