TABLE 3

Cooperativity estimates (logβ) for mGlu5 NAMs from functional assays

Collated data were fitted to the operational model of allosterism. Data represented as means ± S.E.M. from the indicated number (n) of independent experiments performed in triplicate.

Ca2+ mobilizationIP1 accumulationERK1/2 phosphorylationReceptor internalization
logβnlogβnlogβnlogβn
AZD2066full NAM3full NAM4full NAM3−0.30 ± 0.043
Basimglurantfull NAM3full NAM4full NAM4−0.41 ± 0.063
Dipraglurantfull NAM3full NAM4full NAM3−0.32 ± 0.043
F169521full NAM3full NAM4full NAM3−0.44 ± 0.073
F1699611full NAM3full NAM4full NAM3−0.28 ± 0.033
Mavoglurantfull NAM3full NAM4full NAM3−0.26 ± 0.033
Remeglurantfull NAM3full NAM4full NAM3−0.39 ± 0.053
(RS)-remeglurantfull NAM3full NAM4−0.24 ± 0.043−0.41 ± 0.073
STX107full NAM3full NAM4full NAM3−0.30 ± 0.053