A potent and selective melanocortin 4 receptor (MC4R) agonist with EC50 of 2.1 nM.

A potent and selective mTOR inhibitor with Ki of 1.5 nM.

A potent and selective NIMA-related Kinase 2 (NEK2) inhibitor with IC50 of 22 nM, >200-fold selectivity over Plk1, Mps1, Aurora A and CDK2.

A potent and selective non-peptide antagonist of the neurokinin A (NK2) receptor.

A potent and selective PDE10A inhibitor with binding affinity (Kd) of 0.15 nM, IC50 of 2.11 nM.

A potent and selective PDE10A inhibitor with IC50 of 7.28 nM.

A potent and selective RARγ receptor agonist with Ki of 150 nM.

A potent and selective ROCK inhibitor with Ki of 1.6 nM.

UNC-1679 (UNC1679) is a potent and selective small molecule chemical probe of a methyl-lysine reader protein L3MBTL3 with Ki of 0.35 uM.

A potent and selective small-molecule inhibitor of Lck with IC50 of 147 nM.

A potent and selective TAAR1 partial agonist with Ki of 0.5, 1.0, 6.8 and 2.6 nM for mouse, rat, human and monkey TAAR1, respectively.

A potent and selective tachykinin NK1 receptor antagonist with Ki of 2.9 nM.

A potent and selective TGF-βRI (ALK5) inhibitor with IC50 of 34 nM, prevents tissue hyperplasia in the rat urethra or common iliac artery..

A potent and selective TGF-βRI (ALK5) inhibitor with IC50 of 34 nM, prevents tissue hyperplasia in the rat urethra or common iliac artery..

NNC 55-0396, Mibefradil derivative, is a highly selective T-type calcium channel blocker; displays IC50 values of 6.8 and > 100 μM for inhibition of Cav3.1 T-type channels and HVA currents respectively in INS-1 cells. IC50 value: 6.8 nMTarget: Cav3.1 T-type channelNNC 55-0396 can be an essential tool in preventing human ovarian cancer cell proliferation as a result of its ability to inhibit the function of T-type Ca2+ channels. It is believed that NNC 55-0396 may functions by dissolving in or passing through the plasma membrane of cells.

A potent and selective type III phosphatidylinositol 4-kinase (PI4KIIIβ) inhibitor with IC50 of 3.6 nM.

A potent and selective VEGFR2 (KDR) inhibitor with IC50 of 40 nM.

A potent and selective VEGFR2 (KDR) inhibitor with IC50 of 40 nM.

A potent and selective α4β2 nAChR agonist with Ki of 16 nM.

A potent and selective δ-opioid receptor agonist that has high affinity and selectivity for the δ1 subtype with Ki of 1.12 nM.

A potent and selective, CNS penetrant mGlu2 negative allosteric modulator with IC50 of 78 nM.

A potent and selective, CNS penetrant mGlu3 negative allosteric modulator with IC50 of 245 nM.

A potent and selective, CNS-penetrant PDE1 inhibitor with IC50 of 2.4 nM for PDE1B..

A potent and selective, CNS-penetrant PDE1 inhibitor with IC50 of 35 nM for PDE1B..

A potent and selective, non-ATP competitive, allosteric MAPKAPK2/3 (MK2/3) inhibitor with IC50 of 8 nM for MK2, hTNFα EC50 of 0.31 uM.

A potent and selective, orally bioavailable aromatase inhibitor with IC50 of 1.7 nM, 180 times more potent than aminoglutethimide.

A potent and selective, orally bioavailable JAK2 inhibitor with IC50 of 2 nM.

A potent and selective, orally bioavailable, reversible BTK inhibitor with IC50 of 2.8 nM.

A potent and specific antagonist of platelet activating factor (PAF) receptor that inhibits PAF-induced human platelet and neutrophil aggregation in vitro with IC50 of 0.17 and 0.36 uM, respectively.

