DNA topoisomerase II inhibitor

Potent cytotoxin selectively by CYP1A1 as a tumor-selective treatment for human bladder cancers

Novel μ,δ-Opioid Receptor Dual-Biased Agonist, Overcoming the Limitation of Prior Biased Agonist

Novel μ,δ-Opioid Receptor Dual-Biased Agonist, Overcoming the Limitation of Prior Biased Agonist

Novel μ,δ-Opioid Receptor Dual-Biased Agonist, Overcoming the Limitation of Prior Biased Agonist

M1 and M2 Antagonist

Novel highly potent substrate-selective inhibitor of insulin-degrading enzyme (IDE), blocking insulin binding while allowing glucagon cleavage, even at saturating inhibitor concentrations

Novel highly potent substrate-selective inhibitor of insulin-degrading enzyme (IDE), blocking insulin binding while allowing glucagon cleavage, even at saturating inhibitor concentrations

Novel isocitrate dehydrogenase 2 (IDH2) mutants inhibitor for the treatment of cancer

Novel mutant-selective Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitor

The first inhibitor targeting both IDO1/2 that has excellent in vitro inhibitory activity (IDO1 IC50 = 28 nM and IDO2 IC50 = 144 nM)

Selective ER modulator (SERM)

Novel bactericidal agent against M. tuberculosis under acidic conditions, being effective at sterilizing cultures in a concentration-dependent fashion at the highest concentrations

Novel concentration dependent bactericidal agent against M. tuberculosis, being markedly more efficient at killing M. tuberculosis under acidic conditions

Innate Defence Regulator Peptide, Enhancing Monocyte Migration and Adhesion on Fibronectin

Novel immunomodulatory and antibiofilm innate defense regulator peptide

Angiotensin converting enzyme (ACE) inhibitor

Selective serotonin 5-HT2A receptor antagonist

Novel Type I Interferon Inducer

Novel Type I Interferon Inducer

Novel Type I Interferon Inducer; Intercalator of DNA; Inhibitor of the retrovirus replications including HIV

First Small-Molecule Inhibitor of RNA-Binding Protein IGF2BP2/IMP2 for Cancer Therapy

Novel Inhibitor of RNA-Binding Protein IGF2BP2/IMP2 for Cancer Therapy

Novel Inhibitor of RNA-Binding Protein IGF2BP2/IMP2 for Cancer Therapy

Highly potent fluorescent iGlu receptor antagonist

Novel dual SMO-HDAC antagonist, retaining similar specificity for SAHA-targeted HDACs, disabling deviant Hedgehog signaling and preventing GLI binding to DNA

Natural Inhibitor of Clathrin-Mediated Endocytosis

Novel allosteric inhibitor of IκBα phosphorylation and NF-κB transcriptional activity through selective capture of the inactive conformation and hence blockade of IKKβ S177/S181 phosphorylation

Antineoplastic phospholipid, being effective against many tumor types, including ovary, non-small cell lung, kidney, and melanoma, exhibiting competitive inhibition of protein kinase C (PKC) activity

Dual D 2 /5-HT 2 antagonist as an antipsychotic agent

Novel orally effective direct renin inhibitor for treating diabetic nephropathy and hypertension

Novel anti-tuberculosis agent, targeting Mycobacterial tuberculosis (Mtb) aspartate semialdehyde dehydrogenase

Novel inhibitor of protein kinase B (PknB), inhibiting PknB auto-phosphorylation and the phosphorylation of GarA by PknB in a dose-dependent manner

BCL2 i-motif-interactive compound, stabilizing or facilitating the folding of the i-motif

BCL2 i-motif-interactive compound, destabilizing or unfolding the i-motif

Insect neurotoxin, blocking nicotinic acetylcholine receptors and preventing acetylcholine from transmitting impulses between nerves

Novel potent inhibitor of BV2 microglia activation, protecting PC12 cells and primary neurons against indirect toxicity mediated by exposure to conditioned medium (CM) from LPS-treated BV2 cells

Novel resistance breaking antimalarial N-myristoyltransferase (NMT) inhibitor, binding to NMT peptide binding pocket

Novel cell-active and potent inhibitor of bacterial DNA repair, potentiating quinolone antibiotic activity in methicillin-resistant Staphylococcus aureus

