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Quinine

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
ABCB1 MDR1, P-gp 10 MDR1-containing proteoliposomes Borgnia, 1996

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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
SLC47A1 MATE1 Quinine 2 1-methyl-4-phenylpyridinium (MPP+) CHO-MATE1 Astorga, 2012
SLC47A2 MATE2K Quinine 6.4 1-methyl-4-phenylpyridinium (MPP+) CHO-MATE2K Astorga, 2012
SLC22A1 OCT1 Quinine 3.5 1-methyl-4-phenylpyridinium (MPP+) MDCK-OCT1 Hubeny, 2016
SLC22A1 OCT1 Quinine 51.6 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Ahlin, 2008
SLC22A2 OCT2 Quinine 3.4 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT2 van, 2017
ABCB1 MDR1, P-gp Quinine 280 Calcein AM Caco-2 cells Eneroth, 2001
ABCB1 MDR1, P-gp Quinine 167.8 Calcein AM NIH-3T3-G185 cells Wang, 2001
ABCB1 MDR1, P-gp Quinine 22.6 Daunorubicin NIH-3T3-G185 cells Wang, 2001
ABCB1 MDR1, P-gp Quinine 22.4 Digoxin MDCKII-MDR1 Keogh, 2006
ABCC2 MRP2, cMOAT Quinine >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC3 MRP3 Quinine >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC4 MRP4 Quinine >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
SLC22A1 OCT1 Quinine 70 Ethidium CHO-OCT1 Lee, 2009
ABCB1 MDR1, P-gp Quinine 112.4 Fluo-3 NIH-3T3-G185 cells Wang, 2001
ABCB1 MDR1, P-gp Quinine 159.3 JC-1 NIH-3T3-G185 cells Wang, 2001
ABCB1 MDR1, P-gp Quinine 74.4 LDS-751 NIH-3T3-G185 cells Wang, 2001
SLC22A1 OCT1 Quinine 13 N-methylpyridinium HEK293-OCT1 Muller, 2005
SLC22A2 OCT2 Quinine 23 N-methylpyridinium HEK293-OCT2 Muller, 2005
SLC22A3 OCT3 Quinine 37 N-methylpyridinium CHO-OCT3 Muller, 2005
ABCB1 MDR1, P-gp Quinine 87.6 Rhodamine 123 NIH-3T3-G185 cells Wang, 2001
ABCB11 BSEP Quinine >133 Taurocholate Sf9 cell membrane vesicles Morgan, 2013
SLC22A2 OCT2 Quinine 3.4 Tetraethylammonium OCT2-expressing oocytes Gorboulev, 1997
SLC22A1 OCT1 Quinine 22.9 Tetraethylammonium HeLa-OCT1 Zhang, 1998
SLC22A4 OCTN1 Quinine <1000 Tetraethylammonium HEK293-OCTN1 Yabuuchi, 1999
ABCB1 MDR1, P-gp Quinine 184.9 Tetramethylrosamine NIH-3T3-G185 cells Wang, 2001
ABCB1 MDR1, P-gp Quinine 430 Verapamil Caco-2 cells Doppenshmitt, 1998

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Clinical Drug-Drug Interactions

No drug-drug interaction information.


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