TABLE 1.

Representative examples of different types of synthetic or natural ligands (agonists, unless noted), either mononucleotide or dinucleotide (or nucleotide sugar), for each of the P2YRs

The potency (nM) was measured in functional assays at the human P2YRs.

P2YR	Synthetic Agonist (Mononucleotide), Potency	Bifunctional Ligand, Potency	References
	nM
P2Y1	1, MRS2365, 0.4	2, Up4(β-B)A, A isomer, 500	Houston et al., 2008; Yelovitch et al., 2012
P2Y2	3, MRS2698, 8.0	4, INS37217, 220	Houston et al., 2008; Yerxa et al., 2002
P2Y4	5, MRS4062, 26	6, INS365 (Up4U)a, 130	Ko et al., 2008; Maruoka et al., 2011
P2Y6	7, 5-OMe-UDPαB, 8	8, MRS2957, 12	Maruoka et al., 2010; Haas et al., 2014
P2Y11	9, ATP-γ-S, 24,000	10, NAADP, 64,000	Djerada and Millart, 2013
P2Y12	11, 2MeSADPb, 5	12, compound 17 (R/S)c, 13	Zhang et al., 2002; Yanachkov and Wright, 2010
P2Y13	11, 2MeSADPb, 19	13, Ap3A, 72	Zhang et al., 2002
P2Y14	14, MRS2905, 2.0	15, MRS2690, 70	Das et al., 2010

NAADP, nicotinic acid adenine dinucleotide phosphate.

^aINS365 also activates P2Y₂R (EC₅₀ = 210 nM).

^b2MeSADP activates P2Y₁R (EC₅₀ = 6.6 nM), P2Y₁₂R, and P2Y₁₃R (also used as a high affinity ³H- or ³³P-radioligand) (Takasaki et al., 2001).

^cAntagonist.