C82 acts as an inhibitor of Mycobacterium tuberculosis (Mtb) cyclic dinucleotide phosphodiesterase (CdnP), with an IC50 value of 17.5 µM. This particular enzyme is responsible for breaking down cyclic di-AMP (c-di-AMP) into adenosine 5'-monophosphate (AMP). Notably, C82 demonstrates selectivity for Mtb CdnP over other bacterial cyclic dinucleotide phosphodiesterases (CDN PDEs) such as Yybt, RocR, and Group B Streptococcus (GBS) CdnP, as well as the mammalian CDN PDE ENPP1, and the viral CDN PDE poxin, showing effectiveness at a concentration of 200 µM.
NTRC-824 is >150-fold selectivity for NTS2 over NTS1 (Ki >30 μM). NTRC-824 is an effective, selective, and neurotensin-like nonpeptide neurotensin receptor type 2 (NTS2) antagonist (IC50: 38 nM and a Ki : 202 nM).
Melogliptin, also known as EMD-675992 and GRC-8200, is a potent and selective a dipeptidyl peptidase IV (DPP-IV) inhibitor potentially for treatment of type II diabetes. Melogliptin significantly reduced HbA1c from baseline as compared to placebo with a mean average reduction of 0.75 percent in patients receiving 50mg twice daily dose and 0.60 percent in patients receiving 100 mg once daily dose.
c-Kit-IN-2 is a c-KIT inhibitor (IC50: 82 nM), shows superior antiproliferative activities against all the three GIST cell lines, GIST430, GIST882, and GIST48 (GI50s: 1, 3, and 2 nM).