Novel Probe for NLRP3 Inflammasome Inhibitor MCC950

First in-class allosteric inhibitor of a bacterial IMPDH, showing to counteract the activation by the natural positive effector, MgATP, and to block the enzyme in its apo conformation

Novel plant immune-priming agent, acting as a partial agonist of salicylic acid

Novel plant immune-priming agent, acting as a partial agonist of salicylic acid

Mtb growth inhibitor, inhibiting Mtb GlgB activity by interacting to its active site residues

Potent inhibitor of the TGF-β type I receptor activin receptor-like kinase 5 (ALK5)

Novel ALK5 inhibitor

Janus-associated kinase (JAK) inhibitor

Novel potent and selective lysine-specific demethylase 1 (LSD1) inhibitor

Novel selective Mtb-DHFR inhibitor as an antimycobacterial agent

Novel selective inhibitor of PfHsp90, bypassing its highly similar human orthologs

Antiprion agent, reducing PrP(Sc) levels in dividing and stationary-phase cells

Selective estrogen receptor modifier (SERM), being a selective ERß agonist

Antidepressant and cerebral activator, acting as a serotonin releasing agent, norepinephrine reuptake inhibitor, and NMDA receptor antagonist, enhancing acetylcholine release via activation of the 5-HT4 receptor

Topoisomerase I (Top1) inhibitor

Platelet aggregation inhibitor acting as a reversible Cyclooxygenase>cyclooxygenase inhibitor

Metabolite of tryptophan, reducing the interleukin-8 (IL-8) response after IL-1β stimulus, interacting with the transcription factor aryl hydrocarbon receptor (AHR) and preventing transcription of the inflammatory cytokine IL-8, being anti-inflammatory in

Natural antibiotic, selectively inhibiting bacterial tryptophanyl-tRNA synthetase (TrpRS)

Novel inhibitor of dihydroorotate dehydrogenase (DHODH), promoting myeloid differentiation and inhibiting the proliferation of acute promyelocytic leukemia HL-60 cells, also suppressing cell growth in various other types of cancer cells

Topoisomerase I (Top1) inhibitor

Novel sPLA2 inhibitor, suppressing murine endotoxic shock and LDL modification, blocking binding to the M-type receptor

Metabolite of tryptophan, showing adverse effects on bones and the central nervous system, having been most frequently implicated as a contributor to renal disease progression and vascular disease

NIR emitting firefly luciferin analogue

Novel inhibitor of the influenza virus reproduction, inhubiting the formation of the virus specific hemagglutinin

Novel inhibitor of Ark1, the fission yeast member of the conserved Aurora kinase family

Novel dual inhibitor of MAPKAPK5 and MAPKAPK2

Novel Potent Inhibitor of Microbiome ß-Glucuronidases

Novel Potent Inhibitor of Microbiome ß-Glucuronidases

Novel selective inhibitor of the iNOS, without affecting the eNOS isoform

Novel Potent and Selective Inducible Nitric Oxide Synthase (iNOS) Inhibitor (IC50 = 74 nM) with high BBB permeability (Pe = 19.1 × 10-6 cm/s) for Parkinson's Disease

Novel Potent and Orally Active Inducible Nitric Oxide Synthase (iNOS) Dimerization Inhibitor with Efficacy in Rheumatoid Arthritis Mouse Model

Novel putative inhibitor of type III secretion (T3S) in the Gram-negative pathogen Yersinia pseudotuberculosis and Chlamydia trachomatis

Novel potent inhibitor of DDR1 tyrosine kinase

Novel inhibitor of the DNA-binding domain (DBD) of STAT3, suppressing tumor growth, metastasis and STAT3 target gene expression in vivo

Activator of the P2Y6 receptor in bone, increasing survival of osteoclasts

Blocker of the interaction of FAK and IGF-1R; Antagonist of the phosphorylation of tumor AKT

Natural potent inhibitor of H. pylori DHODH, having greater efficacy for treatment of H. pylori infection

Inhibitor of both topoisomerase I and II via intercalating DNA helix

Natural Activator of Programmed Cell Death, leading to membrane damage, mitochondria alteration, chromatin condensation, and ROS accumulation

Novel Potent Fungal-Selective Inhibitor of Mitochondrial Cytochrome bc1

Novel antifungal agent, exhibiting broad spectrum and potent activity against 12 kinds of clinically pathogenic fungi

