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

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

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

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

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

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

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 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 monoacylglycerol lipase (MAGL) with IC50 of <0.4 nM against human and rodent MAGL.

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

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 and orally active inhibitor of PTK2/FAK with IC50 of 1 nM in cell-free assays.

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

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, 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, 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, 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, dual PDK1 and Aurora kinase A inhibitor with IC50 of 416 and 35 nM, respectively.

A potent, dual pan-RET/VEGFR2 kinase inhibitor with IC50s of <1 nM for all RET, RET V804M and VEGFR2.

A potent, dual CDC-like kinase (CLK)/CDK inhibitor with IC50 of 148, 111, 104, 382 and 573 nM for CLK1, CLK2, CLK4, CDK1 and CDK4, respectively..

A potent, dual BET bromodomain-kinase inhibitor with IC50 of 34, 1.1 and 1.1 nM for BRD4 BD1, JAK2 and FLT-3, respectively.

A potent, dual ACE-neutral endopeptidase (vasopeptidase) inhibitor with IC50 of 0.053 and 5.0 nM, respectively.

A potent, competitive inhibitor of quinine-activated bitter taste receptor T2R4 with IC50 of 59 nM..

A potent, competitive inhibitor of HMG-CoA reductase (HMGCR) with IC50 of 11 nM.

A potent, CNS-active Glucosylceramide synthase (GCS) inhibitor with IC50 of 27 nM.

A potent, cell-permeable inhibitor of MK2 with IC50 of 8.5 nM.

A potent, biased allosteric agonist of CXCR3 (pEC50=6.64), selectively induces chemotaxis and receptor internalization, and induces β-arrestin 2 recruitment without any stimulation of G proteins..