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. 2017 Jan;91(1):39–47. doi: 10.1124/mol.116.106666

TABLE 1.

Identification of the minimum pharmacophore: biologic activities and molecular weights of VU0652925 analogs

Platelet activation was induced by 200 μM PAR4-AP, 100 nM γ-thrombin, or 20 μM PAR1-AP. Data are presented as the means of at least three independent experiments. Experiments were conducted at 10 μM antagonist for the percent maximum values.

Example VU Number PAR4-AP
γ-Thrombin
PAR1-AP
MW
Max PAC-1 IC50 PAC-1 Max PAC-1 IC50 PAC-1 Max PAC-1
% pM % nM %
1 VU0652925 0 43 0 229b 94 460.53
2 VU0661247 0 210 0 3.03 51.5 407.44
3 VU0661245 0 472 0 8.42 92.6 331.35
4 VU0807074 0.19 1.68a 21.1 16.2 105 301.32
5 VU0807081 0.27 176 0 7.18 102 301.32
6 VU0806526 0.20 1.69a 6.99 58.8 111 271.04

MW, molecular weight.

a

Values are given in nanomoles.

b

Values are given in picomoles.