A potent, selective dopamine D1 receptor antagonist with Ki of 0.56 nM.

A potent, selective dipeptidyl peptidase-4 (DPP-4) inhibitor for treatment for type 2 diabetes..

A potent, selective D1 dopamine receptor antagonist with Ki of 3.6 nM, >300-fold selectivity over D2 and 5-HT2 receptors.

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

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 choline kinase α (ChoKα) inhibitor with IC50 of 1.0 uM, 33-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 0.12 uM, >400-fold selectivity over ChoKβ.

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

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

A potent, selective CCK1 receptor agonist with EC50 of 0.47 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 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 cannabinoid receptor CB2 agonist with Ki of 3.6 nM, 1200-fold selectivity over CB1.

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 and photo-dependent inhibitor of PKC with IC50 of 50 nM.

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

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

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 adenosine A1 (A1A) receptor antagonist with Ki of 7 nM.

A potent, selective and orally available inhibitor of delta-5 desaturase (D5D) with Ki of <2.7 nM and IC50 of 19 nM, with excellent selectivity over D6D and SCD.

A potent, selective and orally available factor Xa (FXa) inhibitor with IC50 of 54.6 nM.

A potent, selective and orally available CGRP receptor antagonist for the prevention of migraine. Migraine.

A potent, selective and orally active SGLT2 inhibitor with IC50 of 8.9 nM, 280-fold selectivity over SGLT1.

A potent, selective and orally active human neutrophil elastase (HNE) inhibitor with Ki of 12 nM.

A potent, selective and orally active cytosolic phospholipase A2α (cPLA2α) inhibitor with IC50 of 20 nM.

A potent, selective and orally active CRF1 receptor antagonist with Ki of 12 nM, shows no affinity for CRF2 receptor (Ki>10 uM).

A potent, selective and orally active CRF1 receptor antagonist with IC50 of 6.1 nM, >1,000-fold selectivity over CRF-binding protein and biogenic amine receptors.

A potent, selective and orally active COX-2 inhibitor with IC50 of 26 nM for inhibition of the COX-2-dependent production of PGE2 in human osteosarcoma cells.