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

A potent, competitive antagonist for μ, κ, δ, and σ-opioid receptors with Ki of 0.0825 nM, 0.509 nM, and 8.02 nM, for MOR, KOR, and DOR, respectively.

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

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

A potent, covalent inhibitor of ubiquitin-conjugating enzyme UbcH5 with Kd of 5.189 uM, 3.578 uM, and 2.577 uM for UbcH5a, UbcH5b, and UbcH5c, respectively.

A potent, covalent, orally active ALDH1A2 inhibitor with IC50 of 0.3 uM.

A potent, dual ACE-neutral endopeptidase (vasopeptidase) inhibitor with IC50 of 0.053 and 5.0 nM, 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 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 class I PI3K/mTOR inhibitor with IC50 of 2/3/3/15/ for p110α/β/δ/γ, respectively.

RO-5963 is an inhibitor of the interaction of both MDM2 and MDMX with p53.

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

A potent, dual PDK1 and Aurora kinase A inhibitor with IC50 of 416 and 35 nM, 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, 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, equipotent CXCR1 and CXCR2 antagonist with IC50 of 31 nM and 21 nM, 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 5-HT1A receptor partial agonist with Ki of 0.1 nM, displays 460- and 260-fold selectivity for 5-HT1A over the α1-adrenergic and D2 receptors, respectively..

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..

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, 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, 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.

A potent, long acting, orally active, selective ETA receptor antagonist that binds competitively to human ETA receptor with Ki of 0.43 nM, IC50 of 1.4 nM.

A potent, long acting, reversible and competitive DPP-4 inhibitor with IC50 of 0.9 nM.

A potent, long lasting 5-HT(1B/1D) receptor agonist as a antimigraine agent..

A potent, mixed sigma2 agonist and sigma1 antagonist with Ki of 0.28 and 13.0 nM, respectively.

A potent, mixed sigma2 agonist and sigma1 antagonist with Ki of 0.28 and 13.0 nM, respectively.

CEP-11981 is a potent, multi-targeted, orally active, pan-VEGFR, TIE-2 and FGFR1 inhibitor with IC50 of 3-100 nM.

A potent, mutant-selective PfDHODH inhibitor with IC50 of 210 nM for 3D7 E182D PfDHODH.

A potent, noncompetitive TRPV1 antagonist that abrogates capsaicin and pH-evoked TRPV1 channel activity with submicromolar activity.

A potent, noncovalent SARS-CoV papain-like protease (PLpro) inhibitor with IC50 of 2.6 uM.

A potent, non-prostanoid prostacyclin partial agonist that potently inhibits human (IC50=35 nM), rabbit (IC50=136 nM) and rat (IC50=1.3 uM) platelet aggregation.

A potent, non-selective tyrosine protein kinase inhibitor for Trk family, CaMK and other phosphorylase kinases.

A potent, nonselective, brain penetrant, full agonist at both the central CB1 and peripheral CB2 receptors with Ki of 4.6 and 0.31 nM, respectively.

A potent, oral active glucagon receptor antagonist blocking the glucagon effect for the treatment of T2DM.

A potent, orally active dual modulator of FXR and soluble epoxide hydrolase (sEH) that exertss partial FXR agonism (pEC50=7.7) and sEH inhibitory activity (pIC50=8.4).

A potent, orally active gap-junction modifier.

A potent, orally active gap-junction modifier.

A potent, orally active hepcidin production inhibitor with IC50 of 39 nM, with low kinase inhibitory activity.

A potent, orally active iNOS inhibitor (IC50=10 nM, NO release DLD-1 cells) that prevents dimerization of iNOS, but has no effect on the expression or enzyme activity of iNOS.

A potent, orally active microsomal triglyceride transfer protein (MTP) inhibitor that inhibits both human and rodent MTP with IC50 of 2 nM.

A potent, orally active p38 MAPK inhibitor with IC50 of 50 nM, significantly decreases incidence of arthritis in mouse collagen-induced arthritis..

