WM-2474, an inactive analog of WM-8014, is used as a negative control compound with an IC50 value of > 125 μM and without affecting cell proliferation.

IMT1B (LDC-203974; IMT-1B) is a novel first-in-class and allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) with the potential for the treatment of cancer. POLRMT is a human mitochondrial RNA polymerase (POLRMT) and is essential for mtDNA transcription as well as biogenesis of the oxidative phosphorylation (OXPHOS) system.

6-Aminochrysene is a novel and potent aromatic amine

Ziresovir (known also as AK-0529; RO-0529) is a selective and orally bioavailable inhibitor of respiratory syncytial virus (RSV) fusion (F) protein (RSV F) protein with EC50 of 3 nM. Ziresovir is currently in phase 2 clinical trials. RO-0529 demonstrates single-digit nM EC50 potency against laboratory strains, as well as clinical isolates of RSV in cellular […]

Cortistatin-14 (CST-14), a recently discovered cyclic neuropeptide with neuronal depressant and sleep modulating properties, can bind to all five cloned somatostatin receptors (SSTRs) and ghrelin receptor to exert its biological activities and co-exists with GABA within the cortex and hippocampus. However, the role of CST-14 in the control of depression processes is not still clarified. […]

PF-06263276 (PF6263276) is a novel, indazole-based, potent and selective pan-JAK inhibitor with anti- inflammatory and immunomodulatory effects. It inhibits JAK1/2/3 and TYK2 with IC50s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM, respectively. It is suitable for inhaled and topical delivery for the treatment of inflammatory diseases of the lungs and skin and […]

Edotecarin (formerly ED-749; J-107088; J 107088; PF 804950) is a novel and potent inhibitor of topoisomerase I that can induces single-strand DNA cleavage with IC50 of 50 nM. The novel indolocarbazole edotecarin differs from other topoisomerase I inhibitors both pharmacokinetically and pharmacodynamically. In vitro, it is more potent than camptothecins and has a variable cytotoxic […]

CP-96486 is a novel, potent and orally bioavailable antagonist of leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor with Kis of 20 and 24 nM, respectively.

SF2312 is a novel, highly potent and low-nanomolar inhibitor of enolase. SF2312 is a phosphonate antibiotic of unknown mode of action produced by the actinomycete Micromonospora, which is active under anaerobic conditions. Despite being crucial for energy generation in most forms of life, few if any microbial antibiotics specifically inhibit glycolysis.

Gosogliptin (formerly also known as PF-734200 and PF-00734200) is a novel, potent and selective inhibitor of dipeptidyl peptidase-IV (DPP-IV). Systemic exposures of PF-734200 increased approximately 1.5-, 2.2-, 2.1- and 2.8-fold in subjects with mild, moderate, or severe renal insufficiency or ESRD, respectively, compared with subjects with normal renal function. The terminal half-life increased from 16.2h […]