Muscarinic antagonist; inhibiting ACh-induced Ca(2+) responses at rat M(1-5) receptor subtypes

Novel positive allosteric modulator (PAM) of mGlu4

Allosteric modulator of the M2/5 muscarinic acetylcholine receptor

Highly M1-selective antagonist

Novel M4 muscarinic acetylcholine receptor modulator

Novel mGlu4 positive allosteric modulator (PAM)

Novel negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety

Highly selective muscarinic M1 PAM

Selective orthosteric M1 antagonist

Novel, CNS Penetrant Glucagon-Like Peptide 1 Receptor (GLP-1R) Positive Allosteric Modulator (PAM)

Novel potent and selective metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulator (PAM)

Potent and selective mGlu5 negative allosteric modulator (NAM)

Novel potent mGlu4 PAM with an attractive DMPK profile, and robust efficacy in preclinical Parkinsons disease model, haloperidol-induced catalepsy (HIC)

mGlu1 positive allosteric modulator (PAM)

Novel cyclooxygenase-1 (COX-1)-selective inhibitor

Novel modulator of mammalian inward rectifying potassium (Kir) channels

Novel selective negative allosteric modulator (NAM) of metabotropic glutamate receptor subtype 2

Novel potent and highly selective mGlu1 PAM (22nM), reducing striatal DA release in vivo and displaying antipsychotic efficacy

Novel Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM)

Novel Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM)

Novel M4 positive allosteric modulator (PAM)

Novel CNS penetrant pan-muscarinic antagonist

Novel PAM of Group III (mGlu4/6/7/8) mGlu receptors

Novel selective mGlu3 NAM, showing efficacy in tail suspension, elevating zero maze and marble burying, suggesting selective inhibition of mGlu3 affords anxiolytic-like and antidepressant-like phenotypes in mice

First-in-class selective mGlu7 positive allosteric modulator (PAM), displaying CNS penetration in both mice (Kp = 2.74) and rats (Kp= 4.78)

Potent histamine H3 receptor silent antagonist

Novel full inverse agonist at CXCR3 N3.35A

Potent H4R ligand

Novel potent ligand at 5-HT3A and 5-HT3AB receptors with different activities

VUF10497 is a potent histamine H4 receptor (H4R) inverse agonist with anti-inflammatory activity.

Potent human H4 receptor inverse agonist

Highly Potent Human Histamine H4 Receptor Inverse Agonist

Potent CXCR3 Antagonist, extending from the minor pocket into the major pocket of the transmembrane domains and binding between residues in helices 1 (Y1.39), 2 (W2.60), 3 (F3.32), 4 (D4.60), 6 (Y6.51), and 7 (S7.39, Y7.43)

First reported nonpeptidomimetic agonist on The G protein-coupled chemokine receptor CXCR3

Partial agonist in hH 4 R-mediated G protein signalling and β-arrestin2 recruitment, bounding covalently to the hH4R

Novel robust and fatigue-resistant photoswitchable GPCR antagonist

Novel robust and fatigue-resistant photoswitchable GPCR antagonist

Novel inhibitor of Hbp secretion, activating σE stress, impairing Hbp secretion and decreasing the abundance of OMPs, consistent with impaired BAM function

Novel photoswitchable modulator of the CXCR3 chemokine receptor

Novel CXCR3 ligand, photoswitching from antagonism to agonism

Novel photoswitchable modulator of the CXCR3 chemokine receptor

Histamine H3 receptor antagonist

H3R inverse agonist

Adenosine A3 receptor (A3AR) allosteric modulator

Novel full inverse agonist at CXCR3 N3.35A

Full agonist of hH4R with ~300-fold selectivity over hH3R and hH2R, but showing potent inverse agonistic activity at hH1R

Potent histamine H4 receptor full agonist

Allosteric modulator of A3 adenosine receptors

Multidrug resistance inhibitor

Novel Probe of Putative MOR-CCR5 Heterodimers to Inhibit Opioid Exacerbated HIV-1 Infectivity

W-13 hydrochloride is a calmodulin antagonist. W-13 hydrochloride can inhibit Tamoxifen (HY-13757A)-resistant human breast cancer cell growth.

