. Author manuscript; available in PMC: 2017 Mar 22.

Published in final edited form as: Bioorg Med Chem Lett. 2016 Mar 30;26(10):2481–2488. doi: 10.1016/j.bmcl.2016.03.102

Table 4.

In vitro and in vivo DMPK results of select compounds

Compound	D₄ (nM)	Microsome intrinsic clearance (mL/min/kg)		Plasma unbound fraction (F_u)

		hCL_INT	rCL_INT	Human	Rat
4a	12.3	147	4518	0.007	0.007
4g	19.1	65.3	251	0.006	0.012
4i	27	50.5	621	0.002	0.006
4j	16.2	50.5	247	0.002	0.007
4l	14.3	71.9	2128	0.031	0.037
4n	10.4	78.7	1597	0.010	0.019
4p	11.6	79.7	1505	0.010	0.025
4t	160	17.3	154	0.057	0.215
4y	47	60.5	433	0.039	0.074
4z	15.9	135	3137	0.035	0.069
4aa	2.2	46.7	614	0.006	0.010
4dd	5.4	31.6	184	0.037	0.075
4ee	5.2	71.1	1686	0.017	0.047
5m	10.8	93.0	1499	0.006	0.013
5n	10.1	68.9	1774	0.011	0.014
5u	21	101	4010	0.009	0.015
5y	3.3	230	4195	0.015	0.016
5z	29	98.2	5313	0.004	0.008
5aa	9.4	122	3217	0.008	0.005
5bb	7.4	366	6436	0.001	0.004