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. Author manuscript; available in PMC: 2014 Mar 27.
Published in final edited form as: J Med Chem. 2012 Oct 31;55(22):9973–9987. doi: 10.1021/jm301212u

Table 2.

Radioligand Competition Binding Affinity(Ki) Data of PAM Derivatives

graphic file with name nihms562666t2.jpg
compd Ri X MW cLogP Ki(CB2),
nMa,b,c 		Ki(CB1),
nMa,b,c
48 H CH2 372.46 3.99 NB NB
49 H CH2CH2 386.49 4.44 9,319 NB
50 H CH=CH 384.47 4.54 5,683 NB
1d,e 2.1 NT
10d,f NT 10.6
a

Binding affinities of compounds for CB1 and CB2 receptor were evaluated using [3H]CP-55,940 radioligand competition binding assay.

b

NB: no binding, Ki > 20000 nM.

C

NT: not tested.

d

The binding affinities of reference compounds were evaluated in parallel with compounds 9, 11–61 under the same conditions.

e

CB2 reference compound SR144528.

f

CB1 reference compound SR141716.