Inhibitor of cysteine protease

Unique first-in-class antibiotic, being more effective at killing pathogenic methicillin resistant Staphylococcus aureus (MRSA) bacteria than two clinical gold-standard antibiotics-vancomycin and gentamicin

Unique first-in-class antibiofilm antibiotic for biofilm-related wound infections caused by Acinetobacter baumannii

Highly potent and selective H4R antagonist

Novel potent, selective and metabolically stable LRRK2 inhibitor

Novel antiviral agent, blocking microtubule polymerization, disrupting the Golgi complex and inhibiting viral trafficking to the plasma membrane during virus egress

Promoter of spinal muscular atrophy (SMA)

Novel ERK2 inhibitor

Novel dopamine D2 receptor antagonist as a potent multi-target ligand of aminergic G protein-coupled receptors (GPCRs) which dose-dependently stimulates growth, survival of neurons, and promotes their integrity

Novel potent and selective agonist of dopamine D 2 receptor (D 2 R; K i = 4.58 nM)

Novel potent and selective agonist of dopamine D 3 receptor (D 3 R; Ki = 5.72 nM)

Novel ERK2 inhibitor

Novel direct AMPK agonist, showing potential anti-cancer activity via inducing apoptosis, cell cycle arrest, suppressing glycolysis and cholesterol synthesis after activation of AMPK in gefitinib-resistant H1975 cells

Novel dual extracellular signaling-related kinase (ERK)/PI3K inhibitor

Novel 5-HT4 receptor agonist to accelerate colonic motor activity in mice

Novel inhibitor of SET7/9

Novel selective and potent DPP7 inhibitor with a DPP7 IC50 value of 480 pM

Selective inhibitor of human DPP7

Widely used fluorescent detector of nitric oxide in culture medium, tissue sections and biopsy cells

Novel potent Bax inhibitor, showing concentration-dependent inhibition of liposome permeabilization with improved activity in vitro

Lipid bilayer modulator which likely inserts into lipid bilayers in the headgroup region, alters their structure and phase behavior, thins the bilayer and fluidizes it, allowing even saturated lipid to form fluid bilayers

Potent and selective fluorescent adenosine A1 receptor agonist

Novel inhibitor of L,L-diaminopimelate aminotransferase (DapL)

Potent Selective serotonin reuptake inhibitor (SSRI)

An impurity formed in Darapladib production

Proteolysis targeting chimeras (PROTAC), acting as a degrader of oncogenic BCR-ABL

Proteolysis targeting chimeras (PROTAC), acting as a degrader of oncogenic BCR-ABL

Novel PROTAC targeting drug-resistant BCR-ABL

Novel glucagon analog for diabetic hypoglycemia therapy

Novel selective ionotropic glutamate receptor 5 (iGluR5) antagonist

Biological Active Reagents

Novel tyrosine kinase inhibitor for drug resistant T315I mutant BCR-ABL

Novel ERG/DNA binding inhibitor, targeting the DNA-binding activity of the human ERG transcription factor

Novel antileishmanial agent, against both intracellular Leishmania donovani and intracellular Leishmania amazonensis and displaying dose-dependent reduction of liver parasitemia

Novel protein cross-linking agent

p38 MAPK inhibitor, supressing p38 phosphorylation and LPS-induced TNF-α production in macrophages

Potent HCV NS5A inhibitor

Novel selective non-nucleoside inhibitor of DNA methyltransferase 1 (DNMT1)

Novel inhibitor of WDR5-MLL1 interaction

Novel inhibitor of menin-MLL interaction

Novel inhibitor of menin-MLL interaction

Novel inhibitor of menin-MLL interaction

Inhibitor of N-methyl transferases (NMT), preventing the formation of Parkinson's syndrome neurotoxins via methylation of non-methylated pre-neurotoxins.

