Figure 4.
(A) Chemical optimization plan for 16, a two-dimensional library. (B) 8 × 7 member library design that generated 56 analogues of 16. (C) Structure of 17 (CID85285667), the most potent analogue with an IC50 of 1.1 μM in the Ca2+ fluorescence assay. (D) Cav3.2 IonWorks Quattro (patch EP) CRC IC50 = 13.5 μM. (E) Cav3.3 IonWorks Quattro (patch EP) CRC IC50 = 11.5 μM.