LY2979165, a novel and potent mGlu2 agonist being developed as an anti-depressant drug candidate, has potential usefulness in the treatment of bipolar disorder. LY2979165 is being developed by Eli Lilly, and is currently in clinical trials.

BI-671800 is a novel, potent and highly specific antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2), with IC50 values of 4.5 nM and 3.7 nM for PGD2 binding to CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively. BI-671800 can be potentially used for the treatment of poorly controlled asthma.

Pergafast is a proprietary color developer for thermal paper. It was developed as an alternative to BPA and phenolic containing color developers. It is used in thermal print paper. Pergafast® 201 is not only an alternative to BPA but is also nonphenolic.

LY2922083 is a novel, potent, selective and orally bioavailable GPR40 (G protein-coupled receptor 40) agonist. It has the potential for the treatment of type 2 diabetes mellitus. LY2922083 demonstrated potent, efficacious and durable dose dependent reductions in glucose levels along with significant increases in insulin and GLP-1 secretion during preclinical testing. The G protein-coupled receptor […]

Trovirdine HCl (LY-300046 and PETT-1) is a novel and potent reverse transcriptase inhibitor (RTI) that inhibits HIV-1 RT with an IC50 of 7 nM when employing heteropolymeric primer/template (oligo-DNA/ribosomal RNA)and dGTP as substrate. Trovirdine can be potentially used for the treatment of HIV infection. Trovirdine inhibited HIV-1 RT with an IC50 of 0.007 microM when […]

Rilapladib (formerly aslo known as SB-659032 and GTPL-7376) is a novel, potent and selective lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with an IC50 of 230 pM, also a PAFR (Platelet Activating Factor Receptor) antagonist.

GW-274150 is a novel, potent, arginine-competitive,highly selective, NADPH-dependent, and long-acting inhibitor of inducible nitric oxide synthase (iNOS) activity in rat and mouse models of renal I/R. GW274150 was identified from a series of acetamide amino acids that have a high selectivity for iNOS vs both eNOS (> 260-fold) and nNOS (> 219-fold) and high bioavailability […]

NSC16168 is a novel, potent and specific inhibitor of ERCC1-XPF with an IC50 value of 0.42 μM. NSC16168 inhibits DNA repair and potentiates CDDP efficacy in cancer.

GNE-049 is a novel, highly potent and selective CBP/p300 bromodomain inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively. Inhibition of the bromodomain of the transcriptional regulator CBP/P300 is an especially interesting new therapeutic approach in oncology. It was […]

NSC232003 is a novel, highly potent and cell-permeable UHRF1 inhibitor, which inhibits DNA methylation in vitro and disrupts DNMT1/UHRF1 interactions at a cellular level. Compound NSC232003, a uracil derivative freely available by the NCI/DTP Repository, provides a versatile lead for developing highly potent and cell-permeable UHRF1 inhibitors that will enable dissection of DNA methylation inheritance.