A novel potent, selective PDE5 inhibitor with IC50 of 0.056 nM for PDE5A1.

A novel potent, selective PDE1 inhibitor with IC50 of 13/45/1.4 nM for PDE1A/B/C, respectively.

A novel potent, selective orally bioavailable MET tyrosine kinase inhibitor with IC50 of <1 nM and 12 nM for unphosphorylated and phosphorylaed MET, respectively.

A novel potent, selective Nrf2 activator with pEC50 of 7.7 (inducing of NQO1 specific enzyme activity).

A novel potent, selective mTOR inhibitor with biochemical IC50 of 21.7 nM for mTORC1, exhibits cellular potency against mTOR with IC50 of 5 nM.

A novel potent, selective monoamine oxidase B (MAO-B) inhibitor with IC50 of 29-56 nM.

A novel potent, selective mGluR2 positive allosteric modulator with EC50 of 199 and 206 nM for human and rat mGlu2, respectively, without exerting agonist activity.

A novel potent, selective Mcl-1 inhibitor with IC50 of <3 nM in FRET assays.

A novel potent, selective Kv2 channel inhibitor that potently inhibits Kv2.1 and Kv2.2 with IC50 of 0.14 and 0.09 uM, respectively.

A novel potent, selective Kv2 channel inhibitor that potently inhibits Kv2.1 and Kv2.2 with IC50 of 0.14 and 0.09 uM, respectively.

A novel potent, selective Kv2 channel inhibitor that potently inhibits Kv2.1 and Kv2.2 with IC50 of 0.14 and 0.09 uM, respectively.

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.