A potent, orally active pan-inhibitor of HIF prolyl hydroxylase (HIF-PHD) with IC50 of 1.0,1.0, and 14 nM for HIF-PHD1, 2, and 3, respectively.

A potent, orally active PfDHODH inhibitor (IC50=0.3 uM) with antimalarial activity.

A potent, orally active sigma receptor antaognist with Ki of 27 and 7 nM for σ1 and σ2, respectively.

A potent, orally active γ-secretase inhibitor with cell IC50 of 0.3 nM.

A potent, orally active, and irreversible pan-Caspase protease inhibitor with IC50 of <0.08 to 7 nM for inhibition of activated caspase 3, 6 and 8.

A potent, orally active, centrally acting aminopeptidase inhibitor, the prodrug of the specific and selective aminopeptidase A inhibitor EC33.

A potent, orally active, dual NK1 receptor antagonist (IC50=0.5 nM) and SERT inhibitor (IC50=5.2 nM).

A potent, orally available hydrophobic aminopeptidase inhibitor that structurally mimics the aminopeptidase inhibitor Tostedostat..

A potent, orally available, dual ACE-neutral endopeptidase (vasopeptidase) inhibitor with IC50 of 12 and 63 nM, respectively.

A potent, orally bioactive 20S proteasome inhibitor with IC50 of 1.3 nM (inhibition of proteasomal chymotrypsin-like proteolytic activity).

A potent, orally bioavailable brain‐penetrant, NR2B-selective NMDA receptor (GluN2B) antagonist with Ki and IC 50 of 8.1 nM and 3.6 nM respectively, with no off-target activity.

A potent, orally bioavailable dual CXCR2/CXCR1 receptor antagonist with IC50 of 1.3 nM and 7.3 nM, respectively.

Cavosonstat is a potent, orally bioavailable inhibitor of S-nitrosoglutathione reductase (GSNOR) and CFTR modulator.

A potent, orally bioavailable P-selectin inhibitor with improved pharmacokinetic properties and oral efficacy in models of vascular injury..

A potent, orally bioavailable, dual Src/Abl kinase inhibitor with IC50 of 0.5, 0.4, 0.5 and <1 nM for Src, Lck, Yes and Bcr-Abl, respectively.

A potent, orally bioavailable, dual XIAP/cIAP1 inhibitor with EC50 of 5.1/0.32 nM, respectively.

A potent, orally bioavailable, full agonist of GPR40/FFA1 with EC50 of 0.16 uM.

A potent, orally bioavailable, irreversible proteasome inhibitor with potent antimyeloma activity (IC50<60 nM).

A potent, orally bioavailable, small-molecule inhibitor of HDM2/p53 protein-protein interaction.

A potent, orally-active MEK1/2 inhibitor with IC50 of 10-100 nM.

A potent, pan-genotype HCV NS5A inhibitor with replicon EC90 of 0.003, 0.016, 0.067, 0.036, 0.007, and 0.007 nM for GT1a, GT1a L31V, GT1a Y93H, GT2b, GT3a, and Gt4a, respectively..

RC-3095 is a gastrin-releasing peptide receptor antagonist, synergizes with gemcitabine to inhibit the growth of human pancreatic cancer CFPAC-1 in vitro and in vivo. RC-3095 inhibit the growth of human glioblastomas in vitro and in vivo. RC3095 inhibits tumor growth and decrease the levels and mRNA expression of epidermal growth factor receptors in H-69 small cell lung carcinoma.R,BRS-1) antagonist.

A potent, peptide-inhibitor of human chymase with Ki of 1 nM.

A potent, picomolar, dual inhibitor of Aurora A and B with IC50 of 0.02 and 0.03 nM, respectively.

A potent, picomolar, dual inhibitor of Aurora A and B with IC50 of 0.02 and 0.03 nM, respectively.

