Table 4.
Investigation of ring B.
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---|---|---|---|---|
Ring B | hSUCNR1 | mSUCNR1 | ClogPb | |
pEC50 (efficacy, %)a | ||||
3c |
![]() |
5.75 ± 0.08 (72.8 ± 2.6) | 6.46 ± 0.06 (79.3 ± 1.6) | 1.66 |
25 |
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5.91 ± 0.11 (49.7 ± 3.9) | 5.40 ± 0.13 (58.0 ± 4.5) | 2.27 |
26 |
![]() |
4% @10−4M | 7% @10−4M | 2.27 |
27 |
![]() |
6.03 ± 0.25 (78.2 ± 8.0) | 6.10 ± 0.17 (89.3 ± 6.1) | 2.05 |
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 1.