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. 2018 Jul 3;8:10010. doi: 10.1038/s41598-018-28263-7

Table 5.

Combined analogues.

graphic file with name 41598_2018_28263_Figac_HTML.gif
Ring A Ring B hSUCNR1 mSUCNR1 ClogPb
pEC50 (efficacy, %)a
28 graphic file with name 41598_2018_28263_Figad_HTML.gif graphic file with name 41598_2018_28263_Figaj_HTML.gif 6.79 ± 0.12 (58.0 ± 2.7) 5.92 ± 0.09 (64.0 ± 2.5) 2.01
29 graphic file with name 41598_2018_28263_Figae_HTML.gif graphic file with name 41598_2018_28263_Figak_HTML.gif 6.85 ± 0.19 (52.6 ± 3.9) 6.74 ± 0.13 (71.2 ± 3.2) 1.07
30 graphic file with name 41598_2018_28263_Figaf_HTML.gif graphic file with name 41598_2018_28263_Figal_HTML.gif 7.23 ± 0.14 (49.2 ± 2.7) 5.84 ± 0.16 (45.3 ± 3.4) 3.11
31 graphic file with name 41598_2018_28263_Figag_HTML.gif graphic file with name 41598_2018_28263_Figam_HTML.gif 7.64 ± 0.13 (61.7 ± 2.5) 6.75 ± 0.09 (69.9 ± 2.2) 2.18
32 graphic file with name 41598_2018_28263_Figah_HTML.gif graphic file with name 41598_2018_28263_Figan_HTML.gif 7.23 ± 0.23 (88.7 ± 6.1) 7.00 ± 0.09 (68.1 ± 2.5) 1.86
33 graphic file with name 41598_2018_28263_Figai_HTML.gif graphic file with name 41598_2018_28263_Figao_HTML.gif 7.23 ± 0.37 (66.4 ± 7.2) 7.29 ± 0.18 (61.5 ± 3.8) 2.13

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).