Table 4.

FAC−MS Data in Comparison with [³⁵S]GTPyS Binding Results Obtained on GPR17-IAM-II and Mutated GPR17-IAM^a

	GPR17-IAM-II			mutated-GPR17-IAM
compd	tb (min)	EC 50	IC50 c(nM)	tb (min)	EC50	IC50c (nM)
UDP	2.69	1.14 ± 0.2/µM		2.15	3.0 ± 0.3 µM
13	2.79	945 ± 48 nM		2.51	1.87 ± 0.20 µM
12	3.55		582 ± 57
MRS2179	3.62		508 ± 29	3.47		227 ± 22
5	3.69		112 ± 7
7	4.5	11 ± 1 nM
8	4.77	1.7 ± 0.1 nM
6	5.67	1.4 ± 0.1 nM
cangrelor	10.6		0.7 ± 0.02	13.16		0.15 ±0.01
4	13.07	36 ± 3 pM		16.07	25.4 ± 1.0 pM

^aColumns: GPR17-IAM-II (19.5 million cells), mutated GPR17-IAM (19.5 million cells)

^bt is the breakthrough time of the ligand with the immobilized GPR17.

^cVersus UDP-glucose 10 µM.