Novel potent BPTF-BRD inhibitor, showing selectivities 100-fold higher than those of other BRD targets, significantly inhibiting leukemia cell proliferation

Novel potent BPTF-BRD inhibitor, showing selectivities 100-fold higher than those of other BRD targets

Novel potent CBP bromodomain inhibitor with a TR-FRET IC50 value of 19.5 ± 1.1 nM and over 400-fold of selectivity against BRD4 bromodomains

Novel potent EZH2 inhibitor

Novel potent EZH2 inhibitor

Activator of IK and SK channels

Novel inhibitor of lysine methyltransferase G9a

Highly potent agonist for group II mGlu receptors

Novel potent CDK2 inhibitor with selectivities above 10-fold over CDK1/4/6/7/9/12 above 10-fold, displaying anti-proliferative activity against A2058 melanoma and MV4-11 leukemia cell lines and low toxicity on human normal cell lines, inhibiting CDK2-medi

Novel potent and selective DCN1-UBC12 inhibitor for anticardiac fibrotic effects, specifically targetinbg DCN1 at molecular and cellular levels, effectively reversing angiotensin (Ang) II-induced cardiac fibroblast activation

Novel PRC2 Inhibitor, Targeting EZH2-EED Interaction

Novel, Selective Histone Methyltransferase SET7 Inhibitor

Novel, Potent and Selective Histone Methyltransferase SET7 Inhibitor

Novel, Potent and Selective Histone Methyltransferase SET7 Inhibitor

Novel potent and selective TEAD autopalmitoylation inhibitor, inhibiting TEADs transcription activity and downstream gene expression

Novel Hsp90 inhibitor, exerts potent antitumor activity against HER2-positive breast cancer through disruption of Hsp90-Cdc37 interaction

Novel selective BTK degrader, demonstrating prolonged pharmacodynamic effects

Novel inhibitor of α-calcitonin gene-related peptide (α-CGRP) exocytotic release from primary sensory neurons, selectively interacting with Synaptotagmin 1

First-generation allosteric EGFR inhibitor, binding to the allosteric site of EGFR along with ATP that leads to inhibition of cell proliferation and arrest of EGFR L858R/T790M/C797S signalling

Novel activator of the GUS reporter activity, specific increasing in stumpy reporter gene expression

Novel transmission blocker of antimalarials, targeting male gametes

Potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain

Potent inhibitor of Trypanosoma brucei N-myristoyltransferase (TbNMT) with markedly improved blood-brain barrier permeability

Novel potent and broad-spectrum antiviral agent, acting as a chain terminator for viral RNA polymerase

Novel potent blocker of mixed lineage leukemia 1 (MLL1)-WDR5 interaction, inhibiting MLL1 complex H3K4 methyltransferase activity

Novel Potent and Orally Bioavailable Inhibitor of the WDR5-Mixed Lineage Leukemia 1 (MLL1) Protein-Protein Interaction for the Treatment of MLL Fusion Leukemia

Novel NQO1 substrate, inhibiting cancer cell (NQO1-rich A549 cell line) growth

Novel Nrf2 activator

Potent mGAT4 inhibitor

Potent and selective DDR1 receptor tyrosine kinase inhibitor

Inhibitor of nonhomologous end-joining (NHEJ) DNA repair following double strand DNA breaks induced by ionizing radiation, enhancing the effects of DNA-damaging cancer drugs like etoposide, camptothecin and doxorubicin

Negative control for DDR-TRK-1

NO donor, generating a controlled release of nitric oxide in solution.

Coumarin-caged D-luciferin, being excited in the caged group only by light of wavelength ranging within 400-430 nm

Fluorophore to myosin or actomyosin

Novel potent inhibitor of the enoyl-acyl carrier protein reductase FabI, reducing bacterial burden in mice and rescuing mice from lethal infections with clinical isolates of Acinetobacter baumannii, Klebsiella pneumoniae and E. coli

Deferasirox iron complex

Iron chelating agent, chelating iron from intra-lysosomal ferritin and hemosiderin forming ferrioxamine, a water-soluble chelate excreted by the kidneys and in the feces via the bile

