A potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, respectively.

A potent, selective mGluR7 allosteric agonist that inhibits forskolin-stimulated cAMP accumulation in mGluR7b CHO cells with EC50 of 64±32 nM.

EPPTB is a selective antagonist of the trace amine-associated receptor 1 (TAAR1).

A potent, selective NaV1.7 blocker with IC50 of 3 nM.

A potent, selective N-methyl-D-aspartate (NMDA) antagonist with selectivity for the NR2B subunit.

A potent, selective noncovalent competitive inhibitor of HCV NS3/4A protease with Ki of 2.6 and 2.0 nM for GT1a and 1b NS3-NS4A protease, respectively.

A potent, selective nonpeptide antagonist of anaphylatoxin C3a receptor (C3aR) with IC50 of 200 nM.

A potent, selective opiate receptor-like orphan receptor (ORL-1, NOP) antagonist with Ki of 0.33 nM.

A potent, selective orally-bioavailable TRPV4 antagonist with IC50 of 320, 420 and 660 nM for mouse, human and rat TRPV4 channels, respectively.

A potent, selective orally-bioavailable TRPV4 antagonist with IC50 of 320, 420 and 660 nM for mouse, human and rat TRPV4 channels, respectively.

A potent, selective OX1 receptor antagonist with Ki of 57 nM (whole cell assay), and 27 nM (cell membrane-based SPA assay).

A potent, selective p38α MAPK inhibitor with IC50 of 9 nM.

A potent, selective PDE3 inhibitor with IC50 of 36 nM, displays >20,000-fold selectivity over PDE1..

A potent, selective PDE3 inhibitor with IC50 of 50 nM.

A potent, selective peptide inhibitor of hERG channel with IC50 of 3.3 nM for hERG1 channels.

A potent, selective phosphodiesterase 4 (PDE4) inhibitor with IC50 of 26.1, 22.8, 21 and 0.28 nM for PDE4A4, PDE4B2, PDE4C2 and PDE4D3, respectively..

A potent, selective presynaptic dopamine autoreceptor antagonist.

A potent, selective protein tyrosine phosphatase DUSP5, PTP1B and SHP-2 inhibitor with IC50 of 36 uM, 2.1 and 1.1 uM respectively, 8-fold selectivity for PTP1B versus DUSP5.

A potent, selective RARα agonist.

A potent, selective RARβ antagonist that inhibits RA-induced transcriptional activation of RARβ, but not RARα, RARγ or RXRα on a variety of RA response elements.

A potent, selective receptor interacting protein-2 (RIP2) kinase inhibitor..

A potent, selective S1P1 receptor full agonist with EC50 of 13.8 nM, with no activites at the S1P2-5 receptors.