From HTS to Market: the Discovery and Development of Maraviroc, a CCR5 Antagonist for the Treatment of HIV - Accounts in Drug Discovery Case Studies in Medicinal Chemistry - page 196

Table 9.4 Potency is maintained with a range of 4-substituted piperidines,
even when the phenyl ring is removed

R

H N

O

Compound R Binding IC 50 LE log D

8 4 nM 0.36 2.5

N

N

16 15 nM 0.33 1.8

O

N

17 2 nM 0.36 nd

N

O

N

18 55 nM 0.29 2.9

N

N

N

19 2 nM 0.36 3.1

N

N

N

20 10 nM 0.36 43.6

N

N

O