A potent, selective and orally bioavailable adenosine A1 (A1A) receptor antagonist with Ki of 7 nM.

A potent, selective and orally bioavailable CCR5 antagonist IC50 of 6.5 nM, Kd of 3.1 nM in human PBMCs.

A potent, selective and orally bioavailable P2X7 receptor with IC50 of 4 nM and 115 nM for hP2X7 and rP2X7, respectively.

A potent, selective and orally bioavailable S1P lyase (S1PL) inhibitor with enzyme IC50 of 44 nM, cell IC50 of 110 nM.

A potent, selective and orally efficacious factor Xa (FXa) inhibitor with IC50 of 0.32 nM.

A potent, selective and photo-dependent inhibitor of PKC with IC50 of 50 nM.

A potent, selective and, cell and in vivo active p300/CBP catalytic inhibitor with IC50 of 9.8/2.6 nM.

A potent, selective antitumour agent through activation the aryl hydrocarbon receptor (AhR) pathway.

A potent, selective BACE inhibitor with IC50 of 30 nM for BACE1, equally potent against BACE2 (IC50=40 nM) but >1,000-fold selectivity over cathepsin D, cathepsin E, pepsin and renin.

A potent, selective cannabinoid receptor CB2 agonist with Ki of 3.6 nM, 1200-fold selectivity over CB1.

A potent, selective cannabinoid receptor CB2 agonist with Ki of 7.1 nM, >80-fold selectivity over CB1 receptors in radioligand binding assay.

A potent, selective CB1 cannabinoid receptor antagonist with Ki of 350 fM, >60,000-fold selective for the CB1 receptor versus CB2 receptor (Ki=21 nM).

a potent, selective CBP bromodomain inhibitor with IC50 of 69 nM, displays exquisite selectivity over BRD4(1) (IC50=18 uM) and the broader bromodomain family..

A potent, selective CCK1 receptor agonist with EC50 of 0.47 nM.

A potent, selective cell permeable neuronal nitric oxide synthase (nNOS) inhibitor with Ki of 30 nM.

A potent, selective cholecystokinin receptor CCK2 antagonist for treatment of gastroesophageal reflux disease (GERD)..

A potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 0.12 uM, >400-fold selectivity over ChoKβ.

A potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 0.13 uM, >385-fold selectivity over ChoKβ.

A potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 1.0 uM, 33-fold selectivity over ChoKβ.

A potent, selective competitive and nonpeptide PAR-1 antagonist with IC50 of 70 nM.

A potent, selective COX-2 inhibitor with IC50 of 0.34 ug/mL, >50-fold selectivity over COX-1 (IC50=19.4 ug/mL).

A potent, selective CRAC channel Orai1 blocker with IC50 of 3 uM.