Table 2.

 HL3501 Is a Highly Selective A3AR Antagonist

				A3 Functional Assay
	Binding Affinity Assay (Ki)			Calcium Flux Assay (IC50)
Compound	hA1	hA2a	hA3	Agonist Assay	Antagonist Assay
HL3501	>10 µM	>10 µM	20 nM	>10 µM	18 nM

All human AR experiments were performed using adherent CHO cells and HEK293 cells stably transfected with cDNA encoding the appropriate receptor. In the functional assay, NECA was the reference agonist for A3 (E_max = 1.25 µM), and VUF 5574 was the reference antagonist for A3 (I_max = 0.0375 µM).