Extended Data Fig. 4: Optimization toward better drug-like properties.
From: Complex-specific inhibitors for interrogating ATAC histone acetyltransferase complex
a, IC50 determination of LS-160 and LS-161. n = 2 independently biological replicates. b, IC50 determination of LS-162 and LS-163. n = 2 independently biological replicates. c, Chemical structure of compound LS-164 to LS-170 which contains the F derivatives and N-methylated Ala as well as C-terminal piperidine. d, e, The anticancer ability of the indicated compounds was assessed using ATP-monitoring luminescence assay. The luminescence ATP detection system shows the survival rate (%) in A549 (d) and H1299 (e) after the indicated treatment (mean ± s.d., n = 9 including 3 biological replicates and 3 technical replicates). f, PAMPA (Parallel artificial membrane permeability assay) analysis of the inhibitors. Pe: permeability rate. High, medium, and low are compounds provided by the manufacturer with high, medium, and low permeability rates, respectively. (mean ± s.d., n = 4 biological replicates).
