Description |
A quinazolinamine compound that acts as a highly potent inhibitor against G9a (IC 50 = 43 and 57 nM by SAHH production determination/ECSD and substrate lysine methylation detection/CLOT, respectively) and GLP (IC 50 = 50 and 58 nM by ECSD and CLOT, respectively) histone H3K9 methyltransferase activity, while affecting muscarinic M 2 receptor and histamine H 1 receptor only at much higher concentrations (by 82% and 31%, respectively, at 1 µM) and exhibiting little activity against SET7/9, SET8/PreSET7, PRMT3, JMJD2E (IC 50 >40 µM), or a panel of 30 GPCR, ion channels, and transporters (<20% inhibition at 1 µM)
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