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 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 monoamine oxidase B (MAO-B) inhibitor with IC50 of 29-56 nM.

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

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

A novel potent, selective TRPM8 antagonist with IC50 of 15.6 nM (hTRPM8).

A novel potent, selective TRPM8 channel antagonist with IC50 of 10 and 21 nM in hTRPM8 HEK293 cells activated by Cooling Agent 10 or cold.

A novel potent, selective Y4R positive allosteric modulator (EC50=5.1 uM) that potentiates Y4R activation in G-protein signaling and arrestin3 recruitment experiments.

A novel potent, selective, allosteric and orally active dopamine D1 receptor potentiator with Kb of 26 nM.

A novel potent, selective, cell permeable and ATP competitive LIMK inhibitor.

A novel potent, selective, competitive and orally active DPP4 inhibitor with potential for the treatment of type 2 diabetes.

A novel potent, selective, oral PIKfyve inhibitor that selectively decreases c-Rel binding to gene promoters of IL-12p40 and IL-1β, regulates cytokine production through PIKfyve-c-Rel pathway ( IL-12p40 IC50=2 nM).

A novel potent, selective, orally active aldosterone synthase inhibitor with IC50 of 2 nM, displays 150-fold selectivity over related cortisol synthase.

A novel potent, selective, orally active nociceptin/orphanin FQ peptide (NOP, ORL1) receptor agonist with Ki of 4.6 nM, with high selectiivity over classical opioid receptors.

A novel potent, selective, orally active translocator protein 18 kDa (TSPO/PBR) antagonist with Ki of 0.33-9.3 nM for both rat and human TSPO.

A novel potent, selective, orally bioavailable and brain-penetran α7nAChR positive allosteric modulator with EC50 of 60 nM.

A novel potent, selective, orally bioavailable inhibitor of voltage-gated potassium channel KCNH3 with IC50 of 9.0 nM.

Balixafortide(POL 6326) is a novel potent, selective, peptidic CXCR4 antagonist that interferes with the tumor-protective microenvironment and sensitizes tumor cells to chemotherapy.

A novel potent, specific TOPK inhibitor that has no effect on ERK1, JNK1, or p38 kinase activity.

A novel potent, specific, orally available GPR40 agonist that influences glucose-dependent insulin secretion both in vitro pancreas β-cell-derived cells and in vivo.