. Author manuscript; available in PMC: 2019 Jul 26.

Published in final edited form as: J Med Chem. 2018 Jul 16;61(14):6178–6192. doi: 10.1021/acs.jmedchem.8b00613

Table 3:

Solubility (in PBS) and Permeability values of compounds 4, 12h and 12r

Compound	Solubility (μM)		Papp × 106 (cm/s)	Efflux ratio^c
4	3.44 ± 0.03	A-B^a	45.45 ± 0.07	0.68
4	3.44 ± 0.03	B-A^b	30.80 ± 0.08	0.68
12h	51.30 ± 0.02	A-B^a	30.32 ± 0.01	1.43
12h	51.30 ± 0.02	B-A^b	43.48 ± 0.02	1.43
12r	0.52 ± 0.23	A-B^a	31.33 ± 0.03	0.58
12r	0.52 ± 0.23	B-A^b	18.28 ± 0.26	0.58
Propanolol	117 ± 0.15		ND^d
Ketoconazole	32.00 ± 0.03		ND^d
Tamoxifene	1.32 ± 0.09		ND^d
Metoprolol	ND^d	A-B^a	39.29 ± 0.04	0.78
Metoprolol	ND^d	B-A^b	30.66 ± 0.00	0.78
Atenolol	ND^d	A-B^a	1.21 ± 0.00	1.03
Atenolol	ND^d	B-A^b	1.25 ± 0.00	1.03
Quinidine	ND^d	A-B^a	13.03 ± 0.01	3.22
Quinidine	ND^d	B-A^b	41.99 ± 0.01	3.22

A-B: Apical to Basolateral

B-A: Basolateral to Apical

Efflux ratio: B-A/A-B

ND: not determined