A potent, dual BET bromodomain-kinase inhibitor with IC50 of 34, 1.1 and 1.1 nM for BRD4 BD1, JAK2 and FLT-3, respectively.

A potent, dual ACE-neutral endopeptidase (vasopeptidase) inhibitor with IC50 of 0.053 and 5.0 nM, respectively.

A potent, competitive inhibitor of quinine-activated bitter taste receptor T2R4 with IC50 of 59 nM..

A potent, competitive inhibitor of HMG-CoA reductase (HMGCR) with IC50 of 11 nM.

A potent, CNS-active Glucosylceramide synthase (GCS) inhibitor with IC50 of 27 nM.

A potent, cell-permeable inhibitor of MK2 with IC50 of 8.5 nM.

A potent, biased allosteric agonist of CXCR3 (pEC50=6.64), selectively induces chemotaxis and receptor internalization, and induces β-arrestin 2 recruitment without any stimulation of G proteins..

A potent, biased allosteric agonist of CXCR3 (pEC50=5.22) that activates solely G proteins, induces chemotaxis, but fails to induce receptor internalization or β-arrestin 2 recruitment..

A potent, ATP-competitive and relative selective Nek2 inhibitor with IC50 of 0.27 uM.

A potent, and selective GluR5-subunit containing kainate receptor antagonist with Kd of 402 nM.

A potent, and selective FAAH inhibitor with IC50 of 18 nM.

A potent, and selective Bax agonist (Ki=43.3 nM) that induces conformational changes in Bax by blocking S184 phosphorylation.

A potent, allosteric inhibitor of CBFβ-RUNX1 interaction with IC50 of 3.2 uM in FRET assays.

A potent, allosteric HIV integrase inhibitor (Kd=34 nM) that binds the LEDGF/p75 binding site on integrase.

A potent γ-secretase inhibitor that preferentially inhibits cleavage of the APP CTF cleavage with IC50 of 7.1 nM.

A potent tyrosine kinase inhibitor targeting c-Kit and PDGFR with IC50 of 0.15 and 0.05 uM in cell based assays.

A potent tubulin inhibitor that is a toxin payload in antibody drug conjugates (ADCs)..

A potent TNFα/TNFRc1 interaction antagonist with IC50 of 50 nM, with no affinity for the related cytokine receptors TNFRc2 or CD40, and no cytotoxicity (>100 uM).

A potent TLR7 agonist with EC50 of 8.6 nM. .

A potent TLR7 agonist with EC50 of 59 nM..

A potent STAT5 inhibitor with a dual mechanism of action, potently inhibits STAT5 through liberation of endogenous phosphatase activity following NADPH oxidase (NOX) inhibition at 200-300 nM.

A potent Src inhibitor extracted from patent WO/2012003544A1..

A potent SR-3 antagonist

A potent small-molecule inhibitor of the MIR155 host gene/miR-155 axis.

A potent small molecule inhibitor of MELK kinase activity with IC50 of 42 nM.

A potent RIG-I-like receptor (RLR) agonist that triggers IRF3-dependent innate immune antiviral genes and IFN-β expression.

A potent psychopharmacologic agent that shows high affinity for 5-HT, dopamine, histamine and adrenoceptors.

A potent protein tyrosine kinase inhibitor that shows selectivity for PDGFR in vitro and in cells.

A potent photoaffinity ligand for the peripheral-type benzodiazepine binding site with Ki of 4 nM.

A potent phosphodiesterase 12 (PDE12) with Ki of 17.5 nM, with no activity for related enzyme CNOT6 (Ki>10 uM).