A potent and specific BET bromodomain inhibitor with Ki of 3.2-24.7 nM for BD1 and BD2 domains of BRD2, BRD3, and BRD4.

RS102895 is a potent CCR2 antagonist, with an IC50 of 360 nM, and shows no effect on CCR1.

A potent and specific CCR6 antagonist.

OSU-T315 (ILK-IN-1) is a potent and specific integrin-linked kinase (ILK) inhibitor which inhibits PDK2 function in the AKT pathway activation

A potent and specific nuclear export inhibitor that binds to and inhibits CRM1 (XPO1).

A potent and specific, nonlipid agonist of LPA2 receptor with EC50 of 100 nM, without activating or inhibiting LPA1/3/4/5 receptors.

Proxalutamide (GT-0918) is a nonsteroidal antiandrogen (NSAA) – specifically, a selective high-affinity silent antagonist of the androgen receptor (AR) for the potential treatment of COVID-19, prostate cancer, and breast cancer.

A potent anthrax lethal toxin entry inhibitor with IC50 of 1.7 uM, inhibits endosomal trafficking pathways exploited by multiple toxins and viruses.

A potent anticancer agent that demonstrates potent antitumor activity in vitro against several cancer cell lines as well as in vivo against several tumor models, effectively inhibits in vitro tubulin polymerization. .

A potent bactericidal agent that inhibits the KinA autophosphorylation with IC50 of 1.6 uM.

A potent BCL6 protein-protein interaction inhibitor with Kd of 78 nM.

A potent benzodiazepine inverse agonist that displays anxiogenic and potent convulsant activity.

A potent blocker of high-conductance Ca2+-activated K+ (BKCa, KCa1.1) channels that binds to the α-subunit of BKCa with Ki of 1.9 nM.

A potent blocker of voltage-gated potassium channels Kv7 (KCNQ) that enhances ACh release from rat hippocampal slices in vitro with EC50 of 0.7 uM.

A potent calcium sensing receptor (CaSR) negative allosteric modulator with IC50 of 146 nM for hCaSR.

A potent calcium sensing receptor (CaSR) negative allosteric modulator with IC50 of 146 nM for hCaSR.

A potent Caspase-6 inhibitor with IC50 of 192 nM, also inhibits Caspase-4/8/9/10 with IC50 of 0.1-0.8 uM.

A potent CCR2 specific antagonist that blocks MCP-1 mediated response with an IC50 of 3.2 nM.

A potent CCR4 antagonist that blocked CCL22- and CCL17-mediated migration of human peripheral blood CD4+CD25+ Treg and Th2 cells ex-vivo and murine Tregs in-vivo.

A potent CCR4 antagonist that blocked CCL22- and CCL17-mediated migration of human peripheral blood CD4+CD25+ Treg and Th2 cells ex-vivo and murine Tregs in-vivo..

A potent CDK1 and CDK2 inhibitor with IC50 of 9.5 nM and 5.4 nM against CDK1/cyclinB and CDK2/cyclinA3 respectively.

A potent chelator of iron that arrests late stages of cytokinesis by blocking the physical process of constriction in dividing cells.

A potent CYP26A1 inhibitor with IC50 of 10 nM, potently inhibits all-trans-retinoic acid metabolism in intact T47D cells with IC50 of 8.7 nM.

Beaucage reagent is a DNA cleavage reagent.

A potent dopamine D2 receptor antagonist with Ki of 28 nM.

A potent dopamine D2 receptor antagonist with Ki of 28 nM.

A potent dopamine stabilizer with Ki of 447 and 1305 nM for D2 and D3 receptors respectively.

A potent dual H3/H2 receptor antagonist with Ki of 0.07 and 7.8 uM, respectively.

A potent dual inhibitor of EGFR and ErbB2.

A potent G2 checkpoint inhibitor that specifically abrogates the DNA double-stranded break (DSB)-induced G2 checkpoint.

