TABLE 1

List of compounds tested for their modulatory effect against CP-I as substrate, and their classification into type of modulator: compounds with no modulation are listed first, followed by inhibitors in order of increasing IC₅₀, followed by stimulators

Compound	Type of modulator	IC₅₀ (mean ± SD)	Comments	Compound	Type of modulator	IC₅₀ (mean ± SD)	Comments
		µM				µM
Acetaminophen	None	ND	No effect	E17βG	Inhibitor/stimulator	188 ± 32	Moderate inhibitor; maximum net stimulation 39% at 1 µM
Etoposide	None	ND	No effect	Indomethacin	Inhibitor	214 ± 14	Weak inhibitor
Nodolol	None	ND	No effect	TDCA	Inhibitor	228 ± 22	Weak inhibitor
Tolbutamide	None	ND	No effect	Lovastatin	Inhibitor	237 ± 9	Weak inhibitor
α-Bilirubin	None	ND	No effect	DCA	Inhibitor	252 ± 2	Weak inhibitor
CA	None	ND	No effect	Glyburide	Inhibitor	280 ± 79	Weak inhibitor
GCA	None	ND	No effect	Glimpride	Inhibitor	305 ± 43	Weak inhibitor
TCA	None	ND	No effect	GDCA	Inhibitor	325 ± 20	Weak inhibitor
Pravastatin	None	ND	No effect	GCDCA	Inhibitor	410 ± 40	Weak inhibitor
Metformin	None	ND	No effect	Rosuvastatin	Inhibitor	412 ± 183	Weak inhibitor
Benzbromarone	Inhibitor	11 ± 0.5	Strong inhibitor	Irinotecan	Inhibitor	532 ± 171	Weak inhibitor
Bromosulfophthalein	Inhibitor	26 ± 2	Strong inhibitor	Bumetanide	Inhibitor	541 ± 172	Weak inhibitor
MK-571	Inhibitor	39 ± 3	Strong inhibitor	Gemfibrozil	Inhibitor	648 ± 71	Weak inhibitor
Troglitazone	Inhibitor	53 ± 3	Strong inhibitor	Phenylbutazone	Inhibitor	777 ± 47	Weak inhibitor
Rifamycin SV	Inhibitor	59 ± 1	Strong inhibitor	Nimodipine	Inhibitor	793 ± 35	Weak inhibitor
Atorvastatin	Inhibitor	60 ± 3	Strong inhibitor	Probenecid	Inhibitor	1121 ± 67	Weak inhibitor
Losartan potassium	Inhibitor	74 ± 3	Strong inhibitor	Budesonide	Stimulator	ND	Maximum net stimulation 82% at 250 µM
Rifampicin	Inhibitor	83 ± 8	Strong inhibitor	DHA3S	Stimulator	ND	Maximum net stimulation 62% at 100 µM
CDF	Inhibitor	130 ± 20	Moderate inhibitor	Mitoxantrone	Stimulator	ND	Maximum net stimulation 180% at 100 µM
Simvastatin	Inhibitor	132 ± 24	Moderate inhibitor	Progesterone	Stimulator	ND	Maximum net stimulation 95% at 50 µM
Terfenadine	Inhibitor	150 ± 2	Moderate inhibitor	Testosterone	Stimulator	ND	Maximum net stimulation 79% at 100 µM
Sulfasalazine	Inhibitor	161 ± 45	Moderate inhibitor	E3S	Stimulator	ND	Maximum net stimulation 34% at 100 µM
Diclofenac	Inhibitor	168 ± 14	Moderate inhibitor
CDCA	Inhibitor	175 ± 21	Moderate inhibitor	Pyrimethamine	Stimulator	ND	Maximum net stimulation 49% at 1 µM

CA, cholic acid; CDCA, chenodeoxycholic acid; CDF, carboxydichlorofluorescein; DCA, deoxycholic acid; E3S, estrone 3-sulfate; GCA, glycocholic acid; moderate inhibitor, IC₅₀ = 100–200 µM; ND, not determined; strong inhibitors, IC₅₀ <100 µM; TCA, taurocholic acid; weak inhibitor, IC₅₀ >200 µM.