A potent, selective S1P3 antagonist with Ki of 0.25 nM.

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

A potent, selective renal outer medullary potassium channel (ROMK, Kir1.1) inhibitor with IC50 of 0.24 uM in T1+ flux assays.

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

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 RARα agonist.

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 PLK1 PBD inhibitor with IC50 of 1.36 uM.

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 peptide inhibitor of hERG channel with IC50 of 3.3 nM for hERG1 channels.

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

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

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

A potent, selective P. falciparum dihydroorotate dehydrogenase (PfDHODH) with IC50 of 53 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 opiate receptor-like orphan receptor (ORL-1, NOP) antagonist with Ki of 0.33 nM.

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

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 NaV1.7 blocker with IC50 of 3 nM.

A potent, selective MMP-2 inhibitor with Ki of 230 nM.

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

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

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

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

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

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 kappa-opioid receptor agonist with no μ-opioid antagonist effects.

A potent, selective IRAK4 inhibitor with IC50 of 1.3 nM, 200-fold selectivity over IRAK1 (IC50=290 nM).