Novel isocitrate dehydrogenase 2 (IDH2) mutants inhibitor for the treatment of cancer

Novel highly potent substrate-selective inhibitor of insulin-degrading enzyme (IDE), blocking insulin binding while allowing glucagon cleavage, even at saturating inhibitor concentrations

Novel highly potent substrate-selective inhibitor of insulin-degrading enzyme (IDE), blocking insulin binding while allowing glucagon cleavage, even at saturating inhibitor concentrations

M1 and M2 Antagonist

Novel μ,δ-Opioid Receptor Dual-Biased Agonist, Overcoming the Limitation of Prior Biased Agonist

Novel μ,δ-Opioid Receptor Dual-Biased Agonist, Overcoming the Limitation of Prior Biased Agonist

Novel μ,δ-Opioid Receptor Dual-Biased Agonist, Overcoming the Limitation of Prior Biased Agonist

Potent cytotoxin selectively by CYP1A1 as a tumor-selective treatment for human bladder cancers

DNA topoisomerase II inhibitor

Novel inhibitor of heat shock protein 90 (Hsp90), demonstrating anticancer activity against colorectal, osteosarcoma and cervical cancer cell lines

Novel highly selective, substrate-competitive SIRT2 inhibitor, displaying a significant neuroprotective effect in a lactacystin-induced model of Parkinsonian neuronal cell death in the N27 cell line

Novel potent and selective inhibitor of choline kinase alpha (CHKA)

Novel selective bacterial dihydrofolate inhibitor, antibiotic, actively against Gram positive organisms

Antimalarial agent, displaying blood schizonticidal activity against P.berghei

Potent thromboxane receptor antagonist

Novel selective inhibitor of CDK7

Novel inhibitor of CALP, exhibiting affinity of 22.6 ± 8.0 μM for CALP and no interaction with the NHERF PDZ domains

Inhibitor of voltage-gated K(+) (Kv) channels Kv1.3 and Kv1.5

Neuronal Kv7 potassium channel activator

MmpL3 inhibitor, being active against drug-resistant Mycobacterium tuberculosis

Novel HDAC6-selective inhibitor

Novel fluorescent irreversible inhibitor of Bruton's tyrosine kinase (BTK)

Novel Aurora kinase inhibitor, revealing mechanisms of HURP in nucleation of centrosomal and kinetochore microtubules

Novel Aurora kinase inhibitor

First-in-class triple-acting PIM/PI3K/mTOR inhibitor, demonstrating single-agent, anti-tumour efficacy in suppression of pAKT, pmTOR and pBAD in the SKBR-3, BT-474 and HCC-1954 HER2+/PIK3CA-mutated cell lines

Novel activator of LFA-1-ICAM-1 binding

Novel inhibitor of the cluster of differentiation 14 innate immunity pathway

Novel antagonist of IAP (inhibitor of apoptosis protein)

Antibiotic enhancer against resistant Gram-negative bacteria

Antibiotic enhancer against resistant Gram-negative bacteria