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 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.

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, small-molecule inhibitor of HDM2/p53 protein-protein interaction.

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.

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

A potent, selective FABP4 inhibitor with Ki of 30 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 GlyT1 inhibitor that demonstrates >10-fold greater activity in in vitro functional glycine reuptake assay than racemic (±)-NFPS.

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

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.

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 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.

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.

A potent, selective intermediate-conductance KCa3.1 positive-gating modulator with EC50 of 111 nM.

A potent, selective IRAK4 inhibitor with IC50 of 0.094 nM, >500-fold selectivity over IRAK1 (IC50=65 nM).

A potent, selective IRAK4 inhibitor with IC50 of 1.3 nM, 200-fold selectivity over IRAK1 (IC50=290 nM).

A potent, selective kappa-opioid receptor agonist with no μ-opioid antagonist effects.

A potent, selective LIMK inhibitor with IC50 of 0.9 nM and 0.5 nM and 1.2 nM for LIMK1 and LIMK2, respectively.

A potent, selective LIMK inhibitor with IC50 of 3.2 nM and 1.2 nM for LIMK1 and LIMK2, respectively.

A potent, selective LPA2 (EDG4) antagonist with IC50 of 17 nM.

A potent, selective LTA4H (Leukotriene A4 hydrolase) inhibitor (IC50/Kd=47/25 nM) of leukotriene B4 biosynthesis.

A potent, selective melanin concentrating hormone receptor 1 (MCH-R1) antagonist with binding Ki of 12.2 nM.

A potent, selective melanin concentrating hormone receptor 1 (MCHR1) inhibitor with Ki of 10.4 nM.

A potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, respectively.

A potent, selective mGluR7 allosteric agonist that inhibits forskolin-stimulated cAMP accumulation in mGluR7b CHO cells with EC50 of 64±32 nM.

EPPTB is a selective antagonist of the trace amine-associated receptor 1 (TAAR1).

A potent, selective NaV1.7 blocker with IC50 of 3 nM.

A potent, selective N-methyl-D-aspartate (NMDA) antagonist with selectivity for the NR2B subunit.

A potent, selective noncovalent competitive inhibitor of HCV NS3/4A protease with Ki of 2.6 and 2.0 nM for GT1a and 1b NS3-NS4A protease, respectively.

A potent, selective nonpeptide antagonist of anaphylatoxin C3a receptor (C3aR) with IC50 of 200 nM.

A potent, selective opiate receptor-like orphan receptor (ORL-1, NOP) antagonist with Ki of 0.33 nM.

A potent, selective orally-bioavailable TRPV4 antagonist with IC50 of 320, 420 and 660 nM for mouse, human and rat TRPV4 channels, respectively.

A potent, selective orally-bioavailable TRPV4 antagonist with IC50 of 320, 420 and 660 nM for mouse, human and rat TRPV4 channels, respectively.

A potent, selective OX1 receptor antagonist with Ki of 57 nM (whole cell assay), and 27 nM (cell membrane-based SPA assay).

A potent, selective p38α MAPK inhibitor with IC50 of 9 nM.

A potent, selective PDE3 inhibitor with IC50 of 36 nM, displays >20,000-fold selectivity over PDE1..

A potent, selective PDE3 inhibitor with IC50 of 50 nM.

A potent, selective peptide inhibitor of hERG channel with IC50 of 3.3 nM for hERG1 channels.

A potent, selective phosphodiesterase 4 (PDE4) inhibitor with IC50 of 26.1, 22.8, 21 and 0.28 nM for PDE4A4, PDE4B2, PDE4C2 and PDE4D3, respectively..

A potent, selective presynaptic dopamine autoreceptor antagonist.

A potent, selective protein tyrosine phosphatase DUSP5, PTP1B and SHP-2 inhibitor with IC50 of 36 uM, 2.1 and 1.1 uM respectively, 8-fold selectivity for PTP1B versus DUSP5.

A potent, selective RARα agonist.

