TABLE 2
Small-molecule ligands for the PTHR1
| Compound | Structure | Class | Potency (Assay) | References |
|---|---|---|---|---|
| AH-3960 |  | Agonist | EC50 = ∼2 μM (stimulation of cAMP-responsive CRE-luciferase reporter activity in HEK-293/PTHR1 cells) | Rickard et al., 2006 |
| SW106 |  | Antagonist | IC50 = ∼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) |  | Antagonist | IC50 = ∼30 nM (inhibition of cAMP signaling induced by PTHrP(1–34) in SaOS2 cells) | McDonald et al., 2007 |