Small-molecule ligands for the PTHR1

CompoundStructureClassPotency (Assay)References
AH-3960Embedded ImageAgonistEC50 = ∼2 μM (stimulation of cAMP-responsive CRE-luciferase reporter activity in HEK-293/PTHR1 cells)Rickard et al., 2006
SW106Embedded ImageAntagonistIC50 = ∼5 μM (inhibition of cAMP signaling induced by M-PTH(1–14) analog in SaOS2 cells)Carter et al., 2007
Compound-19 (1,3,4-benzotriazepine: R1 = Me; R2 = cC6H11; R3 = H: R4 = Me; X = (CH2)2-1H-imidazol-2-yl)Embedded ImageAntagonistIC50 = ∼30 nM (inhibition of cAMP signaling induced by PTHrP(1–34) in SaOS2 cells)McDonald et al., 2007