Novel highly potent and orally active ABCB1 modulator capable of overcoming MDR, stabilizing ABCB1 by directly binding to ABCB1, stimulating the activity of ABCB1 ATPase without inhibitory activity against CYP3A4, increasing the sensitivity of SW620/Ad300

Novel potent RET kinase inhibitor with >500-fold selectivity against KDR (Kinase insert Domain Receptor) in cellular assays

Analog of K11777; Irriversible effective cysteine protease inhibitor with trypanocidal activity in cell culture and animal model with comparable efficacy to K11777.

Novel potent inhibitor of Schistosoma mansoni cathepsin B1 (SmCB1) with IC50 ~0.2 nM

Novel potent inhibitor of Schistosoma mansoni cathepsin B1 (SmCB1) with IC50 ~0.6 nM

Potent inhibitor of Plasmodium falciparum dihydrofolate reductase (DHFR)

Novel Dual Inhibitor of Nitric Oxide and Prostaglandin E2 Production

Main active metabolite of tazanolast, inhibiting dose-dependently compound 48/80-induced histamine release from rat peritoneal mast cells

Novel inhibitor of the JAK2/STAT3 pathway

Novel GPR52 agonist, dose-dependently inducing elevation of intracellular cAMP in HEK293/GPR52 cells

Novel dual BRD4 and PLK1 inhibitor (IC 50 values of 109 and 22 nM, respectively), showing strong antiproliferative activity against cancer cells

Novel potent dual inhibitor of Wnt and hedgehog signalings, blocking porcupine and smoothened

Novel Allosteric WNK Kinase Inhibitor

Unique neuroprotectant against oxidative injury, being a highly promising remedy for the treatment of amyotrophic lateral sclerosis (ALS)

Potent uncompetitive NMDA receptor antagonist

Novel GluN2B-specific NMDAR antagonist, completely preventing the decrease in insulin secretion of about 32 % provoked by a 24-h-treatment with NMDA/glycine, eliminating NMDA-induced changes in the oxidation status of the islet cells and elevating the sen

Novel potent dual inhibitor of phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR), preventing PI3K signaling and inhibiting the proliferation of transformed cells with oncogenic PI3K mutant

Novel dual inhibitor of histone deacetylase and topoisomerase I

Natural potent antitumoragent, targeting sarco/endoplasmic reticulum calcium-ATPase (SERCA)2

B2 bradykinin receptor antagonist

Dopamine reuptake inhibitor, also having some SERT affinity

Novel Anti-malarial Plasmodium-Selective Proteasome Inhibitor

Novel fluoroquinolone antibiotic with potent antimicrobial activity, showing the potential to overcome major drug resistance; its antimicrobial activity was less affected by both pump-mediated efflux and QRDR mutations in P. aeruginosa compared with LVX a

Novel inhibitor of type III secretion system ATPase EscN from enteropathogenic Eecherichia coli

Novel very potent and long acting hetrazepinoic PAF-antagonist

Highly conserved neuropeptide derived from Chromogranin A (Parathyroid Secretory Protein 1)

Novel Inhibitor of PBP2, Showing Potent β-Lactam Enhancer Activity against Pseudomonas aeruginosa, Including Multidrug-Resistant Metallo-β-Lactamase-Producing High-Risk Clones

Non-peptide GLP-1 receptor agonist, blocking inflammatory nociception by stimulating β-endorphin release from spinal microglia

Novel inhibitor of The epidermal growth factor receptor (EGFR), decreasing NSCLC cell proliferation and colony formation, by causing G2/M arrest and apoptosis.

Secreted frizzled-related protein-1 (sFRP-1) modulaitor