Potent P-glycoprotein (P-gp) inhibitor

Novel selective norepinephrine reuptake inhibitor, displaying significant norepinephrine transporter (NET) inhibitory activity toward the serotonin or dopamine transporters

Tubulin-binding dolastatin-15 analog, demostrating a wide spectrum of In Vivo antitumor activity

Potent and orally active V 1B receptor antagonist with antidepressant and anxiolytic activities in rodents

Potent and selective sphingosine 1-phosphate 1 (S1P1) receptor antagonist (IC50 = 7.8 nM)

Novel potent, selective, and orally active CRTH2 antagonist

Trans-activator of transcription (TAT) peptide, increasing Hepta-histidine (7H) permeability into cells for treatment of iPS cell-derived neurons carrying Tau or APP mutations suppressed Tau phosphorylation

Novel brain penetrant Cx43 hemichannel blocker

Potential neuroprotective agent, showing effects on cellular models of oxidative stress and neuroinflammation

Selective mast-cell-stabilizing agent, inhibiting ozone-induced airway hyperresponsiveness

Novel antagonist of IL-6 signaling

Novel antibiotic against Mycobacterium tuberculosis (Mtb), potently killing replicating, virulent Mtb H37Rv in a clavulanate-dependent manner

Novel potent MCT1 inhibitor, exhibiting good single agent anticancer efficacy properties

Highly potent activator of Nrf2; Potent phase 2 cytoprotective pathway inducer and liver carcinogenesis blocker

Novel TBK1/IKKε inhibitor

Novel anti-angiogenesis and vascular disrupting agent, exhibiting moderate inhibitory cell proliferation activity

Novel anti-angiogenesis and vascular disrupting agent, exhibiting moderate inhibitory cell proliferation activity

Novel agonist for nicotinic acetylcholine receptors (nAChRs), modestly selectively targeting α6β2 subtype

Novel potent and selective ligand of Brd2(2)

Aquaporin 1 (AQP1) channel blocker

Potent CB1 receptor inverse agonist

Novel orally bioavailableγ-secretase modulator, reducing Aβ42 levels

FPR Agonist 43 (compound 43) is a dual formyl peptide receptor 1 (FPR1) and formyl peptide receptor 2 (FPR2)/ALX agonist.

Potent and selective antagonist of adenosine A2A receptors

Non-competitive modulator of the proteasome inducing apoptosis a panel of myeloma and leukemia cell lines

Novel TRPM8 channel blocker

Potent TRPM8 antagonist, exhibiting antiallodynic properties in pain models

Antimalarial; Novel inhibitor of HepG2

Novel Inhibitor of the malaria parasite protein kinase CLK3, inhibiting the development of liver-stage parasites, killing asexual blood-stage parasites at the trophozoite and schizont stages of the erythrocytic cycle, blocking the development of sexual ga

Highly potent NR2B-selective NMDA receptor antagonist

Nonpeptide partial agonist of oxytocin (OT) and vasopressin V2 receptors

Potent and selective polo-like kinase 2 (PLK2) inhibitor

Novel potent and selective CHK1 kinase inhibitor

Novel Integrin very late antigen-4 (VLA-4; α4β1) antagonist, blocking the activation of inflammatory cells.

Novel GPR35 agonist

Insulin receptor sensitizing agent; Selective inhibitor of protein-tyrosine phosphatase 1B (PTP1B)

Potent equilibrative nucleoside transporter 4 (ENT4) inhibitor

Sorafenib analogue, retaining cytotoxicity similar to sorafenib in various human cancer cell lines and strongly inhibiting growth in the NCI-60 cell line panel

Novel degrader of the anaplastic lymphoma kinase (ALK) fusion protein, effectively inducing ALK degradation and inhibiting the growth of ALK fusion positive cell lines, SU-DHL-1 and H3122, significantly reducing the tumor growth in H3122 xenograft model

Novel IKZF1/3 degrader, inhibiting the proliferation of multiple myeloma cells in vitro as well as in vivo

Novel selective opioid receptor antagonist at all three receptor types

Novel potent BET protein degrader, inhibiting cell proliferation due to suppressed C-MYC transcription

Novel long-acting β 2 -adrenoceptor agonist

Hepatotoxicity inducer, significantly up-regulating the expression of genes involved in endoplasmic reticulum stress and Toll-like receptor (TLR) pathway

Novel Specific Copper Chelator, Reducing Memory Impairments in Alzheimer's Disease Mouse Models

Novel potent inhibitor of tyrosyl-DNA phosphodiesterase 1 (Tdp1)

Novel inhibitor of the p53-Hdm2 protein-protein interaction, dose-dependently stabilized P53 and increased P21 and MDM2 expression in JAR choriocarcinoma cells, inducing the p53 regulated gene (PIG-3) and caspase activity

Novel antimalarial agent

Novel inhibitor of viral p37, blocking the ability of virus particles to be released from infected cells, being used for the treatment of smallpox, monkeypox, orthopoxvirus, and orthopoxviral Disease.