Novel selective degrader of BCR-ABL over c-ABL in leukemia cancer cells

Natural polyketide matabolite

Novel selective δ-protein kinase C inhibitor

Vitamin E variant, inhibiting prostate adenocarcinoma, lung tumorigenesis, promoting thermogenic gene expression via PGC-1α upregulation, preventing methylglyoxal-induced apoptosis by reducing ROS generation and inhibiting apoptotic signaling cascades

Potent inhibitor of PI3 kinases

Selective DPP-IV Inhibitor

Antispasmodic agent, improving the elasticity of the soft birth canal and regulating labor contractions

Novel anti-Alzheimer's disease agent, ameliorates spinal cord injury via axonal growth associated with astrocyte-secreted vimentin

Novel selective inhibitor of the DENV2 protease, inhibiting flavivirus protease through targeted covalent modification of active site serine, contrary to an allosteric binding mechanism as previously described

Novel selective inhibitor of the DENV2 protease, inhibiting flavivirus protease through targeted covalent modification of active site serine, contrary to an allosteric binding mechanism as previously described

Novel selective inhibitor of the DENV2 protease, inhibiting flavivirus protease through targeted covalent modification of active site serine, contrary to an allosteric binding mechanism as previously described

Novel reversible microtubule inhibitor, increasing lysosomal V-ATPase activity and lysosome acidity

Novel selective and sensitive near-infrared fluorescent probe for visualization of endogenous nitric oxide in living cells and animals

Selective anti-tumor agent, inducing apoptosis and inhibiting topoisomerase I

Most efficient spin trap for the in vitro and in vivo detection of O-, N-, S- and C-centered free radicals

HIV-1 fusion inhibitor, targeting the membrane-proximal external region of Env spikes, specifically inhibiting the HIV-1 envelope-mediated membrane fusion by blocking CD4-induced conformational changes

Inhibitor of acetyl-CoA carboxylase (ACC), activating GPR40, inhibiting West Nile virus (WNV) infection and reducing the multiplication of Usutu virus (USUV), a WNV-related flavivirus

Desfluoro impurity of Ezetimibe

Precursor for PET imaging 11C-radiolabeled MK-6884

Primary metabolite of diazepam, binding to the GABA A receptor benzodiazepine modulatory site

PET precursor of preparing radiolabel [11C]HD-800, a high affinity brain penetrant PET tracer for imaging microtubules

Cysteine reactive protein labeling agent

Pro-drug of dexamethasone, anti-inflammatory glucocorticoid, stimulating glutamine uptake in the cerebral cortex

Glucocorticoid, Anti-inflammatory Agent

Cholecystokinin antagonist, selective for the CCKA subtype

Norepinephrine-dopamine reuptake inhibitor (NDRI)

Natural modulator of mu-, delta-, and kappa-opioid receptors

5-HT3 Receptor antagonist; Antitussive; Anti-inflammatory; Antiasthmatic

Potent Squalene Synthase Inhibitor

Cell-permeable, reversible and selective inhibitor of ɣ-secretase

Proteolysis targeting chimeras (PROTAC), potently decreasing FKBP12 abundance in MV4;11 cells, leading to over 80% reduction of FKBP12 at 0.1 μM and 50% reduction at 0.01 μM

Novel potent, orally active inhibitor of LTA4H

Selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2)

The major adduct formed by the food-borne carcinogen, PhIP with DNA

Novel human α-galactosidase A ligand, capable of stabilizing α-Gal A and restoring trafficking

Abundant lipid in the membranes of many algae, lower plants, and fungi, showing an inverse concentration relationship with phosphatidylcholine, being capable of replacing phosphatidylcholine

Novel HCV NS3 degrader, reducing susceptibility to resistance mutations, potently inhibiting HCV in a cellular infection model, exhibiting the most potent degradation (DC50 of 50nM at 4h) of HCV NS3,

Novel growth inhibitor of both triple-positive and triple-negative human breast cancer cell lines

Novel inducer of autophagic cell death through upregulation of HMGB1 in A549 cells

