Novel Protein Kinase C-iota (PKC-ι) Inhibitor, Binding Post-kinase Domain Residues

Potent ligand to target the Y220C pocket, stabilizing Y220C

Inhibitor of topoisomerase II, intercalating into DNA and inducing topoisomerase II-mediated DNA strand crosslinks, resulting in inhibition of DNA replication and tumor cell cytotoxicity

Inhibitor of the acetylcholinesterase activity from bovine erythrocytes and electric eel

NSAID with better gastrointestinal (GI) tolerability

Natural nitric oxide (NO) production inhibitor

Novel potent in vitro and in vivo antifungal agent against azole-resistant Candida albicans

Antifungal antibiotic, showing inhibitory activity against fungi and yeasts, especially against Trichophyton

Antipsychotic prodrug, most notably used for schizophrenia

Inhibitor of PIP 4 Ks, efficiently killing transformed BJ cells, but not normal counterparts, displaying a strong selective lethality against Ras-activated or Ras-transformed cells

Antipsychotic agent

Novel potent PIM inhibitor

Potent, highly selective, and orally bioavailable inhibitor of PIM-1 kinases

Natural activator of cryptic biosynthetic gene clusters (BGC), also acting as a potent inhibitor of monoamine oxidase B

Novel PI3K inhibitor, displaying potent preclinical activity against multiple myeloma

Prodrug of GABA, used for treatment of neurogenic bladder in spinal and benign prostatic hyperplasia

Potent and selective beta2-adrenoceptor agonist

Novel Subtype-Selective PPARbeta/delta Agonist

Selective 5-HT4 receptor antagonist

Novel PI3K inhibitor, synergizing with sorafenib in non-small cell lung cancer cells involving the Akt-S6 signaling.

Novel potent PI3K inhibitor with a modified omipalisib structure

Highly potent ATP-competitive PI3Kdelta/Vps34 dual inhibitor

Novel Inhibitor of the PI3K-Akt Pathway, Inducing Autophagy of Female Germline Stem Cells

Novel inhibitor of the PI3K/Akt/mTOR signaling pathways, activating P53 and inducing apoptosis

Novel Tau ligand, displaying high Tau binding, low MAO-A binding, high brain uptake, and fast and complete brain washout

Platelet aggregation inhibitor

Platelet aggregation inhibitor

Natural inhibitor of Wnt signaling, modulating β-catenin-dependent transcription

Natural cytotoxic withanolide antitumor agent, inducing apoptosis by decreasing mitochondrial membrane potential and elevating the Bax/Bcl-2 protein expression ratio

Natural flavonoidal alkaloid from the sea-grass Phyllosphadix iwatensis