A potent, selective kappa-opioid receptor agonist with no μ-opioid antagonist effects.

A potent, selective KDM5 sub-family(JARID1) inhibitor with biochemical IC50 of 71/19/69/69 nM for KDM5A/B/C/D, respectively.

A potent, selective ligand for the mitochondrial translocator protein 18kDa (TSPO/PBR).

A potent, selective LIMK inhibitor with IC50 of 0.9 nM and 0.5 nM and 1.2 nM for LIMK1 and LIMK2, respectively.

A potent, selective LIMK inhibitor with IC50 of 3.2 nM and 1.2 nM for LIMK1 and LIMK2, respectively.

A potent, selective LPA2 (EDG4) antagonist with IC50 of 17 nM.

A potent, selective LTA4H (Leukotriene A4 hydrolase) inhibitor (IC50/Kd=47/25 nM) of leukotriene B4 biosynthesis.

A potent, selective melanin concentrating hormone receptor 1 (MCH-R1) antagonist with binding Ki of 12.2 nM.

A potent, selective melanin concentrating hormone receptor 1 (MCHR1) inhibitor with Ki of 10.4 nM.

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.

A potent, selective MMP-2 inhibitor with Ki of 230 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 P. falciparum dihydroorotate dehydrogenase (PfDHODH) with IC50 of 53 nM.