Novel Pim kinase inhibitor

The most potent inhibitor of sodium iodide symporter (NIS) reported to date

Novel potent, selective and covalent inhibitor of DCN1, selectively inhibiting neddylation of cullin 3 in cells

Novel STING agonist with enhanced binding to STING and cellular function, displaying strong anti-tumour activity

Novel potent and selective STING agonist, activating secretion of IFNβ, IL-6, TNF, and KC/GROα, exhibiting durable anti-tumour effects

Novel probe for protein S-sulfinylation from cells

Selective alpha4beta2 nAChR partial agonist for the treatment of nicotine dependence to assist in smoking cessation

Novel Inhibitor of the AAA-ATPase Drg1, blocking ribosome biogenesis

Histamine H1-receptor antagonist

Morin derivative, enhancing neural glyoxalase pathway (GP) activity and preventing methylglyoxal-mediated oxidative stress (OS) in an AD model

Major biliary metabolite of Diclofenac, a nonsteroidal antiinflammatory drug and COX inhibitor

Non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions

Selective herbicide for the control of dicot weeds

Lipophilic fluorescent reagent, labeling membranes and other hydrophobic structures

Natural Tat inhibitor, blocking HIV-1 transcription by specifically targeting the viral transactivator, Tat

Inhibitor of DTDST inhibitor, a novel intestinal epigallocatechin gallate (EGCg) transporter

Novel inhibitor of CP4H activity in cultured cells at concentrations that do not cause iron deficiency

Novel inhibitor of CP4H activity in cultured cells at concentrations that do not cause iron deficiency

Muscle relaxant, causing general central nervous system depression, relieving pain caused by strains, sprains, and other musculoskeletal conditions

Antiemetic agent used in the treatment of vomiting and vertigo

Agonist of the androgen receptor (AR); #333333; font-family: "Helvetica Neue", Helvetica, Arial, sans-serif; font-size: 14px; font-style: normal; font-variant-ligatures: normal; font-variant-caps: normal; font-weight: 400; letter-spacing: normal; orphans:

Corticosteroid Hormone Receptor Agonist

Novel dose-dependent inhibitor of the SARS-CoV-2 Mac1 Macrodomain

D1-like full agonist with similar affinity for D1 and D5, and roughly 10-fold selectivity over D2-like receptors

Competitive nicotinic receptor antagonist

Closely related co-metabolite of cyclosporin A

Unique antimigration and antiangiogenic agent

Novel lipid-based, high-density, environmentally sensitive (HIDE) probe

Novel lipid-based, high-density, environmentally sensitive (HIDE) probe

Vasodilator for the treatment of cardiopathy and renal disorders, acting as an adenosine reuptake inhibitor.

Building Block

Building Block

Novel inhibitor of AMA1-RON2 interaction, blocking merozoite invasion from schizont-infected RBCs; Antidepressant; Acetylcholinesterase inhibitor

Serotonin antagonist and histamine antagonist

Novel analog of etomidate, potently inhibiting 11-beta-hydroxylase without GABAA receptor positive modulatory and sedative-hypnotic activities

Anti-infective agent against certain protozoa such as Babesia, Trypanosoma, Cytauxzoon, and certain bacteria including Brucella and Streptococcus

Inhibitor of Topoisomerase>DNA topoisomerase II; very potent cytotoxic antitumor agent

Long-lasting prodrug of nalbuphine, acting as a moderate-efficacy partial agonist or antagonist of the μ-opioid receptor and as a high-efficacy partial agonist of the κ-opioid receptor

Natural full D1 dopamine receptor agonist

Potent antagonist of GABA A receptors that contain alpha1 and beta2 subunits

Novel activator of the bone marker alkaline phosphatase (ALP), markedly promoting osteoblast differentiation, including expression of Runx2, Osterix, and Osteocalcin, mediating osteogenesis through activation of p38-β

Novel negative allosteric modulator of the mGlu5 receptor

Inhibitor of ATPase activity of HSP70

Antibiotic, specifically inhibiting the initiation of RNA synthesis, binding isohelically to the minor groove of B-DNA at A/T rich sites

