A novel potent small-molecule BET bromodomain (BRD) inhibitor that binds to BET proteins with Ki values of <1 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, allosteric, simultaneously direct activator and inhibitor of AMPK complexes containing the β1 or β2 isoform, respectively.

A novel potent, and selective prostaglandin EP4 receptor antagonist with binding IC50 of 2.4 nM.

A novel potent, combined serotonin 5-HT1A and 5-HT1B receptor antagonist with Ki of 0.13 and 2.4 nM in brain homogenates, respectively.

A novel potent, competitive squalene synthase inhibitor that upregulate the LDLR in mouse and human liver cell lines with EC50 of 26 nM.

A novel potent, highly selective fatty acid amide hydrolase (FAAH) inhibitor with IC50 of 0.99, 1.65 and 57.3 nM for human FAAH-1, FAAH-1 (P129T) and FAAH-2, respectively.

A novel potent, highly selective, ATP-competitive IKK-2 inhibitor with IC50 of 40 nM, 350-fold selectivity over IKK-1.

A novel potent, in vivo-active BCL6 inhibitor with IC50 of 0.1 uM in ELISA assays.

A novel potent, irreversible and orally active inhibitor of steroid sulfatase (STS) with IC50 of 13 nM in ZR-75-1 cells.

A novel potent, irreversible Myeloperoxidase (MPO) inhibitor with IC50 of 44 nM.

A novel potent, irreversible, T790M mutant-selective inhibitor of mutant EGFR with IC50 of 6.2, 3.4 and 4.2 nM for L858R-T790M, T790M and Del19-T790M, respectively.

A novel potent, irreversible, T790M mutant-selective inhibitor of mutant EGFR with IC50 of 8.3, 4.2 and 4.3 nM for L858R-T790M, T790M and Del19-T790M, respectively.

A novel potent, orally active CCK-2/gastrin receptor antagonist with Ki of 0.47 nM.

A novel potent, orally active, dual-acting aromatase and steroid sulfatase (STS) inhibitor with ICI0 of 0.82 nM and 39 nM, respectively.

A novel potent, partial LXRβ-selective agonist (EC50=9 nM) with 20% LXRα and 88% LXRβ activity compared to a full pan agonist in transactivation assays.

A novel potent, selective and orally active enterocytic microsomal triglyceride transfer protein (MTP) inhibitor that inhibits only MTP localized to enterocytes with IC50 of 6 nM.

A novel potent, selective cannabinoid receptor 2 (CB2) agonist with Ki of 12 nM, >30-fold selectivity over CB1.

A novel potent, selective CDK8 inhibitor with IC50 of 0.5 uM against recombinant Cyclin C/CDK8 complex.

A novel potent, selective hERG potassium channel (Kv11.1) activator that induces a leftward shift in the voltage dependence of activation..

A novel potent, selective inhibitor of phosphorylation and transcriptional activity of STAT5, but not STAT3, AKT, or Erk1/2 phosphorylation.

A novel potent, selective KCNQ2/Q3 (Kv7.2/Kv7.3) potassium channel opener/activator with EC50 of 0.38 uM..