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Fig. 8 | Journal of Cheminformatics

Fig. 8

From: Data driven polypharmacological drug design for lung cancer: analyses for targeting ALK, MET, and EGFR

Fig. 8

Does methionine as gatekeeper correlate generally with the selectivity properties of EGFR inhibitors? a Stereo plot of the first three PCA dimensions of the protein kinase inhibition data of the Ambit panel of 2011 (Fig. 4), with the protein kinases colored according to gatekeeper (red methionine, gray not methionine). EGFR and mutants are distinguished from the other kinases principally by PC axis 3, while the two gatekeeper mutant (T790M) forms of EGFR are distinguished from the other EGFR forms by PC axis 2. b The inhibitors contributing to the composition of PC axes 2 and 3 (loading plot) highlight the inhibitors that are potent for EGFR and most potent for the T790M mutations (upper left), those that are potent for EGFR but less potent for the T790M mutations (upper right), and inhibitors that are less potent or antiselective for EGFR (lower two quadrants)

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