MK-8318 is a novel, potent and selective tricyclic tetrahydroquinoline analog that acts as a CRTh2 receptor antagonist with a Ki of 5.0 nM. MK-8318 demonstrates a favorable PK profile suitable for once daily oral dosing for potential treatment of asthma. MK-8318 showed good in vitro and in vivo activity (Ki = 2.3 nM; IC50 cAMP […]

AZD 4407 is a novel, potent and selective 5-lipoxygenase inhibitor. Arachidonate 5-lipoxygenase, also known as ALOX5, 5-lipoxygenase, 5-LOX, or 5-LO, is a non-heme iron-containing enzyme that in humans is encoded by the ALOX5 gene. Arachidonate 5-lipoxygenase is a member of the lipoxygenase family of enzymes.

AZD1979 is a novel and potent antagonist of Melanin-concentrating hormone receptor 1 (MCHr1) with an IC50 of ~12 nM. AZD1979 affects both food intake and energy expenditure. AZD1979 also lowers body weight in a species expressing both MCH receptors holds promise for the use of MCH1 receptor antagonists for the treatment of human obesity. AZD1979 […]

AZD9056 is a novel, potent, selective, orally bioavailable antagonist of P2X7 receptor which is an adenosine triphosphate (ATP)-gated cation channel expressed on a variety of cell types believed to play a role in inflammation. AZD9056 was an inhibitor of BCRP and weakly inhibited BCRP-mediated transport of methotrexate (IC(50)=92μM). Sulfasalazine inhibited methotrexate transport mediated by all […]

BAY-320 is a novel and potent Bub1 inhibitor with an IC50 of 680 nM for human Bub1 in the presence of 2 mM ATP. It demonstrated potent Bub1 kinase inhibition both in vitro and in intact cells. The kinase Bub1 functions in the spindle assembly checkpoint (SAC) and in chromosome congression, but the role of […]

Diroximel fumarate (also known as ALKS 8700) is a novel compound that is taken orally and rapidly converted into monomethyl fumarate (MMF). The compound is being developed by Alkermes in collaboration with Biogen. Diroximel Fumarete essentially is a prodrug of monomethyl fumarate in a controlled-release formulation that rapidly and efficiently converts to MMF in the […]

Irosustat (formerly known as STX64, BN83495 or 667 coumate) is a novel potent and irreversible inhibitor of steroid sulfatase with an IC50 of 8 nM and has the potential for treating breast cancer. The development of potent steroid sulfatase inhibitors is an important new therapeutic strategy for the treatment of postmenopausal women with breast cancer. […]

BAY-598 R-isomer (R-BAY598) is the R-enantiomer of BAY589 which is a peptide-competitive SMYD2 inhibitor with antineoplastic activity.

Fenebrutinib HCl (formerly known RG-7845; GDC-0853 hydrochloride) is an orally bioavailable, and noncovalent (reversible) bruton’s tyrosine kinase (BTK) inhibitor (Ki = 0.91 nM) with anticancer and anti-inflammatory activity. It is in development for the treatment of rheumatoid arthritis and systemic lupus erythematosus. In Sprague-Dawley (SD) rats, administration of GDC-0853 and other structurally diverse BTK inhibitors […]

Emiglitate (also known as BAY o 1248) is a novel, potent, selective and competitive inhibitor of α-glucoside hydrolase. Emiglitate is a deoxynojirimycin derivative that acts as an α-glucosidase inhibitor and a powerful inhibitor of glucose-induced insulin release.