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SMDC818909 is a potent and selective p97 inhibitor. The IC50 value of SMDC818909 decreased with increasing ATP concentration (26.0 ± 0.9, 11.5 ± 0.9, and 4.9 ± 0.9 μM at 5, 20, and 100 μM ATP, respectively), indicating that it behaved primarily uncompetitively with the ATP substrate. SMDC818909 represents a novel uncompetitive inhibitor with excellent physical and pharmaceutical properties that can be used as a starting point for drug discovery efforts. |
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