Table 4 Investigation of ring B.

From: Structure-Activity Investigations and Optimisations of Non-metabolite Agonists for the Succinate Receptor 1

 

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

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

  1. 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.
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