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. Author manuscript; available in PMC: 2017 Oct 4.
Published in final edited form as: Eur J Med Chem. 2016 May 24;121:517–529. doi: 10.1016/j.ejmech.2016.05.044

Table 3.

Effect of photoactivatable allosteric modulators on stimulation of [35S]GTPγS binding to HEK293 cell membranes expressing the CB1 wild-type receptor.

Concentration of photoactivatable allosteric modulators
Compd 0 µM 3.2 µM 10 µM

Emax
(fmol/mg)a
EC50
(nM) a
Emax
(fmol/mg) a
EC50
(nM) a
Emax
(fmol/mg) a
EC50
(nM) a
26 68.9 ± 1.7 4.7 (2.7–8.0) 41.3 ± 1.1 2.7 (0.9–4.6) ND ND
27 68.9 ± 1.7 4.7 (2.7–8.0) 27.0 ± 1.3 7.9 (2.8–22.0) ND ND
28 68.9 ± 1.7 4.7 (2.7–8.0) 34.1 ± 1.1 2.1 (0.5–8.3) ND ND
36b 68.9 ± 1.7 4.7 (2.7–8.0) 31.1±0.9 1.2 (0.5–3.8) ND ND
a

Emax and EC50 values were determined from the CP55,940 dose-response curves. The level of GTPγS binding of mock-transfected cell membrane (30.1 ± 1.6 fmol/mg) was subtracted from each Emax value. ND, no detectable specific [35S]GTPγS binding.

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