Table 1.

Investigation of miscellaneous amide analogues.

	R	hSUCNR1	mSUCNR1	ClogPb
		pEC50 (efficacy, %)a
3		5.75 ± 0.08 (72.8 ± 2.6)	6.46 ± 0.06 (79.3 ± 1.6)	1.66
4		4.53 ± 0.13 (78.1 ± 7.5)	4.93 ± 0.05 (95.8 ± 2.9)	0.44
5		22% @10−4M	13% @10−4M	0.28
6		50% @10−4M	64% @10−4M	1.52
7		8% @10−4M	15% @10−4M	1.26
8		5% @10−4M	11% @10−4M	1.28
9		25% @10−4M	15% @10−4M	2.44

^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).