A potent, selective RARβ antagonist that inhibits RA-induced transcriptional activation of RARβ, but not RARα, RARγ or RXRα on a variety of RA response elements.

A potent, selective receptor interacting protein-2 (RIP2) kinase inhibitor..

A potent, selective S1P1 receptor full agonist with EC50 of 13.8 nM, with no activites at the S1P2-5 receptors.

A potent, selective sigma 1 ligand with Ki of 0.08 nM, >3000-fold selectivity over sigma 2 (Ki=1377 nM).

A potent, selective sigma-2 receptor agonist with Ki of 16.5 nM, 200-fold selectivity over sigma 1 (Ki=3063 nM).

A potent, selective sigma-2 receptor agonist with Ki of 3.5 nM, 25-fold selectivity over sigma-1 receptors (Ki=86.6 nM).

A potent, selective small molecule inhibitor of transcription factor STAT5b with Ki of 44 nM, >50-fold selectivity over STAT5a..

PAP-1 is a selective inhibitor of Kv1.3, voltage-gated K+ channel. PAP-1 (EC50=2 nM) potently inhibits human T effector memory cell proliferation and delayed hypersensitivity. IC50 value: 2 nM (EC50) [1]in vitro: blocks Kv1.3 in a use-dependent manner, with a Hill coefficient of 2 and an EC50 of 2 nM, by preferentially binding to the C-type inactivated state of the channel. PAP-1 is 23-fold selective over Kv1.5, 33- to 125-fold selective over other Kv1-family channels, and 500- to 7500-fold selective over Kv2.1, Kv3.1, Kv3.2, Kv4.2, HERG, calcium-activated K+ channels, Na+,Ca2+, and Cl- channels [1]. The blockade of Kv1.3 results in membrane depolarization and inhibition of TEM proliferation and function. In this study, the in vitro effects of PAP-1 on T cells and the in vivo toxicity and pharmacokinetics (PK) were examined in rhesus macaques (RM) with the ultimate aim of utilizing PAP-1 to define the role of TEMs in RM infected with simian immunodeficiency virus (SIV). Electrophysiologic studies on T cells in RM revealed a Kv1.3 expression pattern similar to that in human T cells. Thus, PAP-1 effectively suppressed TEM proliferation in RM [2].in vivo: PAP-1 does not exhibit cytotoxic or phototoxic effects, is negative in the Ames test, and affects cytochrome P450-dependent enzymes only at micromolar concentrations. PAP-1 potently inhibits the proliferation of human TEM cells and suppresses delayed type hypersensitivity, a TEM cell-mediated reaction, in rats [1]. When administered intravenously, PAP-1 showed a half-life of 6.4 hrs; the volume of distribution suggested extensive distribution into extravascular compartments. When orally administered, PAP-1 was efficiently absorbed. Plasma concentrations in RM undergoing a 30-day, chronic dosing study indicated that PAP-1 levels suppressive to TEMs in vitro can be achieved and maintained in vivo at a non-toxic dose [2].

A potent, selective small molecule Mcl-1 inhibitor that selectively targets the BH3-binding groove of Mcl-1.

A potent, selective sodium-coupled citrate transporter (NaCT or SLC13A5) with IC50 of 0.51 uM, >20-fold selectivity over NaDC1 and NaDC3.

A potent, selective Src and Syk kinase inhibitor with IC50 of 29.3 uM and 2.5 uM, respectively.

A potent, selective STAT3 inhibitor that blocks STAT3 binding to its phosphopeptide ligand (IC50=20 uM) and inhibits IL-6-mediated phosphorylation of STAT3.

A potent, selective STAT3 inhibitor with IC50 of 9.7 uM, inhibits tyrosine phosphorylation of STAT3 with selectivity over STAT5 and STAT1 in cell-based assays.

A potent, selective STAT3 SH2 domain inhibitor (EC50=5.6 uM) that reduces STAT3 phosphorylation and nuclear transactivation.

