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 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 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 H3 receptor with Ki/EC50 of 0.16/1.5 nM.

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

A potent and selective ATP-competitive inhibitor of CHK2 K5777:N5777with IC50 of 3 nM.

A potent and selective dopamine D3 receptor antagonist with pKi of 8.0.

A potent and selective full β3 adrenergic receptor agonist with EC50 of 1.1 nM.

A potent and selective GC-C agonist (Ki=1.23-1.64 nM) that elicits pharmacological effects locally in the gastrointestinal tract.

A potent and selective GlyT1 inhibitor with EC50 of 54 nM.

A potent and selective GlyT1 inhibitor with IC50 of 15.8 nM, displays no activity for GlyT2 (IC50>30 uM).

A potent and selective HDAC3 inhibitor with IC50 of 0.24 uM, >75-fold selectivity over HDAC1 and no activity against HDAC4/6/8.