NNMT-IN-4 (compound 38) is a selective, uncompetitive inhibitor of nicotinamide N-methyltransferase (NNMT) with in vitro biochemical and cell-based assay IC50 values of 42 nM and 38 nM, respectively. It demonstrates favorable pharmacokinetics/pharmacodynamics (PK/PD) and safety profiles, excellent oral bioavailability, and promising pharmaceutical properties. NNMT-IN-4 serves as an in vivo chemical probe for NNMT [1].

NNMT-IN-4 exhibits its bioactivity within the range of 5 nM to 0.5 µM, effectively inhibiting its target with high specificity. This compound demonstrates a robust response in biochemical assays, maintaining efficacy across the indicated concentration spectrum.

The pharmacokinetic profile of NNMT-IN-4 in mice, as indicated by reference [1], demonstrates that when administered orally at a dose of 50 mg/kg, the compound has a half-life (T 1/2) of 2.89 hours and reaches its maximum concentration (C max) of 22,500 ng/mL in 0.25 hours (T max). The area under the curve to the last measurable concentration (AUC last) is reported as 51,115 ng*h/mL. Intravenously administered at 1 mg/kg, NNMT-IN-4 exhibits a clearance (CI) rate of 36.1 mL/min/kg, with a bioavailability (F) of 220%.