GNF-351 is a potent, pure aryl hydrocarbon receptor (AHR) antagonist (IC50=62 nM) devoid of partial agonist potential; antagonizes agonist and SAhRM-mediated suppression of SAA1, inhibit both DRE-dependent and -independent activity; decreases migration and invasion of HNSCC cells and prevents benzo[a]pyrene-mediated induction of the chemotherapy efflux protein ABCG2.

A potent, reasonably selective agonist of peripheral cannabinoid receptor with Ki of 11 nM for CB2, 22-fold selectivity over the psychoactive CB1 receptors (Ki=245 nM)..

A potent, reasonably selective cannabinoid CB2 agonist with Ki of 0.4 nM, 25-fold selectivity over CB1 receptor..

A potent, reasonably selective Chk1 inhibitor with cell IC50 of 5 nM.

A potent, relatively selective and orally active adenylyl cyclase 1 (AC1) inhibitor with IC50 of 10 uM (cAMP production inhibition).

A potent, relatively selective G protein-coupled receptor kinase GRK2 inhibitor with IC50 of 280 nM.

A potent, relatively selective G protein-coupled receptor kinase GRK2 inhibitor with IC50 of 66 nM.

A potent, reversible type III inhibitor of SAHH (S-adenosyl-L-homocysteine hydrolase) with Ki of 17.9 nM.

A potent, second generation HCV NS3 serine protease inhibitor with Ki of 6 nM.

A potent, second-generation BET protein degrader that exhibits superior selectivity, potency and antitumor activity.

A potent, selectiive inhibitor of WNK1 kinase with IC50 of 95 nM, shows IC50 of 1.39 uM in the cellular OSR1 phosphorylation assay with reasonable aqueous solubility..

A potent, selective 5-HT2A receptor antagonist with Ki of 0.36 nM, > 80-fold selectivity for 5-HT2A over other serotonergic receptors.

A potent, selective 5-HT2B receptor agonist with pKi of 7.1, >10-fold selectivity over 5-HT2A, 5-HT2C, and other 5-HT subtypes.

A potent, selective 5-HT2C receptor agonist with IC50 of 20 nM in HEK293 cells-exppressed 5-HT2C, shows weakly activity for 5-HT2A.

A potent, selective A2A adenosine receptor antagonist with Ki of 6.6 nM.

A potent, selective adenylyl cyclase AC5/6 inhibitor with IC50 of 7.7/17 uM, respectively.

A potent, selective agonist of 5-HT1A and 5-HT1B receptors, with preference for 5-HT1B.

A potent, selective agonist of PBR/TSPO that inhibits [3H]PK 11195 binding to crude mitochondrial preparations of rat whole brain with IC50 of 0.92 nM..

A potent, selective agonist of the human and rat CCK1 receptor with Ki of 36 nM.

A potent, selective agonist of the orphan GPR88 receptor with EC50 of 877 nM.

A potent, selective agonist of the rat (EC50=97 nM) and human (EC50=23 nM) TRPA1 channel.

A potent, selective ALK5 inhibitor with IC50 of 4.8 nM, >100-fold selectivity over 95 different kinases.

A potent, selective and ATP-competitive CK2 inhibitor with Ki of 0.5-1 uM.

A potent, selective and ATP-competitive inhibitor of IKK2 with IC50 of 60 nM and Ki of 20 nM, also interfers directly with FLT3 kinase activation.

A potent, selective and cell active Hedgehog acyltransferase (Hhat) inhibitor with IC50 of 0.87 uM.

A potent, selective and cell active lysine methyltransferase SMYD2 inhibitor with IC50 of 2.8 nM.

A potent, selective and cell permeable inhibitor of mitotic kinesin Eg5 with IC50 of 0.8 uM, does not interact with other microtubule motor proteins.

A potent, selective and competitive corticotropin-releasing factor CRF2 receptor antagonist with Ki of 1.4 nM, 100-fold selectiivity over CRF1.

