BIIB068 (BIIB-068) is a novel reversible and orally bioavailable BTK inhibitor with the potential to be used for autoimmune diseases such as systemic lupus erythematosus (SLE). It demonstrated good kinome selectivity with good overall drug-like properties for oral dosing, was well tolerated across preclinical species at pharmacologically relevant doses with good ADME properties, and achieved […]

BC-DXI-843 is a potent and specific AIMP2-DX2 inhibitor with an IC50 of 0.92 μM, more than 100-fold selectivity over AIMP2 (IC50 >100 μM) in a luciferase assay. BC-DXI-843 acts as a promising lead targeting AIMP2-DX2 in lung cancer.

Sufugolix (formerly known as TAK-013) is a novel, highly potent, non-peptide, selective and orally bioavailable luteinizing hormone-releasing hormone (LHRH) receptor antagonist with anticancer activity. It inhibits LHRH with an IC50 of 0.1 nM. Sufugolix was under development for the treatment of endometriosis and uterine leiomyoma and reached phase II clinical trials for both of these […]

Alendronate sodium hydrate, the sodium salt of alendronate, is a novel and potent farnesyl diphosphate synthase inhibitor with IC50 of 460 nM. Alendronate sodium is a second generation bisphosphonate and synthetic analog of pyrophosphate with bone anti-resorption activity. Alendronate sodium binds to and inhibits the activity of geranyltranstransferase (farnesyl pyrophosphate synthetase), an enzyme involved in […]

Ro 10-5824 is a novel, potent and selective partial agonist of dopamine D4 receptor with Ki of 5.2 nM. RO10-5824 has the potential for the treatment of cocaine use disorders. The identification of effective medications for the management of cocaine use disorders remains an unmet public health challenge. In view of the prominent role of […]

TP-2857 is novel and potent antimicrobial compound.

NSC139021 (also known as ERGi-USU) is a novel, potent and highly selective inhibitor for the growth of ERG-positive cancer cells with IC50s ranging from 30 to 400 nM.

Teixobactin, a naturally occuring antibiotic discovered in a screen of uncultured bacteria, is a novel peptide-like secondary metabolite of some species of bacteria, that kills some gram-positive bacteria, and has the the potential to overcome drug resistance. It appears to belong to a new class of antibiotics, and harms bacteria by binding to lipid II […]

Zotiraciclib (SB1317; TG02) HCl, the hydrochloride salt of SB1317, is a novel and potent small molecule inhibitor of CDK2, JAK2, and FLT3 with the potential for the treatment of cancer. It inhibits CDK2, JAK2 and FLT3 with IC50s of 13, 73, and 56 nM, respectively.

Apomorphine HCl (APL-130277; TAK-251) is a novel and potent dopamine D2 agonist used for the treatment of Parkinson’s disease. Apomorphine also promotes intraneuronal amyloid-β (Aβ) degradation and improves memory function in an Alzheimer’s disease model. Protein levels of two types of serine-phosphorylated insulin receptor substrate-1 (IRS-1), pS616 and pS636/639, significantly decreased following Apomorphine treatment in […]