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. Author manuscript; available in PMC: 2021 Mar 26.
Published in final edited form as: J Med Chem. 2020 Mar 10;63(6):2854–2876. doi: 10.1021/acs.jmedchem.9b01189

Table 2.

In vitro Activity of 5a, 5b, 5b*, 5fa

graphic file with name nihms-1577324-t0018.jpg
Compound R Ratio (5/50)b Fold-Signalc
5a OMe 0.1 1.8
5b F 0.2 2.0
5b* F 0.6 1.8
5f CF3 0.2 1.2
a

All analogues contain the carboxylate head-group at the meta-position of the A-ring unless otherwise indicated.

*

indicates a para-carboxylate.

b

Ratio of relative light unit (RLU) signal at 5 μM and 50 μM compound concentrations.

c

Ratio of maximal signal strength observed for the compound of interest to that obtained with GW590735.