A novel potent gonadotrophin releasing hormone (GnRH) antagonist..

A novel potent DNA-intercalating payload dimer (PBD dimer) payload for antibody-drug conjugates (ADCs).

A novel potent CFTR potentiator with Kd of 31.7 nM.

A novel potent CFTR potentiator that blocks hCFTR with apparent Kd of 71.3 uM.

A novel potent CDK inhibitor with IC50 of 79 nM, 63 nM and 20 nM for Cdk4/cyclin D1, Cdk1/cyclin B and Cdk9/cyclin T1, respectively.

A novel potent cdc2-like kinase (CLKs) and DYRKs inhibitor with IC50 of 40, 35 and 15 nM for DYRK1A, DYRK2 and CLK1, respectively.

A novel potent cannabinoid receptor agonist..

A novel potent bitter receptor (TAS2Rs) antagonist that inhibits activation of hTAS2R31 by saccharin and acesulfame K with IC50 of 6.4 and 7.9 uM respectively.

A novel potent Aurora kinase inhibitor that inhibits Aurora-A and Aurora-B with IC50 of 24 nM and 45 nM, respectively.

A novel potent and selective, orally active URAT1 inhibitor with Ki of 57 nM, 130 and 42-fold selectivity over OAT1 and OAT3, respectively.

A novel potent and selective agonist of GPR84 that induces calcium response with EC50 of 0.213 uM.

A novel potent (IC50=910 ng/mL), highly selective microsomal prostaglandin E synthase 1 inhibitor (mPGES-1) for treatment of undisclosed indications..

A novel potent "funny" If current channel (If channel) inhibitor that inhibits rOct1- and hOCT1-mediated [3H]MPP uptake with IC50 of 23.8 and 40.5 uM, respectively.

A novel peptidic, potent and highly selective CXCR4 antagonist with IC50 of 1.7 nM.

A novel orally bioavailable fungal beta-1,3-D glucan synthetase inhibitor against Candida species C. glabrata (MIC 0.03 to 0.25 ug/ml), C. parapsilosis (MIC 0.06 to 0.25 ug/ml).

A novel orally available, synthetic retinoid with potential antineoplastic and chemopreventive activities.

A novel orally active, anti-inflammatory compound that inhibits leukocyte infiltration and changes in lung function in response to allergen challenge.

A novel Notch inhibitor that reduces protein expression of NOTCH1, NICD and HES1 in HEK293 cells and downregulates Notch target genes.

A novel nonpeptidic inhibitor of 14-3-3 protein-protein interaction that promotes the apoptotic death of cells expressing either wt Bcr-Abl construct or T315I mutation.

A novel Non-competitive AMPA/kainate antagonist.

A novel negative allosteric modulator of dofetilide binding to the Kv11.1 (hERG) channel with the strongest effect at 10 uM (IC50=3.9 uM).

A novel MPT (mitochondrial permeability transition) inhibitor of that inhibits Ca2+-induced MPT in rat liver isolated mitochondria.

A novel mitochondrial and mTOR inhibitor with potent anti-cancer activity, inhibits leukemia cell lines with IC50 of 70-260 nM.

A novel mineralocorticoid receptor antagonist (IC50=0.26 uM) with carbonic anhydrase inhibitory activity (IC50=19 uM).

A novel microtubule targeting agent that induces apoptosis, upregulates death receptors, and potentiates TRAIL-mediated apoptosis in multiple cancer cells.

A novel microtubule inhibitor, downregulates T315I mutant Bcr-Abl and induces apoptosis of imatinib-resistant chronic myeloid leukemia cells.

A novel melatonin melatonin receptor MT1/MT2 and serotonin 5-HT1A/5-HT1D receptor agonist.

A novel lysosomotropic REV-ERB ligand that has a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy.

A novel isocitrate lyase (ICL) inhibitor that displays showed excellent anti-Mycobacterium tuberculosisl activities and low cytotoxicity.

A novel hypoxia-sensitive fluorescent probe.