A potent, selective and competitive CXCR2 inhibitor that selectively inhibits CXCR2-mediated recruitment of β-arrestin-2 with pKi of 8.92.

A potent, selective and competitive NK1 receptor antagonist with IC50 of 2.3 nM.

A potent, selective and oral lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.23 nM, for the treatment of Alzheimer's disease and atherosclerosis..

A potent, selective and orally active adenosine A1 receptor antagonist with Ki of 1.3 nM.

A potent, selective and orally active blocker of voltage-gated potassium channels Kv7 (KCNQ) that blocks KCNQ1, KCNQ2 and KCNQ2+KCNQ3 with Kd of 0.78, 0.7 and 0.6 uM, respectively.

NI-42 is a potent, selective and orally active BRPF1 bromodomain inhibitor with IC50 of 7.9 nM, with excellent selectivity over nonclass IV BRDs; weakly inhibits BRPF2 (BRD1), BRPF3, BRD9 and BRD4 (BD1) with IC50 of 48, 260, 310 and 4500 nM respectively, and no activity for ATAD2A/2B (IC50>100 uM); shows a modest (GI50=1-10 uM) and selective inhibition of proliferation of certain cancer lines, particularly those lines exhibiting monocytic lineage differentiation; a novel, structurally orthogonal chemical probe for the BRPFs suitable for cellular and in vivo studies.

A potent, selective and orally active Chk1 inhibitor.

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.

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 CRF1 receptor antagonist with Ki of 12 nM, shows no affinity for CRF2 receptor (Ki>10 uM).

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

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

A potent, selective and orally active neurotensin receptor antagonist with IC50 of 1.19 nM.

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

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

A potent, selective and orally available factor Xa (FXa) inhibitor with IC50 of 54.6 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 bioavailable adenosine A1 (A1A) receptor antagonist with Ki of 7 nM.

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

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 TRPV1 receptor antagonist with IC50 of 65 nM and 102 nM for hTRPV1 and rTRPV1, respectively.

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

A potent, selective and photo-dependent inhibitor of PKC with IC50 of 50 nM.

A potent, selective and, cell and in vivo active p300/CBP catalytic inhibitor with IC50 of 9.8/2.6 nM.

A potent, selective antitumour agent through activation the aryl hydrocarbon receptor (AhR) pathway.

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 cannabinoid receptor CB2 agonist with Ki of 3.6 nM, 1200-fold selectivity over CB1.

A potent, selective cannabinoid receptor CB2 agonist with Ki of 7.1 nM, >80-fold selectivity over CB1 receptors in radioligand binding assay.

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 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 CCK1 receptor agonist with EC50 of 0.47 nM.

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

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

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

A potent, selective competitive and nonpeptide PAR-1 antagonist with IC50 of 70 nM.

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 CRAC channel Orai1 blocker with IC50 of 3 uM.

A potent, selective CXCR7 antagonist with IC50 of 4.1 nM.

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 dipeptidyl peptidase-4 (DPP-4) inhibitor for treatment for type 2 diabetes..

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

A potent, selective dopamine D4 receptor agonist that activates human dopamine D4 receptors with EC50 of 12.4 nM, with no effect on dopamine D1, D2, D3, or D5 receptors.

A potent, selective dopamine D4 receptor agonist that activates human dopamine D4 receptors with EC50 of 12.4 nM, with no effect on dopamine D1, D2, D3, or D5 receptors.

A potent, selective dopamine D4 receptor agonist with Ki of 12.1 and 7.9 nM for rat and human D4 receptors, respectively.

A potent, selective dual mTORC1 and mTORC2 inhibitor with enzyme IC50 of 1.5 nM.

A potent, selective estrogen receptor downregulator (SERD) with ER downregulation pIC50 of 9.68.

A potent, selective FABP4 inhibitor with Ki of 30 nM..