Novel monocyte/macrophage targeted histone deacetylase inhibitor

CCR2b receptor antagonist

Natural antibacterial agent, being active against gram-positive bacteria.

Potent and selective M1 antimuscarinic

Mucolitic agent, inhibiting activation of nuclear factor kappa-κB (NF-κB) by blocking phosphoinositide 3-kinase/protein kinase B (PI3K/Akt)/IκB kinase (IKK) activities, showing the anti-inflammatory properties on inflammation-associated skin diseases

Photosensitizing agent used in the treatment of squamous cell carcinoma of the head and neck, also showing activity agaimst COVID-19 Mpro

COX/5-LOX inhibitor and cytokine-modulating anti-inflammatory agent

Peptide vaccine, residues (611-626) of the human telomerase reverse transcriptase catalytic subunit (hTERT), for the treatment of solid cancers

Selective Thromboxane_receptor>thromboxane receptor antagonist

Mutually Orthogonal Bioorthogonal Amino Acid, Enabling Efficient Protein Dual-Labeling in Cells

Reversible inhibitor of vesicular monoamine transporter 2, showing anti-chorea effect and decreasing uptake of monamines into synaptic vesicles, as well as depletion of monoamine storage

Activator of the hepatic interferon pathway in rats

Potent inhibitor of protein synthesis, inhibiting translation by binding within the ribosomal exit tunnel

Inducer of S phase arrest and apoptosis in hepatocellular carcinoma QGY-7701

Antitubercular agent

Potent and selective human leukocyte 5-lipoxygenase (5-LOX) inhibitor

Novel endothelin (ET) receptor antagonist

Novel multipotent anti-Alzheimer agent, selectively inhibiting human butyrylcholinesterase (BChE), having strong antioxidant activity and good β-amyloid (Aβ) anti-aggregation properties

Novel GSK-3β inhibitor, showing anti-neuroinflammatory effects in lipopolysaccharide (LPS) activation of spontaneously immortalized SIM-A9 microglial cells and of mouse cortical microglia, inhibiting LPS-induced production of nitric oxide and the proinfla

Novel cell-active, selective class IIa HDAC inhibitor

CNS-penetrant selective class IIa histone deacetylase (HDAC) inhibitor, exploiting the >100-fold selectivity over class I/IIb HDACs

Cyclized tamoxifen analog, selective ER modulator (SERM)

Novel and Potent Stem Cell Mobilizer; Inhibitor of SDF-1α/CXCR4 binding

Novel potent SARS coronavirus (CoV) 3CL protease inhibitor (Ki = 53 nM)

Novel dual VEGFR/Src kinase inhibitor

Novel inhibitor of T315I mutant enzyme, exhibiting reasonable in vivo efficacy in a xenograft mouse model harboring T315I

Novel, Potent, Selective, Water Soluble, Brain-Permeable EP2 Receptor Antagonist

Novel inhibitor of mitochondrial calcium uptake (#333333; font-family: "Open Sans", HelveticaNeue, "Helvetica Neue", Helvetica, Arial, sans-serif; font-size: 15px; font-style: normal; font-variant-ligatures: normal; font-variant-caps: normal; font-weight:

Highly selective, potent, cell-permeable fluorescent irreversible tissue transglutaminase (TG2) inhibitor

EP2 allosteric potentiator

Potent and selective nociceptin opioid receptor (NOP) agonist

Potent and selective nociceptin opioid receptor (NOP) agonist

Potent and selective nociceptin opioid receptor (NOP) agonist

Potent and Selective Antagonist for Human EP2 Receptors

Novel potent and structure-specific inhibitor of pre-miR-200c, reversing a type 2 diabetes phenotype

Novel potent TGR5 agonist, displayind a significant glucose-lowering effect and stimulated GLP-1 and insulin secretion in TGR5H88Y mice but not in wild-type animals

Novel Potent Agonist of TGR5 Receptor

Cell-permeable, potent, and selective inhibitor of PI 3-K isoforms p110ß/p110d

Potent and selective inhibitor of PI 3-K

Novel highly potent and specific inhibitor of TLR8, targeting an unconventional pocket on the TLR8 protein-protein Interface

Natural potent human carboxylesterase 2 (hCES2) inhibitor (IC50: 5.05 μM)

Natural antibiotic, being active against P. aeruginosa both in vitro and in vivo.

