A potent gucokinase (GK) activator with EC50 of 0.29 uM.

A potent glucagon receptor (GCGR) negative allosteric modulator..

A potent GIRK2 inhibitor that inhibits GIRK2-mediated flux with an IC50 of 0.35 uM.

A potent G2 checkpoint inhibitor that specifically abrogates the DNA double-stranded break (DSB)-induced G2 checkpoint.

A potent dual H3/H2 receptor antagonist with Ki of 0.07 and 7.8 uM, respectively.

A potent dopamine stabilizer with Ki of 447 and 1305 nM for D2 and D3 receptors respectively.

A potent dopamine D2 receptor antagonist with Ki of 28 nM.

A potent dopamine D2 receptor antagonist with Ki of 28 nM.

A potent CYP26A1 inhibitor with IC50 of 10 nM, potently inhibits all-trans-retinoic acid metabolism in intact T47D cells with IC50 of 8.7 nM.

A potent chelator of iron that arrests late stages of cytokinesis by blocking the physical process of constriction in dividing cells.

A potent CDK1 and CDK2 inhibitor with IC50 of 9.5 nM and 5.4 nM against CDK1/cyclinB and CDK2/cyclinA3 respectively.

A potent CCR4 antagonist that blocked CCL22- and CCL17-mediated migration of human peripheral blood CD4+CD25+ Treg and Th2 cells ex-vivo and murine Tregs in-vivo..

A potent CCR4 antagonist that blocked CCL22- and CCL17-mediated migration of human peripheral blood CD4+CD25+ Treg and Th2 cells ex-vivo and murine Tregs in-vivo.

A potent CCR2 specific antagonist that blocks MCP-1 mediated response with an IC50 of 3.2 nM.

A potent Caspase-6 inhibitor with IC50 of 192 nM, also inhibits Caspase-4/8/9/10 with IC50 of 0.1-0.8 uM.

A potent calcium sensing receptor (CaSR) negative allosteric modulator with IC50 of 146 nM for hCaSR.

A potent calcium sensing receptor (CaSR) negative allosteric modulator with IC50 of 146 nM for hCaSR.

A potent benzodiazepine inverse agonist that displays anxiogenic and potent convulsant activity.

A potent BCL6 protein-protein interaction inhibitor with Kd of 78 nM.

A potent bactericidal agent that inhibits the KinA autophosphorylation with IC50 of 1.6 uM.

A potent anticancer agent that demonstrates potent antitumor activity in vitro against several cancer cell lines as well as in vivo against several tumor models, effectively inhibits in vitro tubulin polymerization. .

A potent anthrax lethal toxin entry inhibitor with IC50 of 1.7 uM, inhibits endosomal trafficking pathways exploited by multiple toxins and viruses.

A potent and specific, nonlipid agonist of LPA2 receptor with EC50 of 100 nM, without activating or inhibiting LPA1/3/4/5 receptors.

A potent and specific CCR6 antagonist.

A potent and specific BET bromodomain inhibitor with Ki of 3.2-24.7 nM for BD1 and BD2 domains of BRD2, BRD3, and BRD4.

A potent and selective, orally bioavailable, reversible BTK inhibitor with IC50 of 2.8 nM.

A potent and selective, orally bioavailable JAK2 inhibitor with IC50 of 2 nM.

A potent and selective, orally bioavailable aromatase inhibitor with IC50 of 1.7 nM, 180 times more potent than aminoglutethimide.

A potent and selective, non-ATP competitive, allosteric MAPKAPK2/3 (MK2/3) inhibitor with IC50 of 8 nM for MK2, hTNFα EC50 of 0.31 uM.

A potent and selective, CNS-penetrant PDE1 inhibitor with IC50 of 35 nM for PDE1B..