A potent HIV integrase strand transfer inhibitor (InSTIs) with IC50 of 8 nM in HIV replication assay.

A potent histamine 1 receptor antagonist..

A potent HIF-2α inhibitor with IC50 of <500 nM in HIF-2α scintillation proximity assay. .

A potent hERG channel activator that concentration-dependently increases the hERG current (2.1 and 3.4-fold at 3 and 10 uM, respectively) and markedly slows hERG channel deactivation and inactivation.

A potent heat shock protein coinducer.

A potent HDAC inhibitor with IC50 of 27 nM (HeLa cell extracts).

A potent HDAC inhibitor with IC50 of 172 nM.

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 CXCR7 (ACKR3) agonist..

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 BET bromodomian inhibitor with IC50 of 3-7 nM for BRD2/3/4 BD1 and BD2..

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 aromatase inhibitor for the treatment of hypogonadism..