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. 2021 Mar 25;64(7):3827–3842. doi: 10.1021/acs.jmedchem.0c01856

Table 2. Compound Potency and Intrinsic Activity Derived from the Label-Free Whole-Cell Assay Performed on HEK293-hA2AR Cellsa.

compound pEC50 Emax, %
CGS21680 8.85 ± 0.08 100 ± 2
8 8.01 ± 0.22 66 ± 5
1 6.57 ± 0.37 41 ± 5
2 6.09 ± 0.23 –48 ± 5
3 7.35 ± 0.28 –50 ± 5
4 5.78 ± 0.38 37 ± 7
6 N.D. N.D.
a

Data are shown as mean ± S.E.M. of three independent experiments performed in duplicate. Log potency (pEC50) and efficacy (Emax) were calculated from concentration–response curves derived from the peak analysis of CI changes. N.D., not determined.