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Developing selective type II kinase inhibitors. (A) Docking imatinib into the X-ray co-crystal structure of DDR1. (B) Chemical structure of DDR1-IN-1/2 and representative developing rationale. (C) DDR1-IN-1 efficacy on blocking DDR1 autophosphorylation. (D) DDR1-IN-2 efficacy on blocking DDR1 autophosphorylation. (E) KinomeScanTreeSpot description of the DDR1-IN-1/2 selectivity profile.
