TABLE 1

Endogenous substrates of OATP1B1

Substrate	K_m	Expression System	Reference
	μM
Bile acids
Cholic acid	11	HEK293	Cui et al., 2001
Glycocholic acid	+	XO	Kullak-Ublick et al., 2001
Glycoursodeoxycholic acid	+	HEK293	Maeda et al., 2006b
Taurolithocholic acid 3-sulfate	+	MDCKII	Sasaki et al., 2002
Taurocholic acid	34	HEK293c18	Hsiang et al., 1999
	14	XO	Abe et al., 1999
	+	HEK293	König et al., 2000b
	10	HEK293	Cui et al., 2001
Tauroursodeoxycholic acid	+	HEK293	Maeda et al., 2006b
Thyroid hormones
Thyroxine	+	HEK293c18	Hsiang et al., 1999
	3.0	XO	Abe et al., 1999
Triiodothyronine	2.7	XO	Abe et al., 1999
Iodothyronine sulfates	+	COS1	van der Deure et al., 2008
Eicosanoids
Leukotriene C₄	+	XO	Abe et al., 1999
Leukotriene E₄	+	XO	Abe et al., 1999
Prostaglandin E₂	+	XO	Abe et al., 1999
	+	HEK293	Tamai et al., 2000
Thromboxane B₂	+	XO	Abe et al., 1999
Others
Bilirubin	0.16	HEK293	Cui et al., 2001
	0.0076	XO	Briz et al., 2003
Bilirubin monoglucuronide	0.1	HEK293	Cui et al., 2001
Bilirubin diglucuronide	0.3	HEK293	Cui et al., 2001
CCK-8	+	HEK293	Hirano et al., 2004
DHEAS	+	XO	Abe et al., 1999
	22	HEK293	Cui et al., 2001
E₂17βG	+	XO	Abe et al., 1999
	8.2	HEK293	König et al., 2000b
	9.7	XO	Nakai et al., 2001
	3.7	XO	Tamai et al., 2001
	8.2	HEK293	Cui et al., 2001
	28	MDCKII	Sasaki et al., 2002
	8.3	HEK293	Hirano et al., 2004
	6.3	HEK293	Sharma et al., 2009
E₁S	+	XO	Abe et al., 1999
	0.2	HEK293	Tamai et al., 2000
	5.3	XO	Tamai et al., 2001
	13	HEK293	Cui et al., 2001
	0.5	HEK293	Hirano et al., 2004
	+	MDCKII	Kopplow et al., 2005
	0.23, 45	HEK293	Noé et al., 2007
	+	COS1	van der Deure et al., 2008
	+	Flp-In-293	Nakakariya et al., 2008

CCK-8, cholecystokinin octapeptide; CHO, Chinese hamster ovary; DADLE, [d-Ala²,d-Leu⁵]-enkephalin (opioid peptide analog); DHEAS, dehydroepiandrosterone sulfate; E₂17βG, estradiol-17β-D-glucuronide; E₁S, estrone-3-sulfate; HEK293, human embryonic kidney 293 cells; HepG2, a human liver carcinoma cell line; MDCKII, Madin-Darby canine kidney cells; XO, Xenopus laevis oocyte; +, substrate of OATP1B1, but K_m not available.