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..

A potent, highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitor with IC50 of 4 nM for CK1δ.

A potent, highly selective glycine transporter 1 (GlyT2) inhibitor with IC50 of 16 nM with negligible affinity for GlyT1..

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

A potent, highly selective, CNS penetrant mGlu7 negative allosteric modulator with IC50 of 0.76 uM.

A potent, highly selective, orally active MDM2-p53 interaction inhibitor with IC50 of 4 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..

A potent, highly specific JAK3 inhibitor with IC50 of 4 nM.

A potent, irreversible and cell permeable inhibitor of tissue transglutaminase with IC50 of 20 nM..

A potent, irreversible inhibitor of human tissue transglutaminase (hTG2)..

A potent, irreversible inhibitor of human tissue transglutaminase (hTG2)..

A potent, irreversible, and orally active inhibitor of steroid sulfatase (STS) with IC50 of 65 pM in intact MCF-7 cells.

A potent, ligand-efficient, and cell-active inhibitor menin-MLL interaction with IC50 of 56 nM, Kd of 85 nM.