A potent GIRK2 inhibitor that inhibits GIRK2-mediated flux with an IC50 of 0.35 uM.

A potent glucagon receptor (GCGR) negative allosteric modulator..

A potent glutaminyl cyclase (QC) inhibitor with Ki of 60 nM.

A potent GSK3β inhibitor with IC50 of 22 nM.

A potent gucokinase (GK) activator with EC50 of 0.29 uM.

Daclatasvir is an orally available antiviral agent that inhibits the NS5A region of the hepatitis C virus (HCV) and is used in combination with other oral antiviral agents to treat chronic hepatitis C. Elevations in serum enzyme levels during daclatasvir therapy are uncommon, and it has yet to be convincingly implicated in cases of clinically apparent liver injury with jaundice. Nevertheless, and for unknown reasons, successful all-oral regimens of antiviral therapy in patients with chronic hepatitis C and cirrhosis is occasionally complicated by hepatic decompensation and may cause reactivation of hepatitis B in susceptible patients coinfected with the hepatitis B virus (HBV).

A potent HCV NS5B RNA polymerase inhibitor.

A potent HDAC inhibitor with IC50 of 172 nM.

A potent HDAC inhibitor with IC50 of 27 nM (HeLa cell extracts).

A potent hERG channel activator that concentration-dependently increases the hERG current (2.1 and 3.4-fold at 3 and 10 uM, respectively) and markedly slows hERG channel deactivation and inactivation.

A potent HIF-2α inhibitor with IC50 of <500 nM in HIF-2α scintillation proximity assay. .

A potent histamine 1 receptor antagonist..

A potent HIV-1 entry inhibitor that blocks the gp120-CD4 interaction.

A potent Hsp90α/p23 interaction inhibitor with IC50 of 0.15 uM, more effective than CP-9 in degrading pAkt/total Akt and Raf-1.

A potent Hsp90α/p23 interaction inhibitor with IC50 of 3.2 uM.

A potent human indoleamine 2,3-dioxygenase 2 (IDO2) inhibitor with Ki of 0.97 uM, also exhibits significant antitrypanosomal activities with EC50 of 0.82 uM..

A potent inhibitor of developmental angiogenesis in the zebrafish eye, and a cysteinyl leukotriene 1 and 2 receptor (CysLT1 and 2) antaognist with IC50 of 1.2 and 52 uM, respectively.

A potent inhibitor of drug-resistant S31N mutant of the M2 ion channel of influenza A virus with IC50 of 153 nM.

A potent inhibitor of HDAC1/3/6 with IC50s of 43-72 nM.

A potent inhibitor of HIV-1 integrase-LEDGF/p75 interaction.

A potent inhibitor of hTGase (Tissue transglutaminase) with IC50 of 0.8 uM.

ISO-1 is a macrophage migration inhibitory factor (MIF) antagonist with an IC50 of 7 μM.

A potent inhibitor of MLL1/WDR5 protein-protein interaction with IC50 of 0.9 nM.

Elacridar Hcl (GF120918; GW0918) is a P-glycoprotein inhibitor, and has been used both in vitro and in vivo as a tool inhibitor of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules.IC50 value:Target: P-glycoprotein In vitro, GF120918A demonstrated high plasma protein binding across species, although a definitive protein binding evaluation was precluded by poor recovery, particularly in buffer and in mouse, rat, and dog plasma. GF120918A did not demonstrate potent inhibition of several human cytochrome P450 enzymes evaluated in vitro, with IC(50) values well above concentrations anticipated to be achieved in vivo. Together, these data confirm the utility of GF120918A as a tool P-glycoprotein inhibitor in preclinical species and offer additional guidance on preclinical dose regimens likely to produce P-glycoprotein-mediated effects.

A potent inhibitor of sEH (soluble epoxide hydrolase) with IC50 of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively.