Calmodulin antagonist, inhibiting Ca2+/calmodulin-regulated enzyme activities

Mixed competitive/noncompetitive inhibitor of

Nocel inhibitor of BMI1 promoter activity, decreasing BMI1 protein levels in HCT116 human colon carcinoma cells, significantly reducing levels of the CSC biomarker epithelial cell adhesion molecule and diminishing the self-renewal capability of CSCs

Very late adhesion molecule 4 (VLA-4) antagonist, inhibiting VLA-4/VCAM-1 ligation as a means of modulating eosinophil functions beyond its action on cell adhesion and migration

SGLT2 inhibitor

ATP-sensitive potassium channel opener

Inhibitor of human collagenase-3 (MMP-13)

Potent and selective inhibitor of matrix metalloprotease MMP-13 (Collagenase-3)

Inhibitor of matrix metalloproteinase-1 (MMP-1)

Potent and Selective Inhibitor of the Norepinephrine Transporter

Secreted frizzled-related protein-1 (sFRP-1) modulaitor

Novel inhibitor of The epidermal growth factor receptor (EGFR), decreasing NSCLC cell proliferation and colony formation, by causing G2/M arrest and apoptosis.

Non-peptide GLP-1 receptor agonist, blocking inflammatory nociception by stimulating β-endorphin release from spinal microglia

Novel Inhibitor of PBP2, Showing Potent β-Lactam Enhancer Activity against Pseudomonas aeruginosa, Including Multidrug-Resistant Metallo-β-Lactamase-Producing High-Risk Clones

Highly conserved neuropeptide derived from Chromogranin A (Parathyroid Secretory Protein 1)

Novel very potent and long acting hetrazepinoic PAF-antagonist

Novel inhibitor of type III secretion system ATPase EscN from enteropathogenic Eecherichia coli

Novel fluoroquinolone antibiotic with potent antimicrobial activity, showing the potential to overcome major drug resistance; its antimicrobial activity was less affected by both pump-mediated efflux and QRDR mutations in P. aeruginosa compared with LVX a

Novel Anti-malarial Plasmodium-Selective Proteasome Inhibitor

Dopamine reuptake inhibitor, also having some SERT affinity

B2 bradykinin receptor antagonist

Natural potent antitumoragent, targeting sarco/endoplasmic reticulum calcium-ATPase (SERCA)2

Novel dual inhibitor of histone deacetylase and topoisomerase I

Novel potent dual inhibitor of phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR), preventing PI3K signaling and inhibiting the proliferation of transformed cells with oncogenic PI3K mutant

Novel GluN2B-specific NMDAR antagonist, completely preventing the decrease in insulin secretion of about 32 % provoked by a 24-h-treatment with NMDA/glycine, eliminating NMDA-induced changes in the oxidation status of the islet cells and elevating the sen

Potent uncompetitive NMDA receptor antagonist

Unique neuroprotectant against oxidative injury, being a highly promising remedy for the treatment of amyotrophic lateral sclerosis (ALS)

Novel Allosteric WNK Kinase Inhibitor

Novel potent dual inhibitor of Wnt and hedgehog signalings, blocking porcupine and smoothened

Novel dual BRD4 and PLK1 inhibitor (IC 50 values of 109 and 22 nM, respectively), showing strong antiproliferative activity against cancer cells

Novel GPR52 agonist, dose-dependently inducing elevation of intracellular cAMP in HEK293/GPR52 cells

Novel inhibitor of the JAK2/STAT3 pathway

Main active metabolite of tazanolast, inhibiting dose-dependently compound 48/80-induced histamine release from rat peritoneal mast cells

Novel Dual Inhibitor of Nitric Oxide and Prostaglandin E2 Production

Potent inhibitor of Plasmodium falciparum dihydrofolate reductase (DHFR)

Novel potent inhibitor of Schistosoma mansoni cathepsin B1 (SmCB1) with IC50 ~0.6 nM

Novel potent inhibitor of Schistosoma mansoni cathepsin B1 (SmCB1) with IC50 ~0.2 nM

Analog of K11777; Irriversible effective cysteine protease inhibitor with trypanocidal activity in cell culture and animal model with comparable efficacy to K11777.

