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. Author manuscript; available in PMC: 2024 Sep 30.
Published in final edited form as: J Med Chem. 2024 May 24;67(11):9709–9730. doi: 10.1021/acs.jmedchem.4c00856

Table 3.

EC50 and Emax of Compounds 24a−k

graphic file with name nihms-2023639-t0018.jpg
compound R3 Clog Pa EC50 (nM)b Emax (%)b
4a 3-CF3 4.10 119 ± 16 100 ± 5
15b 3-CF3 4.47 47 ± 8 143 ± 5
24a 3,5-di-CF3 5.48 211 ± 51 127 ± 11
24b 2,4-di-CF3 5.48 52 ± 11 150 ± 12
24c 4-CF3 4.47 220 ± 58 120 ± 9
24d 2-CF3 4.47 143 ± 33 122 ± 13
24e 3-Cl, 5-F 4.24 46 ± 8 135 ± 9
24f 3-OMe 3.46 53 ± 10 133 ± 10
24g H 3.45 278 ± 48 139 ± 9
24h 4-Cl, 2-F 4.24 235 ± 47 131 ± 8
24i 3-F 3.59 136 ± 33 137 ± 7
24j 4-F 3.59 90 ± 17 146 ± 9
24k 3-OCF3 4.35 30 ± 8 137 ± 7
a

Clog P is calculated from a web calculator: http://biosig.unimelb.edu.au/pkcsm/prediction.

b

Values are mean ± SEM from n ≥ 3 independent experiments.

Emax (%) is the efficacy maximum of the compounds in the cAMP assay relative to compound 4a as 100% and DMSO as 0%.