Compound class:
Synthetic organic
Comment: This compound is a selective allosteric inhibitor of oncogenic KRASG12C [1].
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Bioactivity Comments |
As the mechanism of action involves irreversible binding, affinity constants cannot be determined for the interaction between ligand and KRAS target. For this reason, Ostrem et al. (2013) [1] used a protein mass spectrometry method to determine the ability of the allosteric inhibitor to modify the mutant RAS protein. Using this method inhibitor 9 gave a readout of 100% modification. |