A novel selective small molecule inhibitor of PDE6δ/KRas interaction with Kd of 358 pM..

A novel SAM-competitive, highly selective, orally bioavailable EZH1/2 dual inhibitor with IC50 of 16/50 nM, respectively.

A novel P-selectin inhibitor that directly binds to P-selectin.

A novel potent, subtype-selective sigma 2 receptor/PGRMC1 ligand with Ki of 61 nM, 9-fold selectivity over sigma 1 receptors (Ki=556 nM).

A novel potent, subtype-selective sigma 2 receptor/PGRMC1 ligand with Ki of 16.2 nM, 574-fold selectivity over sigma 1 receptors..

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.

A novel potent, specific, covalent USP7 inhibitor with Kd of 7.8 uM (USP7 catalytic domain).

A novel potent, slow tight binding LPA1 receptor antagonist with IC50 of 86 nM, Kd of 0.34 nM.

A novel potent, selective, reversible cyclooxygenase-1 (COX-1) inhibitor with IC50 of 4.9 nM.

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

A novel potent, selective, orally available PI3Kδ inhibitor with IC50 of 31 nM.

A novel potent, selective, orally available DPP-4 inhibitor with IC50 of 9 nM.

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 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 CBP/p300 bromodomain with IC50 of 1.0 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, 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, cell permeable and ATP competitive LIMK inhibitor.

A novel potent, selective, brain-penetrable and orally active PDE2A inhibitor with IC50 of 1.5 and 4.2 nM for human and rat PDE2A, respectively.

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 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 TRPM8 antagonist with IC50 of 15.6 nM (hTRPM8).

A novel potent, selective TBK1 PROTAC with DC50 of 12 nM, selectively degrades TBK1 with excellent selectivity against a related kinase IKKε.

A novel potent, selective Sirt2 inhibitor with IC50 of 0.118 uM.

A novel potent, selective PDE9A inhibitor with IC50 of 11 nM, >45-fold selectivity over other PDE isoforms.

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.