. Author manuscript; available in PMC: 2020 Dec 11.

Published in final edited form as: J Med Chem. 2020 Jun 18;63(13):7033–7051. doi: 10.1021/acs.jmedchem.0c00366

Table 5.

Functional and pharmacokinetic properties of pyridine and pyrimidine analogs of 13^α

Cpd	EC50 (nM)	hPPB (%)	mPPB (%)	t1/2 HLM (min)	t1/2 MLM (min)	PAMPA-BBB Pe (nm/sec)
13	8.18 (6.55, 10.15)	90.4	96.7	>145	127	22.9
19	23.15 (6.68, ND)	42.9	29.1	>145	>145	0.441
20	4.14 (3.32–5.11)	27.5	40.9	>145	125.3	0.523
21	1.27 (0.97–1.64)	24.8	18	>145	>145	0.744
22	4.58 (3.40–6.02)	92.5	96.7	>145	>145	0.053

^α

EC₅₀ values are mean with 95% confidence limits.