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Estrone sulfate

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
SLC22A11	OAT4	1.01	OAT4-expressing oocytes	Cha, 2000
ABCC1	MRP1	0.73	MRP1-expressing HeLa vesicles	Qian, 2001
ABCC1	MRP1	2.1	MRP1-expressing HeLa vesicles	Qian, 2001
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	12.5	HEK293-OATP1B1	Cui, 2001
SLCO2B1	OATP2B1, OATP-B	6.3	OATP2B1-expressing oocytes	Kullak-Ublick, 2001
SLC22A8	OAT3	7.5	S2-OAT3	Takeda, 2000
SLC22A8	OAT3	3.1	OAT3-expressing oocytes	Cha, 2001
SLC22A8	OAT3	2.21	S2-OAT3	Takeda, 2001
SLC22A11	OAT4	9.9	S2-OAT4	Takeda, 2002
ABCG2	BCRP, MXR	16.6	BCRP-expressing vesicles from mouse lymphoma (P388) cells	Suzuki, 2003
OSTalpha	OSTA	320	OSTalpha-OSTbeta expressing oocytes	Seward, 2003
OSTbeta	OSTB	320	OSTalpha-OSTbeta expressing oocytes	Seward, 2003
ABCC1	MRP1	4.2	MRP1-expressing HEK vesicles	Nunoya, 2003
ABCG2	BCRP, MXR	6.8	BCRP-expressing K562 vesicles	Imai, 2003
SLCO2B1	OATP2B1, OATP-B	8.09	HEK293-OATP2B1	Nozawa, 2004
SLC10A1	NTCP	27	HeLa-NTCP	Ho, 2004
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	0.46	HEK293-OATP1B1	Hirano, 2004
SLCO2B1	OATP2B1, OATP-B	7.14	HEK293-OATP2B1	Satoh, 2005
SLC22A8	OAT3	6.3	HEK293-OAT3	Ueo, 2005
SLC22A8	OAT3	6.3	HEK293 cells	Ueo, 2005
SLCO2B1	OATP2B1, OATP-B	20.9	HEK293-OATP2B1	Hirano, 2006
SLCO1A2	OATP1A2, OATP-A	13.6	HEK293-OATP1A2	Badagnani, 2006
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	0.23	CHO-OATP1B1	Noe, 2007
SLCO2B1	OATP2B1, OATP-B	10.2	HEK293-OATP2B1	Noe, 2007
SLC47A1	MATE1	470	HEK293-MATE1	Tanihara, 2007
SLC47A2	MATE2K	850	HEK293-MATE2K	Tanihara, 2007
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	2.4	CHO-OATP1B1	Gui, 2008
SLCO1B3	OATP1B3, OATP8	58	CHO-OATP1B3	Gui, 2008
SLC22A8	OAT3	2.18	COS7-OAT3	Duan, 2009
rat_Slco1a1	Oatp1, OATP-1, Slc21a1, Slc21a3	22.9	CHO cells	Yang, 2009
SLC22A11	OAT4	38.1	CHO cells	Yang, 2010
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	0.0872	HEK-OATP1B1	Chapy, 2015
SLC22A8	OAT3	21.2	HEK293 cells	Bruyere, 2017

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
SLC22A8	OAT3	Estrone sulfate	1		6-carboxyfluorescein	HEK293-OAT3	Zou, 2021
SLC22A6	OAT1	Estrone sulfate	170		6-carboxyfluorescein	HEK293-OAT1	Zou, 2021
SLCO1B3	OATP1B3, OATP8	Estrone sulfate	97.1		Cholecystokinin octapeptide	HEK293-OATP1B3	Ishiguro, 2006
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Estrone sulfate		0.0449	Dichlorofluorescein	HEK-OATP1B1	Izumi, 2016
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Estrone sulfate	0.79		Estradiol-17beta-glucuronide	HEK293-OATP1B1	Ishiguro, 2006
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Estrone sulfate		0.2	Estradiol-17beta-glucuronide	CHO-OATP1B1	Gui, 2009
OSTalpha	OSTA	Estrone sulfate	>200		Estrone sulfate	OSTalpha-OSTbeta expressing oocytes	Seward, 2003
OSTbeta	OSTB	Estrone sulfate	>200		Estrone sulfate	OSTalpha-OSTbeta expressing oocytes	Seward, 2003
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Estrone sulfate	0.06		Fluorescein-Methotrexate	CHO-OATP1B1	Gui, 2010
ABCC1	MRP1	Estrone sulfate		0.45	Leukotriene C4	MRP1-expressing HeLa vesicles	Qian, 2001

Clinical Drug-Drug Interactions

No drug-drug interaction information.