GSK682753A is a selective and highly potent inverse agonist of the Epstein-Barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.

EBI2/GPR183:53.6 nM

GSK682753A exhibits dose-dependent inhibition of EBI2, achieving an IC50 of 53.6 nM. It demonstrates similar potency in inhibiting ERK phosphorylation, GTPγS binding, and activation of the cAMP-response element-binding protein (CREB). Additionally, GSK682753A acts as a selective and highly potent inverse agonist for both murine and human EBI2, effectively blocking G protein-dependent and potentially G protein-independent signals. In assays using cAMP-response element-binding protein-based reporters and guanosine 5'-3-O-(thio)-triphosphate (GTPγS) binding, GSK682753A shows a potency range of 2.6-53.6 nM and achieves an inhibitory efficacy of 75%.