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Indomethacin

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
ABCC1	MRP1	Indomethacin	7		2',7'-bis-(3-carboxy-propyl)-5-(and-6)-carboxyfluorescein (BCPCF)	human erythrocytes	Lania-Pietrzak, 2005
SLC22A8	OAT3	Indomethacin	0.11		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
SLC22A6	OAT1	Indomethacin	4.35		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
SLC22A6	OAT1	Indomethacin	3		Adefovir	CHO-OAT1	Mulato, 2000
ABCC2	MRP2, cMOAT	Indomethacin	235		Calcein AM	MRP2-expressing MDCK-II cells	Leyers, 2008
SLCO2B1	OATP2B1, OATP-B	Indomethacin	16.3		Dibromofluorescein	HEK293-OATP2B1	Unger, 2020
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Indomethacin	12	11	Estradiol-17beta-glucuronide	HEK-OATP1B1	Karlgren, 2012
ABCC3	MRP3	Indomethacin	66		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Indomethacin	5.8		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A11	OAT4	Indomethacin	10.1		Estrone sulfate	S2-OAT4	Khamdang, 2002
SLC22A8	OAT3	Indomethacin	0.61		Estrone sulfate	S2-OAT3	Khamdang, 2002
OSTalpha	OSTA	Indomethacin	~200		Estrone sulfate	OSTalpha-OSTbeta expressing oocytes	Seward, 2003
OSTbeta	OSTB	Indomethacin	~200		Estrone sulfate	OSTalpha-OSTbeta expressing oocytes	Seward, 2003
ABCC2	MRP2, cMOAT	Indomethacin	0.06		Methotrexate	MRP2-expressing HEK293 vesicles	El-Sheikh, 2007
ABCC4	MRP4	Indomethacin	6.1		Methotrexate	MRP4-expressing HEK293 vesicles	El-Sheikh, 2007
ABCC6	MRP6	Indomethacin	ND		N-ethylmaleimide S-glutathione	MRP6-expressing Sf9 vesicles	Ilias, 2002
SLC22A6	OAT1	Indomethacin	3.83		Para-aminohippurate	S2-OAT1	Khamdang, 2002
SLC22A6	OAT1	Indomethacin	1.91		Para-Aminosalicylic acid (PAS)	HEK293-OAT1	Parvez, 2017
SLC22A8	OAT3	Indomethacin	2.18		Para-Aminosalicylic acid (PAS)	HEK293-OAT3	Parvez, 2017
SLC22A7	OAT2	Indomethacin	64.1		Prostaglandin F2-alpha	S2-OAT2	Khamdang, 2002
ABCB11	BSEP	Indomethacin	42		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013

Clinical Drug-Drug Interactions

No drug-drug interaction information.