Selective monoamine oxidase A inhibitor

Novel inhibitor of the plant inositol phosphorylceramide synthase ((IPCS), demonstrating herbicidal activity

Muscarinic Acetylcholine Receptor Hybrid Ligand, possessing noticeable M2/M4 mAChR selectivity

Orally bioavailable inhibitor of Hedgehog signaling, inhibiting tumor initiation and metastasis in pancreatic cancer

Natural toxic furanoterpenoid found in mold-damaged sweet potatoes

Natural inhibitor of the in vitro biogenesis of the SARS-CoV-2 spike protein and its host cell membrane receptor, binding Sec61α to Inhibit Protein Translocation

Novel inhibitor of glioblastoma multiforme (GBM), inhibiting cell viability of low-passage patient-derived GBM spheroids, blocking tube-formation of endothelial cells in Matrigel, showing no effect on primary hematopoietic CD34+ progenitor spheroids or as

Inhibitor of the uPAR·uPA protein-protein interaction, blocking cancer cell invasion

Irreversible and nonselective Monoamine_oxidase_inhibitor>monoamine oxidase inhibitor (MAOI)

Novel inhibitor of protein-protein interaction (PPI), targeting integrin αvβ3-osteopontin interface, blocking OC maturation from murine bone marrow-derived macrophages, as well as the resorptive function of OCs, impairing downstream signaling of integrin

Sulfasalazine analog, releasing 5-aminosalicylic acid and a nontoxic carrier molecule in the gastrointestinal tract

Novel potent inverse agonist of the chemokine receptor CXCR4, preventing CXCL12-mediated chemotaxis and triggering apoptosis in a panel of 18 cell lines and primary cultures, with superior mobilizing properties in vivo

NIR-II cyanine dye for cancer treatment and diagnosis

Novel interleukin-1 (IL-I) receptor-associated kinase (IRAK) modulator

Novel potent and selective degrader of IRAK3, inducing proteasome-dependent degradation of IRAK3 and showing both CRBN and IRAK3 binding for activity

Novel Orally Efficacious IRAK4 Inhibitor, Targeting MyD88L265P Mutant Diffuse Large B Cell Lymphoma

Novel inhibitor of CDC25 phosphatases, actively against human cancer cells

Inhibitor of IRE1 endoribonuclease activity, strongly inhibiting XBP-1 splicing in an in vivo model of acute endoplasmic reticulum stress.

ET B receptor agonist, showing anti-apoptotic activity and protecting neural cells in rats with cerebral ischemia

Novel potent hA2BAR antagonist (Ki = 3.66 nM)

Neutral BBB crossing reactivator for acetylcholinesterase inhibited by paraoxon, also acting as anticonvulsant

Selective thromboxane A2 (TXA2) synthase inhibitor

Natural Stabilizer of the 14-3-3/Gab2 Protein-Protein Interaction (PPI) Interface

Novel osteoclastogenesis inhibitor, preventing ovariectomy-induced osteoporosis in ddY mice

Iminosugar, binding selectively to N370S glucocerebrosidase and restoring its correct conformation and, consequently, enhancing its activity

Potent inotropic agent, inhibiting both PDE3 and PDE4

Natural essential oil, showing activity against T. muris

Natural antibacterial agent with cytotoxicity and hemolytic properties against a larger panel of Gram-negative bacteria

P2X-purinoceptor antagonist

Natural genistein derivetive with antibacterial and antifungal activities

Inhibitor of the cellulose biosynthesis, inhibiting anisotropic cell expansion resulting in a severely swollen and stunted growth phenotype

Biological Active Reagents

Novel prodrug of potent IspH inhibitor, killing clinical isolates of several multidrug-resistant bacteria, including those from the genera Acinetobacter, Pseudomonas, Klebsiella, Enterobacter, Vibrio, Shigella, Salmonella, Yersinia, Mycobacterium and Baci

Novel inhibitor of COX and neutrophil migration

Distinct IKur blocker

Unique topoisomerase inhibitor, showing significant growth-inhibitory effects against large-cell lung cancer (Lu-116) and gastric adenocarcinoma (St-4)

Novel Potent and Selective A3 Antagonist

Novel degrader of CRABP proteins

Novel highly potent (EC 50 = 1.6 nM) aryl hydrocarbon receptor (AhR) agonist with high affinity (K i = 88 nM)

