TABLE 6

HPTC P-gp efflux-active concentration and elementary kinetic parameters for the data in Table 5

Cells	Kidney Number^a	Inhibitor	T(0)^a	k_B^a	k_rQ^b	K_QB^c	%CV^d	K_i^e	IC₅₀/K_i
Cells	Kidney Number^a	Inhibitor	M	s⁻¹	s⁻¹	M⁻¹	%CV^d	μM	IC₅₀/K_i
HPTC	6	Carvedilol	3E−05	17	1E+04	1E+05	0.13	0.3	4.9
	10	′′	1E−05	2	1E+04	7E+06	0.04	0.3	0.2
	13	Diltiazem	3E−05	15	7E+04	2E+06	0.09	2.0	0.6
	8	Isradipine	2E−04	8	6E+04	1E+04	0.18	1.7	5.1
	2	Ketoconazole	3E−05	20	3E+04	1E+04	0.19	0.9	11.4
	3	′′	2E−05	45	3E+04	2E+06	0.09	0.9	0.8
	11	′′	1E−05	40	3E+04	1E+05	0.08	0.9	3.3
	7	Mibefradil	2E−04	15	8E+03	5E+03	0.08	0.2	18.4
	4	Nicardipine	1E−05	20	7E+03	5E+05	0.05	0.2	4.0
	13	′′	3E−05	15	7E+03	5E+05	0.08	0.2	1.5
	1	Quinidine	2E−05	9	1E+04	1E+04	0.04	0.3	2.5
	2	′′	3E−05	20	1E+04	2E+05	0.16	0.3	10.9
	12	Ranolazine	3E−05	9	5E+04	4E+05	0.08	1.4	1.3
	1	Verapamil	2E−05	9	2E+04	3E+05	0.08	0.6	1.9
	10	′′	1E−05	2	2E+04	3E+03	0.04	0.6	0.3

↵^a T(0), the P-gp efflux-active concentration (moles P-gp per liter of membrane), and k_B, the basolateral plasma membrane uptake transporter clearance (s⁻¹), are fitted independently for each kidney.
↵^b k_rQ is the consensus dissociation constant of inhibitor from P-gp (Table 3).
↵^c K_QB is the affinity constant of the inhibitor binding to the uptake transporter.
↵^d %CV is the coefficient of variation for the fit to the IC₅₀ curve expressed as a percentage.
↵^e K_i = (k_rQ/k₁) × K_QPC × 10⁶ (μM). Defined in Table 4.