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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 6.

In vitro Activity of Carboxylate Isosteres

Compound X Ratio (5/50)a Fold-Signalb
19a graphic file with name nihms-1577324-t0022.jpg 1.0 0.1
19b graphic file with name nihms-1577324-t0023.jpg 0.5 0.6
19c graphic file with name nihms-1577324-t0024.jpg 1.2 0.1
19d graphic file with name nihms-1577324-t0025.jpg 0.4 1.6
19e graphic file with name nihms-1577324-t0026.jpg 0.9 0.1
19f graphic file with name nihms-1577324-t0027.jpg 0.2 1.1
4b graphic file with name nihms-1577324-t0028.jpg 0.8 1.3
GW590735 1.0 1.0
a

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

b

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