Novel full H1 agonist

Novel Rho-associated coiled coil-formed protein kinase (ROCK) inhibitor, exerting strong intraocular pressure (IOP)-lowering effects into the eyes of monkeys

Novel Rho-associated coiled coil-formed protein kinase (ROCK) inhibitor, exerting strong intraocular pressure (IOP)-lowering effects into the eyes of monkeys

Novel bacterial DNA gyrase inhibitor, exhibiting antimicrobial activity and inhibiting bacterial cell division

AMPA antagonist

GX-936 analog, antagonist of voltage-gated sodium 1.7 (Nav1.7) channels

Novel potent inhibitor of NaV1.7 and highly selective against NaV1.5, having limited selectivity against NaV1.1 and NaV1.2

Novel inhibitor of Nav1.7

Novel modulator of NF-Y transcription, inhibiting the binding of NF-Y to DNA, blocking cellular proliferation and cell cycle progression, interacting with a variety of CCAAT-containing promoters leading to p53-independent cell cycle arrest

Novel NAD+-competitive Sirt2 inhibitor

Novel polo-like kinase (PLK1) inhibitor

Novel potent and selective inhibitor of the cytochrome bc1 complex of mitochondrial electron transport in P. falciparum

Novel inhibitor of mitosis and cytokinesis in T. brucei which causes human African trypanosomiasis (HAT)

Novel Inhibitor of GSK3beta

Potent GSK-3 inhibitor, highly selective over CDK-2

Novel and potent inhibitor of VEGFR2 tyrosine kinase, non-selectivey inhibiting AURKA and AURKB

Potent and selective inhibitor of glycogen synthase kinase 3 (GSK3)

Selective agonist of peroxisome proliferator-activated receptor-γ (PPARγ)

Selective cyclin dependent kinase inhibitor; Inhibitor of Yes1 kinase; Inhibitor of binding or entry into cells for Lassa Virus

Novel inhibitor of firefly luciferase derived from Photinus pyralis (FLuc), the most widely used luciferase

Novel inhibitor of EGFR

Potent inhibitor of PfDHODH, showing greater than 4,000-fold selectivity for the malarial enzyme

Novel VEGFR inhibitor, also a moderate inhibitor of BET proteins with an IC 50 value of 4.6 μM for BRD4(1)

Inhibitor of Mer Kinase, also inhibiting EGFR

Orally active, nonsteroidal tamoxifen derivative and a ligand for the estrogen receptors (ERs), steroid receptor members of the nuclear receptor superfamily of transcription factors

Novel agonist at the adenosine A1 receptor

Potent TrkA kinase inhibitor

Novel potent RET kinase inhibitor

Potent and selective full agonist for peroixisome proliferator-activated receptor-alpha

Novel selective and soluble inhibitor of tumor necrosis factor-alpha converting enzyme (TACE)