Parasympathomimetic with longer duration of action

Novel selective Factor Xa inhibitor, reducing thrombus formation with low risk of bleeding

Novel inducer of apoptotic cell death in TNBC cell lines without causing cytotoxicity in the normal mammary epithelial cell line

Novel inducer of apoptotic cell death in TNBC cell lines without causing cytotoxicity in the normal mammary epithelial cell line

Inhibitor of NF-kappaB-mediated GROalpha expression, suppressing the TNFalpha-induced invasive capability of MDA-MB-231 human breast cancer cells

Novel autophagonizer, inducing autophagic cell death in apoptosis-defective cell line

Novel acetylcholinesterase inhibitor, promoting synaptic function and neuronal survival, ameliorating cognitive deficits in SAMP8 mice via improved mitochondrial dynamics and increased activity of the NMDAR-CREB-BDNF pathway

Novel potent anti-MRSA agent, disrupting biofilms with no resistance development, sensitizing rifampicin and tetracycline against multidrug-resistant Acinetobacter baumannii and Pseudomonas aeruginosa

Specific protein disorder catalyzer of HIV-1 Nef

Competitive inhibitor of both SPHK1 and SPHK2

Ultrasensitive bioluminogenic enzyme substrate

Chromogenic peptide substrate, being highly sensitive for the measurement of activated Protein C.

Prodrug of CPPTL, inducing apoptosis in a dose-dependent manner via the ROS/JNK pathway in acute myeloid leukemia

Novel multi-target anticancer prodrug activated by the tumor specific CYP1B1 enzyme, potently inhibiting HCT-15, HCT-116 and K562 cells growth, showing moderate anti-proliferative activity towards MDA-MB-231, HepG2, PANC, Bel7402 and MGC803 cancer cells,

Novel antineoplastic agent, exhibiting remarkable anticancer activity as well as excellent cellular selectivity

Novel blocker of the TLR2 and TLR4 downstream signaling pathway, effectively inhibiting mRNA expression of MyD88 and p65, major subunit of nuclear factor-kappaB

Novel non-nucleoside inhibitor of Zika viral RNA-dependent RNA polymerase (RdRp) enzymes

Novel potent and selective PROTAC degrader of myeloid cell leukemia 1 (MCL1)

Novel cell permeable caged Luciferin

Novel inducer of ferroptosis and apoptosis through ubiquitination of GPX4 in triple negative breast cancer cells

Potent and highly selective µ opioid agonist

Novel,orally active and selective alpha-7 nicotinic acetylcholine (nACh) receptor

Novel DNA primase inhibitor

Novel DNA primase inhibitor

Novel potentiator of β-lactam activity against Gram positive and Gram negative pathogens

Novel antitubercular and antiparasitic agent, possessing excellent in vitro activity against both L. donovani and Leishmania infantum as well as displaying a better safety profile

Analeptic agent, stimulating central nervous system; Anti-barbiturate-overdose

Highly potent cytotoxic microtubule inhibitor

Selective MAO-B inhibitor

Dual orexin receptor antagonist (OX1R and OX2R antagonist or DORA)

Anthelmintic, for the treatment of parasites such as gastrointestinal roundworms, lungworms, eyeworms, grubs, sucking lice and mange mites in cattle

Tricyclic antidepressant (TCA), acting as a serotonin–norepinephrine reuptake inhibitor (SNRI) and also having other activities including antihistamine, antiadrenergic, antiserotonergic, anticholinergic, and sodium channel-blocking effects

Agonist of GABAA receptors α15 subunits

Novel antibacterial with activity against the Gram-negative bacteria associated with nosocomial infections

Novel effective and selective inhibitor of E. coli topoisomerase I

Novel 2-aminoethyl diphenylborinate (2-APB) analogue, inducing a profound activation of SOCE in DT40 cells, albeit at low concentrations (10 nM), blocking the melatonin-induced [Ca ] cyt increase and SOCE in P. falciparum.