Table 2 Investigation of ring A.

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

 

Ring A

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

10

5.29 ± 0.19 (81.6 ± 8.4)

6.16 ± 0.11 (81.3 ± 3.6)

1.47

11

5.27 ± 0.18 (94.7 ± 8.7)

6.13 ± 0.10 (76.7 ± 3.1)

1.67

12

5.02 ± 0.10 (91.9 ± 5.3)

6.07 ± 0.09 (81.6 ± 3.0)

1.97

13

6.33 ± 0.14 (69.1 ± 3.9)

6.83 ± 0.11 (73.2 ± 2.7)

1.97

14

View full size image

4.81 ± 0.20 (74.2 ± 11.8)

5.71 ± 0.09 (79.6 ± 3.7)

0.43

15

6.13 ± 0.14 (71.1 ± 4.2)

6.82 ± 0.08 (74.8 ± 2.0)

0.87

16

5.29 ± 0.15 (103.8 ± 7.9)

6.14 ± 0.10 (78.1 ± 3.1)

0.89

17

6.41 ± 0.14 (85.3 ± 4.5)

7.39 ± 0.07 (84.2 ± 1.8)

1.45

18

6.55 ± 0.25 (81.0 ± 7.2)

6.81 ± 0.17 (80.6 ± 4.6)

2.43

19

6.39 ± 0.11 (72.1 ± 3.2)

6.79 ± 0.06 (76.0 ± 1.5)

1.00

  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.
Back to article page