A potent, dual receptor tyrosine kinase/Src kinase inhibitor with IC50 of 2-16 nM for VEGFR, FGFR and PDGFR, 0.1-5 nM for Src family.

A potent, dual receptor tyrosine kinase/Src kinase inhibitor with IC50 of 2-16 nM for VEGFR, FGFR and PDGFR, 0.1-5 nM for Src family.

A potent, efficacious, and orally available pan class I PI3K inhibitor with Ki of 4/6/2/1 nM for PI3Kα/β/δ/γ, respectively.

A potent, first-in-class, oral small-molecule agent for the treatment of inflammatory bowel diseases..

A potent, first-in-class, oral small-molecule agent for the treatment of inflammatory bowel diseases..

A potent, full dopamine D1 agonist.

A potent, functionally selective TSH receptor (TSHR) positive allosteric modulator with EC50 of 11.6 uM (β-Arr 1 translocation).

A potent, functionally selective, CNS-penetrating and orally bioavailable inverse agonist of benzodiazepine site of GABAA α5 receptor with Ki of 0.8-1.5 nM for α1-, α2-, α3-, andα5-containing GABAA receptors.

A potent, highly selective and brain-penetrant 5-HT2A receptor agonist with Ki of 1.1 nM ([3H]ketanserin).

A potent, highly selective and orally active inhibitor of PTK2/FAK with IC50 of 1 nM in cell-free assays.

A potent, highly selective antagonist of chemokine receptor CXCR3 with binding IC50 of 146 nM, Ca2+-mobilization IC50 of 28 nM..

PF04802367 is a potent, highly selective GSK-3 inhibitor with IC50 of 2.1 nM for human GSK-3β in enzyme assays; shows equal effectivity against GSK-3α and GSK-3β with IC50 of 10.0 and 9.0 nM respectively in mobility shift assays, inhibits phosphorylation of tau with an IC50 of 466 nM in a stable inducible CHO cell line over-expressing GSK-3β and substrate tau; modulates tau phosphorylation in vitro and in vivo.

A potent, highly selective inhibitor of integrin α4β1 (VLA-4) with Kd of <10 pM, IC50 of 1.8 nM.

A potent, highly selective monoacylglycerol lipase (MAGL) with IC50 of <0.4 nM against human and rodent MAGL.

A potent, highly selective PI3Kβ/δ inhibitor with IC50 of 7.8/5.3 nM respectively, with liitle to no activity on PI3Kα/γ (IC50=850/>10,000 nM).

A potent, highly selective renin inhibitor with IC50 of 0.47 nM.

A potent, highly selective renin inhibitor with IC50 of 0.47 nM.

A potent, highly selective α4β1 integrin antagonist with Kd of <10 pM.

A potent, highly selective, ATP-competitive dual inhibitor of p70S6K and Akt under development for the treatment of solid tumours and non-Hodgkin's lymphoma.

A potent, highly selective, ATP-competitive ROCK inhibitor with IC50 of 0.5/1.1 nM for ROCK1/ROCK2 respectively.

A potent, highly selective, brain-penetrant NOP-R (Nociceptin/orphanin FQ receptor) agonist with EC50 of 8.8 nM.

A potent, highly selective, peptide bombesin receptor subtype-3 (BRS-3) antagonist with IC50 of 2-8 nM for human and rodent BRS-3, displays 1000-fold selectivity over hNMBR and hGRPR, increases food intake and produces an obesity phenotype in mice..