A potent and biologically-active PDE4/7 inhibitor with IC50 of 50-100 nM for PDE4A/B/D, and 140 nM for both PDE7A/B.

A potent and effective calcium-sensitive opener of maxi-K potassium channels (maxi-K) with EC50 of 392 nM at -48.4 mV in HEK293 isolated outside-out membrane patches.

A potent and efficacious hERG channel activator steeply potentiates current amplitudes more than 10-fold with EC50 of 0.5 uM.

A potent and highly selective Chk2 inhibitor with IC50 of 0.14 nM.

A potent and highly selective D4 dopamine receptor antagonist with Ki of 3.5 nM, >200-fold selectivity over D2 and D3 receptors.

A potent and highly selective JAK3 inhibitor with IC50 of 0.15 nM.

A potent and highly specific inhibitor of Aurora B and Aurora C with IC50 of 7 and 12 nM respectively, with less activity against Aurora A (IC50>2 uM).

A potent and highly specific MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM.

A potent and orally active non-peptide C5a receptor (CD88.

A potent and orally active p53-MDM2 interaction inhibitor with IC50 of 2.4 nM.

A potent and orally bioavailable dual antagonist of CCR2 and CCR5 with binding IC50 of 0.7 nM and 2.4 nM, respectively.

A potent and selective (up to 263-fold) inhibitor of breast cancer cells with GI50 of 0.5 uM (MCF-7), via activation the aryl hydrocarbon receptor (AhR) pathway.

A potent and selective 5-HT1A receptor antagonist.

A potent and selective 5-HT2C receptor agonist with EC50 of 190 nM, with excellent selectivity for 5-HT2C over 5-HT2A.

A potent and selective 5-HT3 receptor antagonist has been shown to be beneficial in the treatment of irritable bowel syndrome..

GR79236 is a highly potent and selective adenosine A1 receptor agonist (Ki = 3.1 nM) that has analgesic and anti-inflammatory actions in humans and animals.

A potent and selective agonist for the cannabinoid receptor CB1 with Ki of 0.28 nM, 180-fold selectivity over CB2..

A potent and selective Akt inhibitor with Ki of 0.16 nM for Akt1.

A potent and selective ALK5 inhibitor with IC50 of 5.5 nM, displays 300-fold selecitvity over ALK3.

A potent and selective antagonist of CXCR4 with IC50 of 13 nM in a CXCR4 125I-SDF inhibition binding assay.

A potent and selective antagonist of CXCR4 with IC50 of 13 nM in a CXCR4 125I-SDF inhibition binding assay.

A potent and selective antagonist of H3 receptor with Ki/EC50 of 0.16/1.5 nM.