Table 8

Category I: possible inhibitors (NNY)

Compound Name	P_app A → B	Mass Balance A → B	P_app B → A	Mass Balance B → A	BA/AB Ratio	Effluxed (Y/N)	ATPase Assay Ratio	ATPase Activator (Y/N)	Calcein-AM Assay	Calcein-AM Inhibitor (Y/N)
	nm/s		nm/s						% max
GF 120918	2.12 ± 1.21	20.5	18.6 ± 1.41	62.3	N.D.^8-a	N	0.23	N	100^8-b	Y
GW 420867	758 ± 142	98.9	726 ± 66.8	93.9	0.96^8-c	N	1.02	N	13.3	Y
Testosterone	916 ± 49.6	131	668 ± 49.2	122	0.73	N	1.32	N	69.0	Y
Mean	559		471		0.85		0.86		60.8
Median	758		668		0.85		1.02		69.0
Minimum	2.12		18.6		0.73		0.23		13.3
Maximum	916		726		0.96		1.32		100

n = 3 compounds.

Y, yes; N, no; N.D., not determined.
↵8-a GF120918 has high cellular accumulation, 37% of donor is associated with the cell.
↵8-b Calcein-AM results are for GF120918 tested at 1 μM.
↵8-c Run in the presence and absence of 2 μM GF120918 to confirm whether the compound is transported by Pgp.