Novel potent RET kinase inhibitor with >500-fold selectivity against KDR (Kinase insert Domain Receptor) in cellular assays

Novel highly potent and orally active ABCB1 modulator capable of overcoming MDR, stabilizing ABCB1 by directly binding to ABCB1, stimulating the activity of ABCB1 ATPase without inhibitory activity against CYP3A4, increasing the sensitivity of SW620/Ad300

Novel xanthine oxidase inhibitor

Simplified analog of the selective Gαq/11 inhibitor YM-25489

Novel α/ß-hydrolase domain 6 (ABHD6) inhibitor

Novel urokinase inhibitor

Potent, ATP-competitive inhibitor of mammalian target of rapamycin (mTOR)

Potent inhibitor of proliferation activity against a broad spectrum of human cancer cell lines, induces G2/M phase arrest and apoptosis through the PI3K/Akt pathway

Natural antibacterial agent against Gram-positive bacterial pathogens such as methicillin-resistant Staphylococcus aureus (MRSA), Enterococcus faecium and Enterococcus faecalis

Antibiotic, exhibiting strong antibacterial activities and showing potent cytotoxicity, inhibiting HSP47 gene expression produced by Streptomyces sp

Novel antibiotic, showing 3- to 10-fold greater cytotoxicity than Xantholipin against a select panel of human cancer cell lines, demonstrating powerful antimicrobial activity against both Gram-positive bacteria and fungi

Quantity (mg or Unit) Unit Price ($/mg or $/Unit) Final Price 100 $26.55 Total: $2,655.00 50 $30.68 Total: $1,534.00 25 $35.99 Total: $899.75 10 $42.48 Total: $424.80 5 $50.15 Total: $250.75

Novel PKM2 activator

Potent and Selective Stearoyl-CoA Desaturase-1 Inhibitor

Novel INK4C inhibitor, specifically blocking the bioactivity of p18 protein and promoting human and murine hematopoietic stem cell ex vivo expansion

Novel non-coding RNA prototype Xist ligand, specifically binding the RepA motif of Xist, reducing the conformational space of RepA, displacing cognate interacting protein factors (PRC2 and SPEN), suppressing histone H3K27 trimethylation, and blocking init

Novel dual inhibitor of AF9 and ENL YEATS domains

Novel Potent Pan-Filovirus Inhibitor, showing potent inhibition against infectious EBOV Zaire (0.09 μM) and MARV (0.64 μM)

Novel Akt1/2 inhibitor

Potent modulator of P-glycoprotein-mediated multidrug resistance (MDR), inhibiting the binding of cytotoxics to P-glycoprotein

Novel selective β-catenin degrader

Carbonic anhydrase inhibitor; Fungal metabolite

Novel activator of p21 promoter in a p53-independent manner

Novel TRIM24/BRPF1 dual inhibitor with IC 50 values of 0.98 and 1.16 μM, respectively

Novel non-peptidic highly potent, soluble and selective NPY Y2 antagonist

Novel, selective, soluble non-​peptidic NPY Y2 receptor antagonist with enhanced CNS exposure

Selective Rho-associated kinase (ROCK) inhibitor

Tamoxifen-analog that Suppresses Glial L-Glutamate Transport Activity without Interaction with Estrogen_receptor>Estrogen Receptors

