Table 1.

Structures and activities for A-ring variants 5a-5e

Cmpd	R=	Synthetic Route	Kir6.2/SUR1 EC50 (μM) [Emax (%)]
5HTS hit		1	1.1a [93]
5a		1	1.8a,c [91]
5b		1	0.46b [82]
5c		1	0.25b [87]
5d		1	0.66b [90]
5e		1	0.78b [87]

^aThallium flux assays with T-REx-HEK293 cells; values represent means from one experiment performed in triplicate. 4 was used as a positive control. 0.48 mM Tl₂SO₄ was used.

^bThallium flux assays with T-REx-HEK293 cells; values represent means from one experiment performed in triplicate. 2 (EC₅₀ = 0.75 ± 0.08 μM) was used as a positive control.

^cValues represent means from two experiments performed in triplicate.