Table 1 Comparison of the DAv values of nine GPCRs in various phylogenetic positions with or without ligands.

The class, group, and cluster of GPCRs are listed according to previous reports (1, 2). DAv was calculated from the MSD in fig. S8 based on Eqs. 1 and 2 in Materials and Methods. All data are means ± SEM of 20 cells. P values indicating the statistically significant difference between the vehicle and ligand conditions were calculated on the basis of Welch’s two-tailed t test. Under ligand conditions, GPCR-expressing HEK 293 cells were stimulated by the compound listed in the rightmost column. MECA is initials of GPCRs in this branch: the melanocortin receptors (MCRs), endothelial differentiation G-protein coupled receptors (EDGRs), cannabinoid receptors (CNRs), and adenosin binding receptors (ADORAs); DHA, docosahexaenoic acid; NECA, 5′-N-ethylcarboxamidoadenosine; TRAP-6, thrombin receptor activator peptide 6.

GPCRClassGroupBranchEndogenous
ligand
G protein
selectivity
DAv (μm2/s)t test
P value
Compounds
tested
VehicleLigand
ADRB2AαAmineAdrenalineGs0.078 ± 0.00240.051 ± 0.00231.2 × 10−9Isoproterenol (10 μM)
HTR2AAαAmineSerotoninGq/Gi0.079 ± 0.00220.065 ± 0.0342.1 × 10−3Serotonin (10 μM)
HRH1AαAmineHistamineGq0.064 ± 0.00230.045 ± 0.00251.1 × 10−6Histamine (1 μM)
ADORA2AAαMECAAdenosineGs0.66 ± 0.00220.058 ± 0.00168.0 × 10−3NECA (10 μM)
FFAR4AαMelatoninFree fatty acidGq0.083 ± 0.00250.048 ± 0.00733.5 × 10−13DHA (100 nM)
CXCR4AγChemokineChemokineGi0.087 ± 0.00340.068 ± 0.00171.7 × 10−5CXCL12 (20 nM)
F2RAδPurineThrombinGq/Gi/G120.084 ± 0.00410.060 ± 0.00171.4 × 10−5TRAP-6 (10 μM)
GCGRBSecretinPeptideGlucagonGs/Gq0.075 ± 0.00280.042 ± 0.00258.7 × 10−11Glucagon (1 μM)
mGluR3CAmino acidGlutamateGi0.47 ± 0.00220.039 ± 0.00189.1 × 10−3LY379268 (100 μM)
0.047 ± 0.00150.064 ± 0.00181.6 × 10−8LY341495 (1 μM)