GNE-616 is a novel, highly potent, metabolically stable, orally bioavailable, and subtype selective Nav1.7 inhibitor with Ki of 0.79 nM and Kd of 0.38 nM for hNav1.7. It has the potential for the treatment of chronic pain. GNE-616 shows >1000 nM Kd and >2500-fold selectivity over hNav1.1, hNav1.3, hNav1.4, and hNav1.5. Selectivity over hNav1.2 and […]

LY3020371 HCl is a novel, potent, selective mGlu2/3 (metabotropic glutamate 2/3) receptor antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM. LY3020371 hydrochloride exerts an antidepressant-like signature in vivo. The novel mGlu2/3 receptor antagonist, LY3020371, has been shown to produce antidepressant-like effects comparable to that of the […]

GS-6207 (CA inhibitor 1) is a novel and potent HIV capsid inhibitor that inhibits HIV virus and has the potential for HIV treatment.

Clovoxamine fumarate (formerly also known as DU 23811) is a potent non-TCA (tricyclic antidepressant) with a dual action in blocking the reuptake of both noradrenaline and serotonin. Clovoxamine has little affinity for muscarinic, histaminergic, serotonergic and adrenergic binding sites. Clovoxamine induces a decrease in the functional beta-adrenergic receptor coupled c-AMP response.

Cobimetinib R-enantiomer is the less active R-enantiomer of Cobimetinib (formerly GDC-0973, RG7420 or XL-518; Cotellic) which is a small-molecule MEK1 inhibitor approved for cancer treatment.

BI-224436, an investigational new drug under development for the treatment of HIV infection, is the first non-catalytic site integrase inhibitor (NCINI) with EC50 values of less than 15 nM against different HIV-1 laboratory strains.. It inhibits HIV replication via binding to a conserved allosteric pocket of the HIV integrase enzyme. This makes the drug distinct […]

ONO8430506(ONO-8430506) is a novel and potent autotaxin inhibitor that enhances the antitumor effect of paclitaxel in a breast cancer model. Lysophosphatidic acid (LPA) is a bioactive lipid mediator that elicits a number of biological functions, including smooth muscle contraction, cell motility, proliferation, and morphological change. LPA is endogenously produced by autotaxin (ATX) from extracellular lysophosphatidylcholine […]

Diflapolin is reported to be the first potent dual soluble epoxide hydrolase (sEH)/5-lipoxygenase-activating protein (FLAP) inhibitor. Whereas 5-LOX (5-lipoxygenase) activating protein facilitates 5-LOX-mediated conversion of arachidonic acid to pro-inflammatory leukotrienes, soluble epoxide hydrolase (sEH) degrades anti-inflammatory epoxyeicosatrienoic acids (EETs). Dual inhibition might therefore offer increased efficacy as an anti-inflammatory intervention compared to single target agents. […]

PI4KIII beta inhibitor 3, extracted from WO 2013034738 A1, is a novel and potent PI4KIIIβ inhibitor with IC50 of 5.7 nM.

SB269652 is a novel and potent drug-like allosteric modulator of the dopamine D2 receptor (D2R). SB269652 acts by binding in a bitopic manner at one protomer of a D2R dimer and modulating the binding of dopamine at a second protomer. SB269652 potently abolished specific binding of [(3)H]nemanopride and [(3)H]spiperone to Chinese hamster ovary-transfected D(3) receptors […]