NOD-IN-1 is a potent mixed inhibitor of nucleotide-binding oligomerization domain (NOD)-like receptors, NOD1 and NOD2, with IC50 of 5.74 μM and 6.45 μM, respectively.
NOD-IN-1 (compound 4) is potent mixed inhibitor of NOD1 and NOD2, displaying a balanced inhibitory activity on both targets in the low micromolar range. NOD-IN-1 (IC50 (NOD1)=5.74 μM; IC50 (NOD2)=6.45 μM) is identified as the best of the series, possessing NOD1- and NOD2-inhibitory activities in the lower micromolar range. These results show that NOD-IN-1 is 7-fold less potent than Noditinib-1 in terms of NOD1 inhibition and completely devoid of selective activity for NOD1 or NOD2 as opposed to Noditinib-1. NOD-IN-1 exhibits balanced dual activities of less than 10 μM on the two targets[1].
[1]. Kecek Plesec K, et al. Identification of indole scaffold-based dual inhibitors of NOD1 and NOD2. Bioorg Med Chem. 2016 Nov 1;24(21):5221-5234.