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.

A potent, selective inhibitor of the Na+/citrate transporter NaCT (SLC13A5) that shows inhibition of citrate uptake in the HEKNaCT cells with IC50 of 0.41 uM.

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).

CLP257 (CLP-257) is a potent, selective K+-Cl- cotransporter KCC2 activator with EC50 of 616 nM; displays selectivity for KCC2 over other KCC family members, NKCC1 and GABAA receptors, and a panel of 55 other receptors; restores impaired Cl(-) transport i

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

A potent, selective KDM5 sub-family(JARID1) inhibitor with biochemical IC50 of 71/19/69/69 nM for KDM5A/B/C/D, respectively.

A potent, selective ligand for the mitochondrial translocator protein 18kDa (TSPO/PBR).

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.

A potent, selective MMP-2 inhibitor with Ki of 230 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 P. falciparum dihydroorotate dehydrogenase (PfDHODH) with IC50 of 53 nM.

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 PLK1 PBD inhibitor with IC50 of 1.36 uM.

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 renal outer medullary potassium channel (ROMK, Kir1.1) inhibitor with IC50 of 0.24 uM in T1+ flux assays.

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

A potent, selective S1P3 antagonist with Ki of 0.25 nM.

A potent, selective S1P3 antagonist with Ki of 0.25 nM.

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 CCR2 antagonist with binding IC50 of 5.1 nM.

A potent, selective, allosteric CCR2 antagonist with IC50 of 103 nM..

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 oral renal outer medullary potassium channel (ROMK) inhibitor with IC50 of 68 nM.

A potent, selective, and orally active p53-MDM2 antagonist with IC50 of 6 nM.

A potent, selective, and orally active p53-MDM2 antagonist with IC50 of 7 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 Chk1 and Chk2 inhibitor with IC50 of 4.4 nM and 4.5 nM, respectively.

A potent, selective, ATP-competitive Chk1 inhibitor with IC50 of 13.3 nM.

A potent, selective, ATP-competitive c-MET inhibitor with IC50 of 0.93 nM.

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 PDE9A inhibitor with IC50 of 1.8 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, brain-penetrant and orally bioavailable mGluR4 positive allosteric modulator with EC50 of 79 nM.

A potent, selective, brain-penetrant and orally bioavailable mGluR4 positive allosteric modulator with EC50 of 79 nM.

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 permeab anti-apoptotic protein kinase CK2 with Ki of 5 nM.

BAY-678 is a cell-permeable inhibitor of human neutrophil elastase (HNE).

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 dual leucine zipper kinase (DLK, MAP3K12) inhibitor with Ki of 3 nM.

A potent, selective, CNS penetrant, orally bioavailable RORγt with pIC50 of 8.3 in FRET assays.

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, competitive, orally active dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 13 nM.

A potent, selective, competitive, orally active dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 13 nM.

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, full agonist of human and murine MC1R with EC50 of 16.8 and 11.6 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 EGFR mutants with IC50 of 12, 3, 4 and 5 nM for EGFR L858R-T790M, Del-T790M, L858R, and EGFR Del, respectively.

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, noncompetitive, orally active CCR2 antagonist with IC50 of 172 nM.

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, non-peptide NK1 receptor antagonist with Ki of 0.74 nM, IC50 of 1.6 nM.

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 agonist of dopamine D3 receptor with EC50 of 21 nM.

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.

A potent, selective, orally active BACE1 inhibitor for the treatment of Alzheimer's disease..

A potent, selective, orally active BACE1 inhibitor with IC50 of 0.7 nM, demonstrates limited selectivity for over BACE2 and high selectivity both renin and pepsin.

A potent, selective, orally active bombesin receptor subtype-3 (BRS-3) agonist with EC50 of 250/100 nM for human/rat BRS-3, resp+H1437+M1438.

A potent, selective, orally active bombesin receptor subtype-3 (BRS-3) agonist with EC50 of 270/130 nM for human/rat BRS-3, respectively.

A potent, selective, orally active cannabinoid CB2 receptor inverse agonist with Ki of 35.9, 1.55 and 0.38 nM for human, mouse and rat CB2, respectively.

A potent, selective, orally active Chk1 inhibitor with IC50 of < 1 nM, Ki=69 pM.

A potent, selective, orally active cholecystokinin receptor 2 (CCK2) antagonist with IC50 of 2 nM.

A potent, selective, orally active EGFR inhibitor with IC50 of 23 nM.

A potent, selective, orally active inhibitor of cathepsin K with Ki of 0.1 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively.

A potent, selective, orally active monopolar spindle 1 (MPS1) inhibitor with IC50 of 3 nM, with no activity for CDK2 and Aurora A (IC50>40 uM).

