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. Author manuscript; available in PMC: 2016 Nov 1.
Published in final edited form as: Bioorg Med Chem Lett. 2015 Aug 10;25(21):4733–4739. doi: 10.1016/j.bmcl.2015.08.021

Table 1.

Inhibition of P2Y14R binding in whole cells by known ligands of P2Y14R and P2Y6R using 11 as a FCM tracer. Results are expressed as mean±S.E (n=3).a

Compound hP2Y14R cAMP assay
(EC50 or IC50b, μM)		 FCM binding at hP2Y14R
(Ki, μM)
P2Y14 ligands
1 UDP 0.160 0.63±0.03
2 UDP-glucose 0.261 2.23±0.2
3 MRS2690 0.011 0.34±0.04
4 UDP-glucuronic acid 0.370 5.3±0.4
5 PPTN 0.00043 0.0019±0.0001
P2Y6 ligands
12 MRS2957c ND 5.18±0.20
13 MRS2578c ND No inhibition at 10 μM
a

FCM binding was measured in CHO cells expressing the hP2Y14R using a fixed concentration (50 nM) of 11, following an incubation of 30 min. Values in the cAMP assay were from published reports.10,20,21,24 ND, not determined.

b

IC50 values for P2YR antagonists 5 and 13.

c

Structures:

c