TABLE 1

K_i values obtained using pooled HLMs

Global S.E. for data fitting was less than 20% and r² = >0.80 for each effector.

Effector	K_i Values with Probe Substrate
Effector	TST	MDZ	SIL	FLU	BUD	QUI	BUS	SIM	FEL
	μM
AMG 458	0.55	7.3^{^a}	1.0	3.3	7.3	5.6	ACT^{^b}	7.7	8.6^{^c}
Budesonide	ACT	0.10	0.17	0.14	X	0.18	0.038	1.3	13.1
Buspirone	50	0.54	2.1	9.3	13.2	1.3	X	10.3	50
Clozapine	7.4	0.42	17.6	9.3	2.1	5.4	0.74	17.1	10.4
Cyclosporine	24.2	3.1^{^c}	3.5	6.9^{^c}	1.5	0.36	1.1	12.7	4.3
Dextromethorphan	50	8.6	50	50	50	50	26.2	50	24.8^{^c}
Felodipine	ACT	0.25^{^c}	0.65	0.44	0.085	0.20^{^c}	0.87	0.43	X
Fluoxetine	8.7	4.2^{^c}	3.3	50	47.0	2.7	5.5^{^c}	ACT	50
Fluticasone	ACT	0.085	0.39	X	0.16	0.93	0.080	17.1	0.79
Fluvoxamine	20.4	2.6	2.7	50	0.68	1.6	5.3^{^c}	16.1	50
Haloperidol	27.4	2.3^{^c}	2.4	3.1	0.84	3.6	0.61	9.4	2.9^{^c}
Itraconazole	0.013	0.013	0.016	0.012	0.044	0.016	0.016^{^c}	0.052	0.045
Ketoconazole	0.023	0.014^{^c}	0.017	0.044	0.011	0.009	0.021^{^c}	0.072	0.079
Midazolam	6.4	X	1.8	0.74	4.2	0.97	0.85	8	30.5
Nifedipine	ACT	1.8^{^c}	8.7	0.46	0.27	1.9^{^a}	0.95	1.7	14.9
Sertraline	10.4	3.1^{^c}	2.1^{^c}	12.6	0.20	1.2^{^c}	2.1^{^c}	1.6	50
Sildenafil	50	0.71	X	3.9	2.1	1.1	2.0	14.6	50
Simvastatin	35.0	0.16	0.37	0.38	0.31	0.81^{^c}	0.54	X	16.5^{^c}
Terfenadine	11.2	1.0^{^c}	0.21	0.31	0.055	0.066	0.13	1.3	1.2
Testosterone	X	2.7^{^a}	9.5	1.8	5.0	50	3.7	1.2	ACT

TST, testosterone; MDZ, midazolam; SIL, sildenafil; FLU, fluticasone; BUC, budesonide; QUI, quinicine; BUS, buspirone; SIM, simvastatin; FEL, felodipine.
↵a Linear-mixed inhibition.
↵b Activation.
↵c Noncompetitive inhibition.