Novel Potent and Selective Histone Deacetylase 6 (HDAC6) Inhibitor, showing a remarkably low toxicity both in vitro and in vivo and increasing the function of regulatory T cells (Tregs) at well-tolerated concentrations

Novel selective HDAC6 inhibitor

Novel PP2A ligand, protecting against memory impairment and focal cerebral ischemia in mice

Novel neuroprotective agent

Novel, potent, selective, and BBB-permeable P2X7 antagonist

Novel highly potent, orally bioavailable hepatitis C virus (HCV) entry inhibitor

First-in-class iodothyronine deiodinase type 3 (DIO3) inhibitor, demonstratig attenuated cell counts, induction in apoptosis, and a reduction in cell proliferation in DIO3-positive HGSOC cells (OVCAR3 and KURAMOCHI)

Selective inhibitor of the funny channel pacemaker current (If) in the sinoatrial node in a dose-dependent fashion, resulting in a lower heart rate and thus more blood to flow to the myocardium

The first Ang IV-analogue being able to abolish IRAP-availability completely at the cell surface in vitro

Prodrug of QVO, being quickly converted to QVO in mice and rats following administration, ameliorating hyperglycemia, and suppressing hepatic gluconeogenesis and activating AMPK signaling pathway in the liver tissues

Novel, orally available soluble guanylate cyclase (sGC) stimulator with once-daily dosing potential for the treatment of cardiovascular diseases

Novel WNT inhibitor, suppressing cytoplasmic and nuclear biochemical markers of WNT signaling in cultured cells, inhibiting recombinant TNKS activity, or WNT fatty acylation

Novel WNT inhibitor, suppressing cytoplasmic and nuclear biochemical markers of WNT signaling in cultured cells, inhibiting recombinant TNKS activity, or WNT fatty acylation

Novel potent noncleavable proteolysis targeting chimeric (PROTAC) for TrkC degradation in metastatic breast cancer cells

Novel potent and cleavable proteolysis targeting chimeric (PROTAC) for TrkC degradation in metastatic breast cancer cells

Potent and selective agonist of human somatostatin receptor 4 (sst4), reducing mechanosensitivity of peripheral nerve afferents and spinal neurons in an inflammatory pain model

Novel highly potent JAK1-selective inhibitor, exhibiting excellent selectivity over JAK2, JAK3, and TYK2 (IC 50 : JAK1 0.145 nM; JAK2 2.94 nM; JAK3 2.31 nM; TYK2 8.17 nM)

Novel JAK1 inhibitor

Novel selective Jak2 inhibitor, demonstrating a time-dependent knock-down of pSTAT5, a downstream target of Jak2

Novel irreversible selective JAK3 inhibitor through the covalent interaction with a Jak3 active-site cysteine

Novel irreversible selective JAK3 inhibitor through the covalent interaction with a Jak3 active-site cysteine

Novel irreversible selective JAK3 inhibitor through the covalent interaction with a Jak3 active-site cysteine

Novel Selective JAK3 Inhibitor with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket

Novel Selective JAK3 Inhibitor with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket

Novel potent JAK1/2/3 inhibitor

Novel potent JAK1/3 inhibitor, targeting JAK3 and JAK1 with IC 50 at 3nM and 5nM, respectively

Novel positive allosteric modulator of AMPA receptor

Novel anti-triple-negative breast cancer (anti-TNBC) agent with a high selectivity against BC cells over normal human cells, downregulating phosphatidylinositide 3-kinase (PI3K)/Akt pathway by suppressing protein-tyrosine phosphatase 1B (PTP1B) expression

Novel fluorogenic yellow fluorescent dye for use in self-labeling tag systems

Novel mitophagy inducer with therapeutic potential for Parkinson's disease, acting as light chain 3 (LC3) interactors, similar to cardiolipin or ceramide, triggering mitophagy via Pink1/Parkin

Novel Inhibitor of Jumonji AT-Rich Interactive Domain 1B (JARID1B) Histone Demethylase

Natural naphthyridine alkaloid

Potent inhibitor of the proliferation of PC3 prostate carcinoma cells

Natural Inhibitor for Protein−Protein Interaction of the Homodimer of Proteasome Assembly Factor 3

Natural radical scavenger, inhibiting L-glutamate toxicity in neuronal hybridoma N18-RE-105 cells