A potent inhibitor of sEH (soluble epoxide hydrolase) with IC50 of 18 nM and 69 nM for mouse sEH and human sEH, respectively.

A potent inhibitor of the mRNA decapping scavenger enzyme (DcpS) with IC50 of 0.11 nM.

A potent inhibitor of TrkA with IC50 of 2.9 nM, also inhibits TrkB, TrkC.

A potent inhibitor of tumor promoting phorbol ester TPA/PMA and inhibitor of Ca2+/calmodulin dependent EF-2 phosphorylation

A potent inhibitors of Botulinum Neurotoxin A (BoNT) Light Chain with IC50 of 0.9 uM..

A potent integrin αvβ3 antagonist with IC50 of 18 nM.

A potent Kv11.1 (hERG) channel allosteric modulator that protects cardiac tissue from hERG-related drug-induced arrhythmias.

NS5806 is a potent potassium current activator, increases KV4.3/KChIP2 peak current amplitudes with an EC50 of 5.3 μM. NS5806 slows KV4.3 and KV4.2 current dacay in channel complexes containing KChIP2[1].

A potent lipid peroxidation inhibitor that has antishock and endothelial protective actions.

Cevimeline HCl is a cholinergic agonist that binds to muscarinic receptors. Muscarinic agonists in sufficient dosage can increase secretion of exocrine glands, such as salivary and sweat glands, and increase tone of the smooth muscle in the GI and urinary tracts.

Cevimeline is a parasympathomimetic and muscarinic agonist that affects M1 and M3 receptors. It is used in the treatment of dry mouth and Sjögren's syndrome. Cevimeline has also been shown to reduce Xerostomia symptoms and increase salivary flow in head and neck cancer survivors after radiotherapy.

A potent matrix metalloproteinase (MMP) inhibitor..

A potent melanocortin MC3 and MC4 receptor antagonist with IC50 of 0.23 nM and 0.06 nM, respectively.

A potent microtubule inhibitor that not only inhibits the expression levels of HIF-1α protein but also destabilizes HIF-1α mRNA.

A potent mutant c-Src T338C kinase inhibitor with IC50 of 317 nM.

A potent mutant Src T338C inhibitor with IC50 of 111 nM.

A potent neutral endopeptidase EC 3.4.24.11 (atriopeptidase) inhibitor that increases endogenous ANF levels and produces natriuretic and diuretic responses intravenously in mice..

A potent non-peptide antagonist of tachykinin NK2 receptor with pKi of 9.5 in CHO cells.

A potent Nrf2 activator that upregulates Nrf2 expression and resulted in translocation of Nrf2 into the nucleus..

A potent nucleoside analog reverse transcriptase inhibitor (nRTI). An analog of cytidine that can inhibit both types (1 and 2) of HIV reverse transcriptase as well as the reverse transcriptase of hepatitis B. Needs to be phosphorylated to its triphosphate

A potent pan HER/VEGFR inhibitor with IC50 of 5/20/60/50 nM for EGFR/HER2/ERBB4/VEGFR2 respectively.

A potent pan-HDAC inhibitor with IC50 of 16-30 nM, inhibits cell proliferation of P815, C2, and BR cells with IC50 of 0.65, 0.30, and 0.23 uM, respectively.

A potent PD-1/PD-L1 interaction inhibitor with IC50 of 2.25 nM in a homogenous time-resolved fluorescence binding assay..

A potent PD-1/PD-L1 interaction inhibitor with IC50 of 2.25 nM in a homogenous time-resolved fluorescence binding assay..

A potent PD-1/PD-L1 interaction inhibitor with IC50 of 6-100 nM in a homogenous time-resolved fluorescence binding assay..

A potent PD-1/PD-L1 interaction inhibitor with IC50 of 80 nM in a homogenous time-resolved fluorescence binding assay..

A potent PDE4 inhibitor with IC50 of 94.5 nM..

