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Orthogonal inhibition of two Eph kinases in cells afforded by the bump-hole and Ele-Cys approaches. (A) 1 at 300 nM only inhibited EphB1G703C, while 3MB-PP1 (3MB) at 100 nM only inhibited EphB1T697G when they were tested on three EphB1 alleles in cells. (B) 1 and 3MB afford orthogonal inhibition of EphB3WT and EphB1T697G in the same cell. The top band in both total Eph and phospho-Eph blots is BRIL-fused EphB3 and the bottom one is EphB1.
