CID-16020046

CID-16020046 is a GPR55 inverse agonist that antagonizes GPR55 constitutive activity with an IC50 value of 15 ?M.{29659} It inhibits GPR55-mediated ERK1/2 phosphorylation, LPI-induced Ca2+ signaling (IC50 = 0.21 ?M in HEK-GPR55 cells), and GPR55-mediated transcription factor activation.{29659} It does not affect ERK1/2 phosphorylation or transcription factor activation in CB receptor expressing cells and demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptors.{29659} This compound has been shown to block GPR55-mediated endothelial wound healing and reverse LPI-inhibited platelet aggregation.{29659}