Fig. 1: Data for compounds discussed in the manuscript.
From: Metabolism-driven in vitro/in vivo disconnect of an oral ERɑ VHL-PROTAC
a Redesign of AZD9496 to VHL-PROTACs. Linker length is measured from the oxygen of the phenyl ether to the carbonyl of the amide. # Maximum level of degradation observed for the compound where 0% is vehicle control and 100% is maximal concentration observed for fulvestrant. Data presented is the mean across replicates with standard deviation noted as the ± value. Numerical values in brackets are the number of replicates. ND not determined. muHeps mouse hepatocytes. b Approximate ternary complex of estrogen receptor, PROTAC, and VHL; snapshot from molecular dynamics (see Supplementary Note for details).