A potent, selective G protein-coupled receptor kinase GRK2 inhibitor with IC50 of 8 nM.

A potent, selective GLP-1 agonist.

A potent, selective glucose transporter 4 (GLUT4) inhibitor with IC450 of 10.8 uM, inhibits MM cell proliferation.

A potent, selective GluN2C-selective NMDA receptor glycine site superagonist with EC50 of 1.7 nM at GluN1/2C.

A potent, selective glycine transporter 1 (GlyT1) inhibitor with IC50 of 100 nM.

A potent, selective GlyT1 inhibitor that demonstrates >10-fold greater activity in in vitro functional glycine reuptake assay than racemic (±)-NFPS.

A potent, selective Grp94 inhibitor with IC50 of 8 nM.

A potent, selective Grp94 inhibitor with Kd of 0.2 uM.

A potent, selective Grp94 inhibitor with Kd of 0.44 uM.

PU-H54 is potent, selective Grp94 inhibitor.

A potent, selective HDAC1 and HDAC2 inhibitor with IC50 of 6 nM and 45 nM, respectively.

A potent, selective HDAC1 inhibitor with IC50 of 1.5 uM.

A potent, selective HDAC6 inhibitor with IC50 of 84 nM, with IC50s of >3.5 uM for the other HDAC isoforms..

A potent, selective hERG potassium channel (Kv11.1) activator that increases peak tail hERG current of 111.1% at 10 uM in HEK293 cells.

ML-T531 is a potent, selective hERG potassium channel (Kv11.1) activator with EC50 of 3.13 uM.

A potent, selective HIF-1 inhibitor with IC50 of 1.9 nM, with no signigicant inhibition on HSF and NF-κB.

A potent, selective high affinity TrkA receptor agonist with Kd of 75 nM.

A potent, selective human Arginase inhibitor with Ki of 0.25 uM (pH=7.5), 8.5 nM (pH=9.5) for type II arginase.

Bay-8040 is a potent, selective human neutrophil elastase (HNE) inhibitor with IC50 of 28 nM; displays no significant inhibition toward 68 other pharmacologically relevant targets (>10 uM), and a panel of related serine proteases; shows in vivo efficacy with regard to decreasing cardiac remodeling and amelioration of cardiac function in monocrotaline-induced rat model for pulmonary arterial hypertension.

A potent, selective IMPDH2 inhibitor that covalently binds to Cys140 with IC50 of 620 nM (inhibition of NO production).

A potent, selective inhibitor of cdc2-like kinase CLK1 and CLK2 with IC50 of 1.1 and 2.4 nM, respectively.

A potent, selective inhibitor of clathrin-independent endocytosis with IC50 of 18 uM (inhibition of clathrin TD-amphiphysin B/C complex formation).

A potent, selective inhibitor of CXCL12 binding to CXCR4 and CXCR7 with IC50 of 200 nM.

A potent, selective inhibitor of CXCR4 with IC50 of 13 nM, has no effect on CXCR1, CCR3, CCR4, or CCR5.

A potent, selective inhibitor of HIV integrase (IC50=8-15 nM) with potent antiviral activity in cell culture and good pharmacokinetic properties.

A potent, selective inhibitor of human LIMK1 with IC50 of 38 nM .

CL-82198 is a selective inhibitor of MMP-13. CL-82198 binds to the entire S1’ pocket of MMP-13, which is the basis for its selectivity towards MMP-13 and the lack of inhibitory activities against other MMPs. CL-82198 is a pharmacologic treatment for preventing osteoarthritis (OA) progression.

A potent, selective inhibitor of p300 histone acetyltransferase (IC50=4.2 uM).

A potent, selective inhibitor of phosphodiesterases PDE4 with IC50 of 3 nM, 130 nM and 240 nM for PDE4A, PDE4B, and PDE4D, respectively.

A potent, selective inhibitor of protein phosphatase 2A (PP2A) with IC50 of 0.04 nM.