Novel Inhibitor of Antiapoptotic Bcl-2 Family Proteins

Novel GPR119 Agonist, improving glucose tolerance and augmenting the glucose lowering effect as well as the plasma level of active GLP-1 in normal mice in combination treatment with a dipeptidyl peptidase 4 (DPP-4) inhibitor

Novel glucokinase activator, significantlt decreasing in blood glucose levels with no adverse effects on serum lipids or body weight

Novel dual action combretastatin A-4 (CA-4) prodrug, releasing CA-4 through a disulfide bond cleavage mechanism and containing a near-infrared (NIR) fluorophore

Novel salt inducible kinase (SIK) inhibitor, increasing bone formation and bone mass

Novel, Orally Active Bioavailable Inhibitor of VEGFR2 Signaling with Potent Antiangiogenic Activity and Antitumor Efficacy

Novel Inducer of Apoptosis in Human Colorectal Cells via Mitochondrial Apoptosis Pathway, Inhibiting Tumor Growth

Novel non-analogous leukotriene agonist

Selective growth inhibitor of endothelial cells

YM-244769 is a potent, selective and orally active Na+/Ca2+ exchanger (NCX) inhibitor. YM-244769 preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 can also increase urine volume and urinary excretion of electrolytes in mice.

Potent and selective mGLu1 antagonist

Novel AMPA receptor antagonist

Potent and selective microbicidal agent against wild type (wt) HIV-1, NNRTI-, NRTI-, PRI-resistant mutants

Water-soluble analog of YNT-707, acting as a potent orexin 1 receptor (OX1R) antagonist

Novel potent orexin 1 receptor (OX1R) antagonist

DNA-intercalating dye as sensitive amyloid probe

Novel Proteasome Inhibitor, Enhancing Cisplatin Cytotoxicity in Cisplatin-Resistant Human Ovarian Cancer Cells, inducing cell cycle arrest on G2 phase in MCF-7 cells via ERα and PI3K/Akt pathways

Selective A 2A receptor agonist

Novel γ-lactam pyrazolidinone, targeting penicillin-binding proteins (PBPs) and incorporating a siderophore moiety to facilitate uptake into the periplasm, being effective against multidrug-resistant gram-negative Bacilli

Novel inhibitor of Wnt signaling by stabilizing Axin-1, a scaffolding protein that regulates proteasome degradation of β-catenin

Novel YycG inhibitor, inhibiting planktonic cells of E. faecalis, including the vancomycin- or linezolid-resistant strains

Novel YycG inhibitor, significantly inhibited biofilm formation in static and dynamic conditions

Novel activator of JNK, binding directly to microtubules, inducing ERK-mediated mitotic arrest and subsequent apoptosis

Novel first-in-class inhibitor of BRD4 and EGFR kinase

Novel potent ligand of σ2 receptor (K i =7nM)

Novel riboswitch activator, binding ZTP riboswitches, and activating transcription more strongly than ZMP in vitro

Novel potent dual σ1/2 ligand (σ1 K i =5nM, σ2 K i =3nM), showing anti-allodynic in a model of neuropathic pain

Novel USP10 inhibitor

Inhibitor of the nuclear division in germinating zoospore cysts of Phytophthora capsici via destruction of the microtubule cytoskeleton, and a consequent inhibition of mitosis

Serotonin 5-HT3 receptor antagonist

Novel camptothecin derivative, revealing potent antitumor activities mainly through cell apoptosis pathway, being more effective than CPT-11 and SN38 at inhibiting topoismerase-1

Endothelin Receptor Antagonist

Potent, orally active inhibitor of 5-lipoxygenase (5-LO)

Vascular targeting agent (VTA)

Potassium channel opener

ZDHHC (zinc finger Asp-His-His-Cys) substrate peptide, a 15-mer peptide sequence from KRas4a plus two tryptophan residues

Novel potent HDAC inhibitor with IC50 values for class I HDACs 1, 2, and 3 below 4 nM, and IC50 for HDAC6 at 6 nM.