Inhibitor of renal transporters OAT1 and OAT3; Antihepatitis agent as a substrate for intestinal PEPT1

Natural anti-inflammatory agent, showing potential for the treatment of inflammatory bowel disease (IBD)

Metabolite of JBSNF-000088

Novel RORα activator, diminishing diethylnitrosamine-induced acute liver injury and repressing transcriptional expression of APPs such as CXCL1 and LCN2 in mice

Novel dose-dependent inhibitor of ABHD6

JCP174 analog used for affinity purification of labeled targets

Negative control of JCP174

Novel dose-dependent inhibitor of ABHD6

Covalent dual inhibitor of DPAP1 and DPAP3

Covalent dual inhibitor of DPAP1 and DPAP3

Novel potent inhibitor of Mpro

Novel irriversable serine hydrolases inhibitor

Peripheral Selective CB1 Receptor Antagonist

Novel apoptosis inducer, significantly inhibiting tumor growth in the xenograft model

Novel human flap endonuclease 1 (FEN1) inhibitor with in vitro inhibition of flap cleavage activity as well as cytotoxic activity against a colon cancer cell line, DLD-1

Novel inhibitor of the heat shock protein 70 (Hsp70) with anti-proliferative activity in breast and prostate cancer cells

Novel type I Interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor, binding preferentially to unphosphorylated IRAK4

Novel Interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor, binding preferentially to unphosphorylated IRAK4

Novel Ras homologous A (RHOA) inhibitor, potently inhibiting cell viability and migration/invasion of gastric cancer (GC) cell lines, and mouse xenografts, diversely expressing RHOA, binding affinity for RHOA was >140-fold greater than Rhosin, a nonclinic

Novel specific dual inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2) and cyclin-dependent kinase 1 (CDK1), targeting cell cycle progression and angiogenesis

Potent non-nucleoside inhibitor of HIV-1 reverse transcriptase (NNRTIs)

Novel potent GHS-R1a agonist (EC50 (Ca ): 1.6 nM), significantly stimulating GH secretion

Novel ghrelin receptor (GHS-R1a) antagonist [IC 50 (affinity): 5 nM IC 50 (Ca ): 60 nM]

Novel partial inverse agonist of GHS-R1a (K i = 3 nM, EC 50 = 70 nM, Emax = −37%)

Novel inhibitor of viral protease function, suppressing Zika virus Infection both In vitro and In vivo

Novel Potent NS4B Inhibitor for the Treatment of Dengue Virus Infection

Novel Potent Human Adenovirus Inhibitor, showing improved anti-HAdV activity (IC50 = 0.27 μM), significantly decreasing cytotoxicity (CC50 = 156.8 μM), and lowering in vivo toxicity (maximum tolerated dose = 150 mg/kg in hamster) as compared with niclosam

Novel potent and selective IRAK1 degrader, effectively degraded cellular IRAK1 protein with a DC50 of 3 nM in HBL-1 cells

Novel, potent dual inhibitor of the leukocyte proteases cathepsin G and chymase

Vascular endothelial growth factor receptor-2 (VEGF-2) kinase inhibitor

Estrogen receptor ESR1 agonist

Novel Positive Allosteric Modulator of the α7 Nicotinic Acetylcholine Receptor

Selective delta opioid receptor agonist as a potent and efficacious antihyperalgesic agent

Novel EthR inhibitor, boosting antituberculous activity of ethionamide

Selective androgen receptor modulator with minimal prostate hypertrophic activity stimulating sexual behavior in female rats

Histamine H3 receptor antagonist and serotonin reuptake inhibitor

Novel potent, selective, and systemically active positive allosteric modulator (PAM) of mGlu2-receptors

Novel Adenosine A 2A /A 1 Antagonist With Efficacy In Preclinical Models of Parkinson's Disease

Negative control for JNJ-40068782

JNJ-40355003 is a potent and selective atty acid amide hydrolase (FAAH) inhibitor.

Negaive control for JNJ-42396302

Novel potent, orally active LTA4H inhibitor

Novel inhibitor of PDE10A

Novel ago-PAM for the metabotropic glutamate receptor subtype 2 (mGluR2)

Novel inhibitor of respiratory syncytial virus (RSV), binding the RSV F glycoprotein and inhibiting membrane fusion

Negative control for JNJ-54119936