A novel potent, selective IRAK4 inhibitor with IC50 of 51 nM.

A novel potent, selective HIV non-nucleoside reverse transcriptase inhibitor (NNRTI) with EC50 of 1, 1.3, 2.8 and 11 nM for WT, K103N, Y181C and K103N/Y181C, respectively.

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 CXCR2 inhibitor with IC50 of 7.6 nM.

A novel potent, selective CXCR2 inhibitor with IC50 of 0.4 nM.

A novel potent, selective CHK1 inhibitor 2 nM, >80-fold selectivity over CHK2.

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

A novel potent, selective and reversible dual inhibitor of G9a/DNMTs with IC50 of 16 nM and 32 nM for G9a and DNMT1, respectively.

A novel potent, selective and orally active ASK1 (MAP3K5) inhibitor with pIC50 of 8.3.

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, pan-AMPK activator with similar potency for all AMPK heterotrimers.

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, orally active proton pump inhibitor that irreversibly inhibits H+,K+-ATPase activity with IC50 of 0.28 uM.

A novel potent, orally active HIF prolyl hydroxylase (PHD) inhibitor with IC50 of 0.22 uM for PHD2.

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

A novel potent, orally active 3-phosphoinositide-dependent kinase-1 (PDK-1) with IC50 of 2 uM.

A novel potent, non-agonist PPARγ ligand that blocks CDK5-mediated PPARγ phosphorylation, without the classical agonism.

A novel potent, multikinase inhibitor with IC50 of 10, 7.6 and 25 nM for c-Kit, RET and PDGFRβ, respectively.

A novel potent, multikinase inhibitor with IC50 of 10, 7.6 and 25 nM for c-Kit, RET and PDGFRβ, 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, 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 and orally active inhibitor of steroid sulfatase (STS) with IC50 of 13 nM in ZR-75-1 cells.

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

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

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, competitive squalene synthase inhibitor that upregulate the LDLR in mouse and human liver cell lines with EC50 of 26 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, and selective prostaglandin EP4 receptor antagonist with binding IC50 of 2.4 nM.

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

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