Site specific inhibitor of tissue transglutaminase

Novel daul inhibitor of GSK-3β (IC 50 = 71 nM) and DYRK1A (IC 50 = 103 nM) with good blood-brain barrier penetrability, inhibiting hyperphosphorylation of tau protein in okadaic acid (OKA)-induced SH-SY5Y cells

Novel inhibitor of pro-HGF activation

Novel Potent and Orally Bioavailable Hypoxia-Inducible Factor 2α (HIF-2α) Agonist

Fluorogenic peptide substrate for a direct fluorometric assay of urokinase, tissue-type plasminogen activator, trypsin and thrombin

Atypical analgesic agent for the amelioration of severe and chronic pain

Growth promotant, acting as a ß-AR (ß-Adrenergic) agonist

The first nonpeptidic inhibitor of ovarian cancer cells growth targeting human thymidylate synthase (hTS)

Novel antagonist for mLST8

Potent VEGFR-2 inhibitor

Novel blocker of AKT1-FAK interaction, reducing the stimulation of FAK phosphorylation in response to extracellular pressure in human SW620 colon cancer cells without affecting basal FAK phosphorylation

Novel Nef Protein Inhibitor; Anti-HIV

Novel TNF-α inhibitor

Novel effective immune checkpoint inhibitor (ICI) against the suppression of T-cell activation, proliferation, and tumor cell eradication.

Novel potent small molecule lligand of miR-21, binding to the major groove of miR-21 hairpin conformation

Novel TNF-α inhibitor

Potent and selective agonist of peroxisome proliferator activated receptors-α (PPAR-α)

Potent and selective agonist of peroxisome proliferator activated receptors-α (PPAR-α)

Novel SIRT1 inhibitor

Novel SIRT1 inhibitor

Novel SIRT1 inhibitor

Novel effective immune check point inhibitor (ICI) against the suppression of T-cell activation, proliferation, and tumor cell eradication.

Potent Ebolavirus (EBOV) Inhibitor

Novel dose-dependent inhibitor of TNF-α-induced NF-κB activation

Novel CDK6 inhibitor

Potent and selective agonist of peroxisome proliferator activated receptors-α (PPAR-α)

Novel EGFR triple mutant T790M/C797S allosteric inhibitor

Novel GDNF Family Receptor Agonist

Potent Ebolavirus (EBOV) Inhibitor

Novel Nef Protein Inhibitor; Anti-HIV

Novel blocker of AKT1-FAK interaction, reducing the stimulation of FAK phosphorylation in response to extracellular pressure in human SW620 colon cancer cells without affecting basal FAK phosphorylation

Novel Zika virus RNA polymerase inhibitor

Novel CtpF inhibitor, inhibiting Ca -dependent ATPase activity in Mtb membrane vesicles

Novel gp120 of HIV-1 Antagonist

Novel potent and specific inhibitor of the UNC119-Src interaction, binding to UNC119 in cells, and inducing redistribution of Src to endomembranes and reduction of activating Src autophosphorylation on Y419

Novel ASCT2 inhibitor

Cell-permeable fluorometric zinc sensor

Non-competitive AMPA receptor antagonist

Type III progesterone receptor antagonist with enhanced antiproliferative properties

Novel oral multitarget tumour growth inhibitor

Novel potent inhibitor of factor Xa (FXa)

Novel dual mordulator of nNOS-PSD-95 interaction and GABA A receptor

Novel potent and selective BRD4 bromodomain 1 (BD1) inhibitor

Novel potent and selective BRD4 bromodomain 1 (BD1) inhibitor

Novel β-catenin/B-cell lymphoma 9 (BCL9) inhibitor, disrupting the β-catenin/BCL9 protein-protein interaction (PPI) with a Ki of 0.96 μM and without affecting the β-catenin/E-cadherin interaction in living cells, displaying good selectivity for β-catenin/

Novel potent and highly selective inhibitor of wild-type and mutant versions of EZH2