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. 2015 Feb;87(2):197–206. doi: 10.1124/mol.114.095471

TABLE 4.

LDK1229 binding to the wild-type or mutant CB1 receptors using [3H]CP55,940 or [3H]WIN55,212-2 as a tracer

Receptor [3H]CP55,940
Kia Ki Ratiob
nM
CB1 wild type 220 (106–457) 1:1
K3.28192A 1316 (1115–1626)c 1:4c
W5.43279A ND
W6.48356A 1987 (895–2736) 1:9
C7.42386M 1010 (832–1154) 1:5

ND, not detectable; 39% displacement at 32 µM.

a

Data are the median and corresponding 95% confidence limits of three independent experiments performed in duplicate. Ki values were determined from competition binding assays using [3H]CP55,940 as tracer at its respective Kd values, as described in Results.

b

Wild type:mutant.

c

Binding was performed with [3H]WIN55,212-2 as a tracer. LDK1229 binding to CB1 wild type using [3H]WIN55,212-2 as a tracer yielded a Ki of 324 nM (205–524).