A potent, selective TAAR1 agonist with Ki of 1.9, 2.7, 31 and 24 nM for mouse, rat, cynomolgus monkey and human TAAR1 stably expressed in HEK293 cells.

A potent, selective TAK1 inhibitor with IC50 of 8 nM, displays >33-fold and >62-fold selectivity over MEKK1 and MEKK4 respectively.

A potent, selective thrombopoietin (TPO) receptor agonist..

A potent, selective TLR9 antagonist with IC50 of 13 nM (human TLR9), displays 75-fold selectivity over TLR7 and no activity against TLR8 (IC50>10 uM).

A potent, selective transcriptional CDK inhibitor with Ki of 2.3 and 0.38 nM for CDK7 and CDK9, respectively.

A potent, selective translocator protein 18 kDa (TSPO/PBR) agonist with IC50 of 2.59 and 1.03 nM in competing with [3H]-PK11195 for binding to membrane preparations from rat cerebral cortex and ovary, respectively.

A potent, selective TRPC6 channel inhibitor with IC50 of 0.1-0.6 uM, 12- and 5-fold selectivity over related TRPC3 and TRPC7.

A potent, selective TRPM8 agonist with EC50 of 12 uM, a cooling agent.

A potent, selective ubiquitin-specific protease USP8 inhibitor with IC50 of 0.28 uM.

A potent, selective ubiquitin-specific protease USP8 inhibitor with IC50 of 0.56 uM.

A potent, selective ubiquitin-specific protease USP8 inhibitor with IC50 of 0.85 uM.

A potent, selective α2A-adrenoceptor antagonist with Ki of 1.7 nM, 80-fold selectivity over α2B-adrenergic receptors.

A potent, selective α2A-adrenoceptor antagonist with Ki of 1.7 nM, 80-fold selectivity over α2B-adrenergic receptors.

A potent, selective α2B adrenoceptor antagonist with pKd of 8.8, 200-fold selectivity over α2A, and α2D receptors.

A potent, selective, allosteric and oral mGluR1 antaognist with IC50 of 2.6 and 2.3 nM for human and rat mGluR1, respectively.

A potent, selective, allosteric and orally acitve positive modulator of small-conductance calcium-activated K+ channel KCa2.2 and KCa2.3 with EC50 of 1.6 and 0.14 uM, respectively.

A potent, selective, allosteric LMPTP inhibitor with IC50 of 1.68 uM, displays good selective against other phosphatases.

A potent, selective, and bioavailable OX2 receptor antagonist with Kb of 4.5 nM.

A potent, selective, and centrally active positive allosteric modulator of AMPAR-mediated neurotransmission, which increase ion channel flux in the presence of agonist by suppressing desensitization and/or deactivation of the receptors..

A potent, selective, and centrally active positive allosteric modulator of AMPAR-mediated neurotransmission, which increase ion channel flux in the presence of agonist by suppressing desensitization and/or deactivation of the receptors..

A potent, selective, and irreversible BTK inhibitor with IC50 of 7 nM.

A potent, selective, and irreversible inhibitor of SSAO/VAP-1 (AOC3) with Ki of 37 nM, IC50 of <10 nM.

A potent, selective, and orally bioavailable factor Xa (FXa) inhibitor for prevention and treatment of thromboembolic diseases..

A potent, selective, and orally bioavailable ghrelin receptor (GHSR) inverse agonist with binding pKi of 8.36.

A potent, selective, and orally bioavailable inhibitor of interleukin-1 receptor-associate kinase-4 (IRAK4) with IC50 of 2.8 nM, 217- and 892-fold selectivity over IRAK-1 and TAK1, respectively.

A potent, selective, and orally efficacious pan-Pim inhibitor with IC50 of 5/25/16 nM for Pim1/2/3, respectively.

A potent, selective, ATP competitive AKT inhibitor with IC50 of 2.3 uM for Akt1.

A potent, selective, ATP-competitive and orally acitve Rho kinase inhibitor with IC50 of 33.1 and 8.5 nM for ROCK1 and ROCK2, respectively.