A potent, selective, orally active Mps1 (TTK) inhibitor with IC50 of 3.1 nM.

PF-1355 is a potent, selective, orally active Myeloperoxidase (MPO) inhibitor with EC50 of 1.47 uM.

A potent, selective, orally active neurokinin 3 (NK3R) antagonist for the treatment of schizophrenia.

Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.

A potent, selective, orally active nociceptin opioid receptor (NOP) agonist with EC50 of 12 nM, Ki of 0.3 nM.

A potent, selective, orally active orexin-2 receptor (OX2R) antagonist with pKi of 8.0 and 8.1 for human and rat OX2R, respectively.

A potent, selective, orally active p110δ/γ PI3K dual inhibitor with cellular IC50 of 0.29 and 7.1 nM, respectively.

A potent, selective, orally active p38α/p38β inhibitor with IC50 of 11.2/36.5 nM respectively, with no effect on p38γ and δ isoforms (IC50>1 uM).

A potent, selective, orally active S1P receptor-1 (S1P1) agonist with EC50 of 1.1 nM, 320-fold selectivity over S1P3.

A potent, selective, orally active S1P1 antagonist with IC50 of 2.5 nM Ca2+ mobilization assays, without activity on S1P2, S1P3 and S1P4 (IC50>10 uM).

A potent, selective, orally active somatostatin receptor SSTR3 antagonist with binding Ki of 0.66 nM, >500-fold selectivity over SSTR1/2/4/5.

A potent, selective, orally active somatostatin receptor SSTR3 antagonist with binding Ki of 2.3 nM, >2,500-fold selectivity over SSTR1/2/4/5 (IC50>5 uM).

A potent, selective, orally active TAAR1 partial agonist with Ki of 6 nM, EC50 of 23 nM (hTAAR1), 140-fold selectivity over β2 adrenergic receptors.

A potent, selective, orally active TRPA1 channel antagonist with IC50 of 71 and 131 nM for rTRPA1 and hTRPA1 in Ca2+ flux assays respectively, without agonist activity (EC50>40 uM).

A potent, selective, orally active TRPM8 channel antaognist with IC50 of 0.8 nM, .

A potent, selective, orally active γ-secretase modulator with Aβ42 IC50 of 39 nM.

A potent, selective, orally active, small-molecule antagonist of human glucagon receptor with Ki of 6.66 nM.

A potent, selective, orally available CX3C chemokine receptor 1 (CX3CR1) modulator that inhibits the fractalkine-induced chemotaxis of human peripheral blood NK cells with IC50 of 4.9 nM.

A potent, selective, orally available GlyT1 inhibitor with IC50 of 1.6 nM, weakly inhibits rat GlyT2 (IC50=138 nM).

A potent, selective, orally available GlyT1 inhibitor with IC50 of 29 nM, demonstrates excellent in vivo occupancy of GlyT1 transporters in vivo..

PF-0346275 is a potent, selective, orally available GlyT1 inhibitor with Ki of 11.6 nM, without activity against GlyT2 (IC50>10 uM).

A potent, selective, orally available GPR40 agonist with EC50 of 3.7 nM.

A potent, selective, orally available GPR40 agonist with EC50 of 8 nM.

A potent, selective, orally available GPR40 agonist with EC50 of 9 nM.

A potent, selective, orally available GPR40 agonist with Ki of 15 nM, β-arrestin EC50 of 108 nM.

A potent, selective, orally available IAP antagonist with IC50 of 1.3, 2.2 and 200 nM for cIAP-1, cIAP-2 and XIAP, respectively.

A potent, selective, orally available inhibitor of both native and mutant Bcr-Abl with IC50 of 20-80 nM.

A potent, selective, orally available inhibitor of HCV NS3/4A protease with Ki of 0.05 and 0.9 nM for GT1b and 2a protease, respectively.

A potent, selective, orally available RIPK2 inhibitor with IC50 of 3 nM.

Avacopan is a potent, selective, orally availale C5aR (CD88) inhibitor with IC50 of 0.1 nM.

A potent, selective, orally bioavailable BET bromodomain inhibitor with IC50 of 7.2 and 28.2 nM for BRD4 BD2 and BRD4 BD1, respectively.

A potent, selective, orally bioavailable GPR120 agonist with EC50 of 42 nM in calcium flux assays.

JNJ-39758979 is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity.

A potent, selective, orally bioavailable inhibitor of class I PI3K isoforms with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/β/δ/γ, respectively.

A potent, selective, orally bioavailable inhibitor of CXCR4 that efficiently inhibits SDF-1α binding to CXCR4 with IC50 of 0.61 nM.

A potent, selective, orally bioavailable inhibitor of EZH2 with Ki of < 3 nM.