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NNMT-IN-3 (compound 14) is a potent and selective inhibitor of nicotinamide N-methyltransferase (NNMT) with IC50 values of 1.1 nM and 0.4 μM in cell-free and cell-based assays, respectively. nNMT-IN-3 can be used in studies of obesity, cancer, type II diabetes and skeletal sarcopenia, among other diseases.