A potent, selective, ATP-competitive and orally bioavailable inhibitor of VEGFR-2 with Ki of 0.7 and 8.8 nM for unactivated and fully phosphorylated VEGFR-2, respectively.

A potent, selective, ATP-competitive inhibitor of IKKβ kinase with Ki of 2 nM.

A potent, selective, ATP-competitive inhibitor of IKKβ kinase with Ki of 2 nM.

A potent, selective, ATP-competitive inhibitor of MAP4K4 with IC50 of 1.9 uM, without effect on other stress pathway related kinases.

A potent, selective, ATP-competitive ITK inhibitor with IC50 of 19 nM.

A potent, selective, brain penetrant and orally active mGluR1 antagonist with 4.3 nM and 3.6 nM for huam and rat mGluR1, respectively.

A potent, selective, brain penetrant partial negative allosteric modulator of mGlu5 receptor with Ki of 14 nM, Ca assay IC50 of 32 nM.

A potent, selective, brain penetrant PDE10A inhibitor with Ki of 4 nM.

A potent, selective, brain penetrant phosphodiesterase 2A (PDE2A) inhibitor with IC50 of 2 nM, >4,000-fold selectivity over PDE1 and PDE3-11.

A potent, selective, brain penetrant, orally acitve mGluR7 allosteric agonist that inhibits forskolin-stimulated cAMP accumulation in mGluR7b CHO cells with EC50 of 64±32 nM.

A potent, selective, brain permeable, orally available glycine transporter-1 (GlyT1) inhibitor with IC50 of 92 nM (rat GlyT1), 50-fold selectivity over GlyT2.

A potent, selective, cell active SHP2 inhibitor with IC50 of 200 nM, displays >5-fold selectivity against 20 other mammalian PTPs.

A potent, selective, cell-active CBP/EP300 bromodomain inhibitor with IC50 of 0.47 uM for CBP.

A potent, selective, cell-permeable I338G v-Src inhibitor with IC50 of 430 nM, shows no inhibition of wild-type v-Src at 300 uM.

A potent, selective, CNS penetrant 5-HT2C receptor agonist with Ki of 3 nM and EC50 of 9 nM, without significant P-gp efflux liability.

A potent, selective, CNS penetrant and competitive orthosteric antagonist of M1 mAChR with IC50 of 132 nM, >75-fold selectivity over M2-M5.

A potent, selective, CNS penetrant and orally bioavailable mGlu5 positive allosteric modulator that potentiates human mGlu5 with EC50 of 130 nM.

A potent, selective, CNS penetrant and orally bioavailable mGlu5 positive allosteric modulator that potentiates human mGlu5 with EC50 of 260 nM.

A potent, selective, CNS-penetrant P2X7 antagonist with pKi of 9.1 and 7.9 for rat and huamn P2X7 channel, respectively.

SW106 is a potent, selective, competitive PTH/PTH-related peptide receptor (PPR) antagonist with IC50 of 0.99 uM.

A potent, selective, covalent KRAS G12C inhibitor that selectively inhibit KRAS G12C-dependent signaling and cancer cell growth at sub-micromolar concentrations..

A potent, selective, dual CysLT1 and CysLT2 antagonist with IC50 of 17 and 0.87 nM, respectively..

A potent, selective, highly CNS-penetrant and orally available mGluR5 negative allosteric modulator Kd of 2.8 nM.

A potent, selective, highly CNS-penetrant mGluR5 antagonist.

A potent, selective, irreversible sigma-2 receptor partial agonist with Ki of 14.6 nM, >700-fold selectivity over sigma-1 receptors.

A potent, selective, low glutamate fold shift (2.4) mGluR5 positive allosteric modulator with EC50 of 2.6 nM, without inherent mGluR5 agonist activity (EC50>30 uM).

A potent, selective, non-ATP-competitive inhibitor of p38α-mediated MK2a phosphorylation with apparent Ki of 330 nM.

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.