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. Author manuscript; available in PMC: 2021 Mar 12.
Published in final edited form as: J Med Chem. 2019 Dec 16;63(5):2372–2390. doi: 10.1021/acs.jmedchem.9b01287

Table 2.

Agonist activities of compounds 17–26 at LPA1 receptor

graphic file with name nihms-1602792-t0020.jpg
Cpd graphic file with name nihms-1602792-t0021.jpg n Emax (%)a EC50 (μM)b
17 graphic file with name nihms-1602792-t0022.jpg 118 ± 14 0.24 ± 0.09
18 graphic file with name nihms-1602792-t0023.jpg 6 N.E.c -
19 7 N. E. -
20 8 74 ± 4 2.1 ± 0.3
21 9 112 ± 3 0.5 ± 0.1
22 10 135 ± 31 3.2 ± 0.5
23 14 N.E. -
24 graphic file with name nihms-1602792-t0024.jpg 6 N.E. -
25 9 127 ± 9 3.3 ± 0.6
26 12 37 ± 1 19 ± 2
LPA graphic file with name nihms-1602792-t0025.jpg 100 0.83 ± 0.02
a

Emax = maximal efficacy of the drug/maximal efficacy of LPA, expressed as the percentage.

b

For Emax > 30%, EC50 values are expressed as mean ± s.e.m, from a minimum of two independent experiments, performed in triplicate.

c

N.E., no effect was observed at the highest concentration of compound tested (10 μM).