A novel potent, allosteric, orally available muscle glycogen synthase 1 (GYS1) activator with EC50 of 5.2 uM.

A novel potent ULK1 inhibitor with IC50 of 11 nM..

A novel potent TOPK inhibitor that effectively suppresses SUV-induced activation of MAPKs signal transduction resulting in reduced SUV-induced skin carcinogenesis.

A novel potent specific histone acetyltransferaseTip60 inhibitor.

A novel potent specific histone acetyltransferaseTip60 inhibitor.

A novel potent soluble guanylate cyclase (sGC) activator.

A novel potent small-molecule BET bromodomain (BRD) inhibitor that binds to BET proteins with Ki values of <1 nM.

A novel potent proton pump inhibitor that irreversibly inhibits H+,K+-ATPase activity with IC50 of 0.28 uM.

A novel potent MAP3K14 kinase inhibitor with IC50 of 1.8 nM (NIK autophosphorylation).

A novel potent LIMK inhibitor with IC50 of 8 nM and 32 nM for LIMK1 and LIMK2, respectively.

A novel potent LIMK inhibitor with IC50 of 0.3 nM and 1 nM for LIMK1 and LIMK2, respectively.

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

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.