. Author manuscript; available in PMC: 2018 Jun 8.

Published in final edited form as: J Med Chem. 2017 May 19;60(11):4594–4610. doi: 10.1021/acs.jmedchem.6b01885

Table 6.

Physicochemical Properties, Solubility at pH 7.4, and Microsomal Stability in Mouse Liver Microsomes of Selected Compounds^a

compd	EC₅₀ (µM)	% activation	MW	PSA	cLogP	solubility at pH 7.4 (µM)	mouse microsome T_1/2 (min)	human microsome T_1/2 (min)
4	1.8	242	282	51	3.4	6	<5	NT
4c	0.28 ± 0.03	190 ± 32	230	51	2.7	59	<5	NT
23	0.5 ± 0.08	182 ± 23	297	51	3.9	NT	<5	NT
4r	0.26 ± 0.0	211 ± 2	270	75	2.4	12	<5	NT
4e	0.34 ± 0.03	180 ± 32	248	51	2.8	49	<5	NT
4m	0.36 ± 0.09	195 ± 15	231	63	2.0	77	>120	>120
26	0.5 ± 0.15	100 ± 16	311	42	4.8	NT	<5	NT
27	0.29 ± 0.09	190 ± 11	327	62	3.4	31	39	>120

NT, not tested.