A potent, selective, and orally active p53-MDM2 antagonist with IC50 of 7 nM.

A potent, selective, and orally active p53-MDM2 antagonist with IC50 of 6 nM.

A potent, selective, and oral renal outer medullary potassium channel (ROMK) inhibitor with IC50 of 68 nM.

A potent, selective, and irreversible inhibitor of SSAO/VAP-1 (AOC3) with Ki of 37 nM, IC50 of <10 nM.

A potent, selective, and irreversible BTK inhibitor with IC50 of 7 nM.

A potent, selective, and centrally active positive allosteric modulator of AMPAR-mediated neurotransmission, which increase ion channel flux in the presence of agonist by suppressing desensitization and/or deactivation of the receptors..

A potent, selective, and bioavailable OX2 receptor antagonist with Kb of 4.5 nM.

A potent, selective, allosteric LMPTP inhibitor with IC50 of 1.68 uM, displays good selective against other phosphatases.

A potent, selective, allosteric CCR2 antagonist with IC50 of 103 nM..

A potent, selective, allosteric CCR2 antagonist with binding IC50 of 5.1 nM.

A potent, selective α2B adrenoceptor antagonist with pKd of 8.8, 200-fold selectivity over α2A, and α2D receptors.

A potent, selective α2A-adrenoceptor antagonist with Ki of 1.7 nM, 80-fold selectivity over α2B-adrenergic receptors.

A potent, selective ubiquitin-specific protease USP8 inhibitor with IC50 of 0.85 uM.

A potent, selective ubiquitin-specific protease USP8 inhibitor with IC50 of 0.56 uM.

A potent, selective TRPM8 agonist with EC50 of 12 uM, a cooling agent.

A potent, selective TRPC6 channel inhibitor with IC50 of 0.1-0.6 uM, 12- and 5-fold selectivity over related TRPC3 and TRPC7.

A potent, selective translocator protein 18 kDa (TSPO/PBR) agonist with IC50 of 2.59 and 1.03 nM in competing with [3H]-PK11195 for binding to membrane preparations from rat cerebral cortex and ovary, respectively.

A potent, selective transcriptional CDK inhibitor with Ki of 2.3 and 0.38 nM for CDK7 and CDK9, respectively.

A potent, selective TLR9 antagonist with IC50 of 13 nM (human TLR9), displays 75-fold selectivity over TLR7 and no activity against TLR8 (IC50>10 uM).

A potent, selective thrombopoietin (TPO) receptor agonist..

A potent, selective TAAR1 agonist with Ki of 1.9, 2.7, 31 and 24 nM for mouse, rat, cynomolgus monkey and human TAAR1 stably expressed in HEK293 cells.

A potent, selective STAT3 SH2 domain inhibitor (EC50=5.6 uM) that reduces STAT3 phosphorylation and nuclear transactivation.

A potent, selective STAT3 inhibitor with IC50 of 9.7 uM, inhibits tyrosine phosphorylation of STAT3 with selectivity over STAT5 and STAT1 in cell-based assays.

A potent, selective STAT3 inhibitor that blocks STAT3 binding to its phosphopeptide ligand (IC50=20 uM) and inhibits IL-6-mediated phosphorylation of STAT3.

A potent, selective Src and Syk kinase inhibitor with IC50 of 29.3 uM and 2.5 uM, respectively.

A potent, selective small molecule Mcl-1 inhibitor that selectively targets the BH3-binding groove of Mcl-1.

A potent, selective sigma-2 receptor agonist with Ki of 3.5 nM, 25-fold selectivity over sigma-1 receptors (Ki=86.6 nM).

A potent, selective sigma-2 receptor agonist with Ki of 16.5 nM, 200-fold selectivity over sigma 1 (Ki=3063 nM).

A potent, selective sigma 1 ligand with Ki of 0.08 nM, >3000-fold selectivity over sigma 2 (Ki=1377 nM).

A potent, selective S1P3 antagonist with Ki of 0.25 nM.