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. Author manuscript; available in PMC: 2021 Feb 13.
Published in final edited form as: J Med Chem. 2020 Jan 16;63(3):1032–1050. doi: 10.1021/acs.jmedchem.9b01218

Table 3.

Middle ring and right side ring modified EP2 antagonists. Potency and aqueous solubilitya

Compound ID graphic file with name nihms-1607948-t0019.jpg EP2 KB (nM) Aqueous Solubilityb (μM)
20a graphic file with name nihms-1607948-t0020.jpg 10.7 27
20b graphic file with name nihms-1607948-t0021.jpg 8.0 25
20c graphic file with name nihms-1607948-t0022.jpg 6.4 15
20d graphic file with name nihms-1607948-t0023.jpg 44.5 5
20e graphic file with name nihms-1607948-t0024.jpg 6.1 25
20f graphic file with name nihms-1607948-t0025.jpg 96 41
20g graphic file with name nihms-1607948-t0026.jpg 230 13
20h graphic file with name nihms-1607948-t0027.jpg 7.8 15
20i graphic file with name nihms-1607948-t0028.jpg 1220 10
20j graphic file with name nihms-1607948-t0029.jpg 32.5 5
20k graphic file with name nihms-1607948-t0030.jpg 104 ND
20l graphic file with name nihms-1607948-t0031.jpg 166 ND
20m graphic file with name nihms-1607948-t0032.jpg 39 6
20n graphic file with name nihms-1607948-t0033.jpg 79.3 25
20o graphic file with name nihms-1607948-t0034.jpg 9.7 15
20p graphic file with name nihms-1607948-t0035.jpg >1000 38
20q graphic file with name nihms-1607948-t0036.jpg 8.3 17
20r graphic file with name nihms-1607948-t0037.jpg 88.1 100
a

Schild KB values are calculated similarly as indicated at Table 1 legend. KB values are average of 2 measurements run in duplicate. ND = not determined

b

The solubility of the compounds is measured in PBS buffer (pH 7.4) with 1% DMSO by nephelometry.46