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. Author manuscript; available in PMC: 2019 May 15.
Published in final edited form as: Bioorg Med Chem. 2018 Apr 6;26(9):2514–2529. doi: 10.1016/j.bmc.2018.04.016

Table 1.

Inhibition data of select antagonists in the PAR1-mediated iCa2+ mobilization assay.

Entry ID# Structure % Inhibition & IC50a Log IC50 ± Std. Error
1 Vorapaxar graphic file with name nihms961974t1.jpg 95%;
0.032 μM		 − 7.5 ± 0.084
2 Atopaxar graphic file with name nihms961974t2.jpg 94%;
0.033 μM		 − 7.5 ± 0.10
3 RWJ-58259
11a 		graphic file with name nihms961974t3.jpg 94%;
0.020 μM		 − 7.7 ± 0.065
4 DG-207
12 		graphic file with name nihms961974t4.jpg 76%;
0.29 μM		 − 6.5 ± 0.074
5 ML161
16 		graphic file with name nihms961974t5.jpg 82%;
0.85 μM		 − 6.7 ± 0.099
6 CJD-125
17 		graphic file with name nihms961974t6.jpg 74%;
3.16 μMb 		N.D.
7 EMG-21
18 		graphic file with name nihms961974t7.jpg 68%;
3.31 μM		 − 5.5 ± 0.26
8 EMG-23
19 		graphic file with name nihms961974t8.jpg 49% N.D.
9 RR-90
21 		graphic file with name nihms961974t9.jpg 77%;
0.97 μM		 − 6.0 ± 0.19
10 DG-5
26 		graphic file with name nihms961974t10.jpg 77%;
94 μM		 − 4.0 ± 2.9
11 RR-10
20 		graphic file with name nihms961974t11.jpg 79%;
81 μM		 − 4.0 ± 5.1
a

%Inhibition of PAR1 antagonists in presence of 5 μM TFLLRN-NH2. N.D. = not determined.

b

Estimated IC50 (incomplete curve at high concentration).