A potent PfDHODH inhibitor that exhibits low nanomolar in vitro potency against DHODH from P falciparum, P vivax, and P berghei.

A potent phosphodiesterase 12 (PDE12) with Ki of 17.5 nM, with no activity for related enzyme CNOT6 (Ki>10 uM).

A potent photoaffinity ligand for the peripheral-type benzodiazepine binding site with Ki of 4 nM.

A potent PI3K inhibitor with IC50 3 nM, does not inhibit PI4K activity.

A potent PIKfyve inhibitor that inhibits autophagy by impairing lysosomal maturation, potently and reversibly inhibits autophagosome-lysosome fusion by activating RAB5A.

A potent protein tyrosine kinase inhibitor that shows selectivity for PDGFR in vitro and in cells.

A potent psychopharmacologic agent that shows high affinity for 5-HT, dopamine, histamine and adrenoceptors.

A potent RIG-I-like receptor (RLR) agonist that triggers IRF3-dependent innate immune antiviral genes and IFN-β expression.

A potent small molecule inhibitor of MELK kinase activity with IC50 of 42 nM.

A potent small-molecule inhibitor of the MIR155 host gene/miR-155 axis.

A potent SR-3 antagonist

A potent Src inhibitor extracted from patent WO/2012003544A1..

A potent STAT5 inhibitor with a dual mechanism of action, potently inhibits STAT5 through liberation of endogenous phosphatase activity following NADPH oxidase (NOX) inhibition at 200-300 nM.

A potent TLR7 agonist with EC50 of 59 nM..

A potent TLR7 agonist with EC50 of 8.6 nM. .

3M-011 is a potent TLR7/8 agonist and cytokine inducer; stimulates type I interferon (IFN) and other cytokines such as TNF-alpha, IL-12, and IFN-gamma from rat peripheral blood mononuclear cells; induces IL-12 and COX-2 expression in mDC from HIV+ and HIV- individuals, and inhibits H3N2 influenza viral replication in the nasal cavity; potentiates NK cytotoxicity, and shows antitumor effects in scid/B6 mice and scid/NOD mice.

A potent TLR7/8 agonist that induces robust production of the Th1-polarizing cytokines TNF-alpha and IL-12 from neonatal antigen-presenting cells (APCs)..

A potent TNFα/TNFRc1 interaction antagonist with IC50 of 50 nM, with no affinity for the related cytokine receptors TNFRc2 or CD40, and no cytotoxicity (>100 uM).

A potent tubulin inhibitor that is a toxin payload in antibody drug conjugates (ADCs)..

A potent tyrosine kinase inhibitor targeting c-Kit and PDGFR with IC50 of 0.15 and 0.05 uM in cell based assays.

A potent tyrosine kinases inhibitor with IC50 of 13/9/3/26/2 nM for Lck/Btk/Lyn/Syk/Txk..

A potent γ-secretase inhibitor that preferentially inhibits cleavage of the APP CTF cleavage with IC50 of 7.1 nM.

A potent, allosteric HIV integrase inhibitor (Kd=34 nM) that binds the LEDGF/p75 binding site on integrase.

A potent, allosteric inhibitor of CBFβ-RUNX1 interaction with IC50 of 3.2 uM in FRET assays.

A potent, and selective Bax agonist (Ki=43.3 nM) that induces conformational changes in Bax by blocking S184 phosphorylation.

A potent, and selective FAAH inhibitor with IC50 of 18 nM.

A potent, and selective GluR5-subunit containing kainate receptor antagonist with Kd of 402 nM.

A potent, ATP-competitive and relative selective Nek2 inhibitor with IC50 of 0.27 uM.

A potent, biased allosteric agonist of CXCR3 (pEC50=5.22) that activates solely G proteins, induces chemotaxis, but fails to induce receptor internalization or β-arrestin 2 recruitment..

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..

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

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, 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.

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, 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 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..

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, 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, 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..

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.