Fig. 2: Pharmacological profiling of niacin, MK6892 and GSK256073 on GPR109A. | Nature Communications

Fig. 2: Pharmacological profiling of niacin, MK6892 and GSK256073 on GPR109A.

From: Structure-guided engineering of biased-agonism in the human niacin receptor via single amino acid substitution

Fig. 2

a Chemical structure of MK6892 and GSK256073. NanoBiT-based heterotrimeric GoA/GoB dissociation assay in response to MK6892 and GSK256073 with niacin as a reference ligand. b, c showing GoA and GoB dissociation respectively (mean ± SEM; n = 4; fold normalized with the minimum concentration for each ligand as 1). d Agonist stimulated forskolin-induced cAMP decrease measured by GloSensor assay (mean ± SEM; n = 4; % normalized with the minimum concentration for each ligand as 100). e, f βarr1/2 recruitment downstream of GPR109A in response to MK6892 and GSK256073 was studied by NanoBiT-based assay (mean ± SEM; n = 6; fold normalized with the minimum concentration for each ligand as 1). Source data is provided as Source Data file.

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