Table 3.
Alkoxy analogues.
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---|---|---|---|---|
R | hSUCNR1 | mSUCNR1 | ClogPb | |
pEC50 (efficacy, %)a | ||||
17c | Me | 6.41 ± 0.14 (85.3 ± 4.5) | 7.39 ± 0.07 (84.2 ± 1.8) | 1.45 |
20 | F3C | 6.99 ± 0.15 (61.7 ± 3.6) | 6.72 ± 0.11 (69.7 ± 2.8) | 3.17 |
21 | Et | 6.59 ± 0.14 (56.3 ± 3.1) | 7.44 ± 0.09 (70.2 ± 2.0) | 1.98 |
22 | iPr | 6.84 ± 0.14 (69.6 ± 4.3) | 7.29 ± 0.07 (75.6 ± 1.7) | 2.29 |
23 |
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6.27 ± 0.11 (76.5 ± 3.1) | 6.97 ± 0.07 (82.4 ± 1.9) | 1.81 |
24 |
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6.10 ± 0.09 (63.9 ± 2.4) | 7.33 ± 0.09 (74.6 ± 2.1) | 0.53 |
apEC50 values were determined from dose-response curves of induction of IP3 turnover in SUCNR1 transfected HEK cells (N = 3), efficacy is determined relative to succinate (100%). bCalculated by BioByte’s algorithm as implemented in ChemDraw Professional 16.0.1.4 (ClogP option). cDuplication of data from Table 2.