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It was identified through a medicinal chemistry programme at the University of Texas Health Science Center as the lead NNMT inhibitor candidate among a series of 1-methylquinolinium analogues bearing primary amine substitutions, selected for its combination of high passive membrane permeability (confirmed in PAMPA assays), high active transport membrane permeability (confirmed in bidirectional Caco-2 cell assays), potent NNMT inhibitory activity, and high selectivity including confirmed absence of inhibitory effects on related SAM-dependent methyltransferases or enzymes in the NAD+ salvage pathway

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10.1007/s00592-020-01657-8 11 ChenZ.RadjabzadehD.ChenL.KurilshikovA.KavousiM.AhmadizarF.et al (2021)

Gefitinib enhances arsenic trioxide (AS 2 O 3 )-induced differentiation of acute promyelocytic leukemia cell line