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].

该化合物NNMT-IN-4在5 nM至0.5 μM范围内显示活性，能够有效抑制靶标蛋白。其作用呈剂量依赖性，即随着浓度的增加，抑制效果显著增强。

1.19 NNMT-IN-4在小鼠中的药代动力学性质 [1]。小鼠口服50 mg/kg时，半衰期（T 1/2）为2.89小时，最大血药浓度时间（T max）为0.250小时，最大血药浓度（C max）为22500 ng/mL，AUC last达51115 ng*h/mL，每分钟每千克体重的清除率（CI）为36.1 mL/min/kg，生物利用度（F）为220%。