. Author manuscript; available in PMC: 2022 Apr 22.

Published in final edited form as: J Med Chem. 2021 Mar 31;64(8):5099–5122. doi: 10.1021/acs.jmedchem.1c00164

Table 2.

Species Dependence of Binding of Various P2Y₁₄R Antagonists, as Determined in a Fluorescent Antagonist Binding Assay in Whole Cells (n = 3–4)^c

compound	mP2Y₁₄R, IC₅₀ (nM)^a	hP2Y₁₄R, IC₅₀ (nM)^a
1b^b	29.7 ± 9.3	27.6 ± 4.3
3a^b	142 ± 58	31.7 ± 8.0
4^b	384 ± 88	169 ± 42
5^b	902 ± 344	269 ± 121
6^b	499 ± 57	233 ± 26
11	155 ± 79	197 ± 29
19	375 ± 175	308 ± 63
29	184 ± 24	296 ± 13
32	18.6 ± 8.4	15.0 ± 4.4

Fluorescence binding assays using 2 (20 nM, for a 45 min incubation) as a tracer. The hP2Y₁₄R was stably expressed in CHO cells, and the mP2Y₁₄R was stably expressed in HEK293 cells.

Data from Jung et al.² and Mufti et al.⁷

See Table 1 for structures.