GPR61 inverse agonist compound 1 is a potent and selective GPR61 inverse agonist with functional IC50 of 10-11 nM in cAMP assays.
Compound 1 is selective for GPR61 among a panel of GPCRs (off-target IC50 values >10 μM), with an excellent in vitro off-target profile.
Compound 1 binds an induced allosteric site that overlaps the binding site for Gαs and unexpectedly promotes a GPR61 conformation more similar to its active state than the inactive state.
Compound 1 is selective for GPR61 in a panel of common off-target GPCRs and against related receptors GPR62 and GPR101.
Compound 1 shows high potency and excellent off-target profile, Compound 1 is a high-quality tool compound for functional studies of GPR61.
