A potent, selective, noncompetitive human α4β2 nAChRs negative allosteric modulator with IC50 of 13.5 uM, displays no inhibitory activity on Hα3β4 nAChRs at 100 uM..

A potent, selective, noncompetitive inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH) with IC50 of 7 uM.

A potent, selective, non-competitve inhibitor of 15-lipoxygenase (15-LOX) with Ki of 197 nM.

A potent, selective, noncovalent FAAH inhibitor with IC50 of 28 nM toward human FAAH and 100 nM toward rat FAAH.

A potent, selective, nonpeptide vasopressin V1A and V2 receptor antagonist with Ki of 0.48 nM and 3.04 nM respectively.

A potent, selective, non-peptidic integrin α4β1 (VLA-4) antagonist with IC50 of 9 nM, displays 200-fold selectivity over α4β7 (IC50=2.1 uM).

A potent, selective, non-pseudosubstrate inhibitor of O(6) -alkylguanine DNA methyltransferase (MGMT) with low-nanomolar potency.

A potent, selective, non-RGD-mimetic αIIbβ3 integrin receptor antagonist with IC50 of 45 nM, with no activity on αVβ3 receptors. .

A potent, selective, orally acitve SGLT2 inhibitor with IC50 of 2.26 nM, 1650-fold selectivity over SGLT1.

A potent, selective, orally active 5-HT3 receptor agonist with high affinity for canine intestinal smooth muscle 5-HT3 receptors.

A potent, selective, orally active and CNS penetrant 5-HT6 receptor antagonist with pKi of 8.5, displays 1300-fold selectivity over other 13 5-HT receptor subtypes.

A potent, selective, orally active BACE1 inhibitor for the treatment of Alzheimer's disease..

A potent, selective, orally active BACE1 inhibitor with IC50 of 0.7 nM, demonstrates limited selectivity for over BACE2 and high selectivity both renin and pepsin.

A potent, selective, orally active bombesin receptor subtype-3 (BRS-3) agonist with EC50 of 250/100 nM for human/rat BRS-3, resp+H1437+M1438.

A potent, selective, orally active bombesin receptor subtype-3 (BRS-3) agonist with EC50 of 270/130 nM for human/rat BRS-3, respectively.

A potent, selective, orally active cannabinoid CB2 receptor inverse agonist with Ki of 35.9, 1.55 and 0.38 nM for human, mouse and rat CB2, respectively.

A potent, selective, orally active Chk1 inhibitor with IC50 of < 1 nM, Ki=69 pM.

A potent, selective, orally active cholecystokinin receptor 2 (CCK2) antagonist with IC50 of 2 nM.

A potent, selective, orally active EGFR inhibitor with IC50 of 23 nM.

A potent, selective, orally active inhibitor of cathepsin K with Ki of 0.1 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively.

A potent, selective, orally active monopolar spindle 1 (MPS1) inhibitor with IC50 of 3 nM, with no activity for CDK2 and Aurora A (IC50>40 uM).

PF-1355 is a potent, selective, orally active Myeloperoxidase (MPO) inhibitor with EC50 of 1.47 uM.