Table 10

Category IIB₁: transported substrates (YNN)

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
Actinomycin	<0.21^10-a	92.3	16.0 ± 7.94	103	>80	Y	1.20	N	1.39	N
Chloroquine	44.9 ± 3.34	89.0	172 ± 5.54	93.8	3.83	Y	0.77	N	2.49	N
Cimetidine	12.3 ± 1.29	86.4	26.9 ± 1.09	92.1	2.19	Y^10-b ^10-c	1.31	N	0.16	N
Colchicine	17.9 ± 1.75	76.4	202 ± 9.71	76.0	11.34	Y	1.23	N	−0.74	N
Daunorubicin	5.47 ± 1.08	74.9	77.7 ± 4.33	74.6	14.2	Y^10-b	1.69	N	−0.69	N
Dexamethasone	43.5 ± 18.6	139	537 ± 24.5	117	12.4	Y	1.15	N	1.72	N
Etoposide	21.4 ± 6.65	111	60.6 ± 4.58	124	2.8	Y	1.01	N	1.34	N
Hoechst 33342	3.35 ± 0.98	64.2	26.0 ± 4.07	73.2	7.75	Y	0.86	N	3.49	N
Mitoxantrone	1.91 ± 0.66	85.4	6.44 ± 1.17	81.2	3.38	Y	0.85	N	2.89	N
Neostigmine	7.58 ± 1.58	71.3	13.7 ± 1.46	83.4	1.81	Y^10-b	1.06	N	0.31	N
Puromycin	11.5 ± 0.35	89.1	35.6 ± 3.30	105	3.1	Y^10-b	1.21	N	1.91	N
Vincristine	2.36 ± 0.19	95.3	14.9 ± 1.32	93.7	6.31	Y	1.46	N	8.40	N
Vinorelbine	2.52 ± 1.94	89.5	176 ± 12.9	94.3	69.8	Y^10-b	1.15	N	6.24	N
Mean	14.6		105		11.6		1.15		2.22
Median	9.54		35.6		5.07		1.15		1.72
Minimum	1.91		6.44		1.81		0.77		−0.74
Maximum	44.9		537		69.8		1.69		8.40

n = 13 compounds.

Y, yes; N, no.
↵10-a Compound concentrations in samples below the limit quantification (BQL). P_app value is calculated from the lowest detectable standard.
↵10-b Run in the presence and absence of 2 μM GF120918 to confirm whether the compound is transported by Pgp.
↵10-c Run twice with the results and mass balances similar between experiments.