Novel glutaminase activity inhibitor, showing a partial uncompetitive inhibition in vitro and a significant reduction of ammonia and glutamate production in vivo

Prodrug of Thiamphenicol, inhibiting the 50S subunit of the bacterial ribosome and protein translation

Novel antibiofilm agent, disturbing symbiotic balance between C. albicans and S. mutans in dual species biofilm

Highly efficient bioregulator of plant morphogenesis in the tissue culture technique, inducing diverse responses ranging from induction of callus to embryogenesis or organogenesis, acting through modulation of the endogenous plant growth regulators, modif

Novel protein-protein interaction inhibitor of PAC3 homodimer

Novel selective anticancer agent, selectively inducing cancer cell death in a caspase independent pathway

First-in-class potent, selective, reversible, and tight binding inhibitor of human monoamine oxidase B (hMAO-B) (hMAO-B IC 50 = 1.52 ± 0.15 nM)

Novel potent DENV2-NS2B/NS3pro inhibitor

Firefly luciferin analog as a key element of bioluminescent reporters for oxidation state and thiol/disulfide equilibria

GABAA receptor agonist

Novel Potent Inhibitor of the Opioid Receptors and the Ion Channels

Novel inducer of apoptotic cell death in platinum-resistant A2780cis human ovarian cancer cells, exhibitong a strong inhibitory effect in ovarian CSC-LCs in combination with cisplatin

Steroidomimetic and Chimeric Microtubule Disruptor

Selective Tau ligand, selectively binding to neurofibrillary tangles and neuropils in people with Alzheimer's disease

Novel orthosteric-allosteric dual inhibitor of PfHT1 as selective antimalarial agent

Novel orthosteric-allosteric dual inhibitor of PfHT1 as selective antimalarial agent

Novel orthosteric-allosteric dual inhibitor of PfHT1 as selective antimalarial agent

Novel potent, highly selective and orally available PI3Kδ inhibitor

Novel phosphodiesterase 10A (PDE10A) inhibitor for treatment of schizophrenia

Phosphodiesterase 10A (PDE10A) inhibitor

Novel dose-dependent inhibitor of HDAC1, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, and HDAC9; NOX Inhibitor

Novel selective thrombin inhibitor, inducing conformational allostery

Novel multivalent ligand that bridges the allosteric and orthosteric binding sites of the M2 muscarinic receptor

Anti-epileptic and anticonvulsant agent, acting as a selective GABA reuptake inhibitor

Anthraquinone-fused enediyne antitumor agent for development of antibody-drug conjugates (ADCs)

Muscarinic receptor antagonist, anticholinergic,and parasympatholytic

Natural anticancer agent fortreatment of mast cell tumor (MCT)

Widely used oxidation-reduction indicator

Macrolide antibiotic for the treatment of bovine respiratory disease and ovine respiratory disease associated with Mannheimia (Pasteurella) haemolytica

Antiviral, antineoplastic, and anti-inflammatory agent; Orally active interferon inducer, inhibiting Ebola virus (EBOV)

Novel pan-histone-deacetylase inhibitor with alkylating activity

Neurotoxin, acting via vanilloid receptors of sensory nerves

Novel hepcidin antagonist

hPPAR

Dual PPA

hPPAR-pan agonist

Anti-arrhythmia agent

Novel AC220-based FLT3 degrader

Novel AC220-based FLT3 degrader

The first small molecule degrader, inducing anaplastic lymphoma kinase (ALK) degradation, including in non-small-cell lung cancer (NSCLC), anaplastic large-cell lymphoma (ALCL), and neuroblastoma (NB) cell lines

The first small molecule degrader, inducing anaplastic lymphoma kinase (ALK) degradation, including in non-small-cell lung cancer (NSCLC), anaplastic large-cell lymphoma (ALCL), and neuroblastoma (NB) cell lines

Novel Insulin Receptor Modulator

Novel Toll-Like Receptor 4 (TLR4) Inhibitor

Novel potent and selective dual TLR7/8 inhibitor

Novel toll-like receptor 8 (TLR8) inhibitor, potently and selectively reducing TLR8-mediated signaling

The first small molecule inhibitor of translesion synthesis (TLS) that target Rev1-CT

Potent histone methyltransferase inhibitor with rapid antimalarial activity against all blood stage forms in Plasmodium falciparum

Novel inhibitor of both JAK/STAT and proteasome activities, inducing cell death in myeloma cells

Novel inhibitor of plasminogen activator inhibitor-1 (PAI-1)

Penem beta-lactam antibiotic

Novel protease inhibitor (PI) against a variety of HIV-1 strains, including multi-PI-resistant strains, and may be less likely to generate resistance, also showing antiviral avtivity as a potential treatment for COVID-19 caused by SARS-CoV-2

Dual Inhibitor of SIRT2 Deacetylase and Defatty-Acylase Activities

Novel degrader of E. coli DHFR (eDHFR), as well as eDHFR-EGFP fusion proteins, demonstrating that degradation does not require covalent attachment of the tag to the target protein

Novel caged protein labeling agent

Allosteric agonist and positive allosteric modulator (PAM) of 5-HT3 receptor

Novel activator of necrostatin-1 sensitive necroptotic cell death, triggering apoptosis, autophagy and necroptosis crosstalk in chronic myeloid leukemia

Novel potent inhibitor of TNF-α

Novel inhibitor of tumor necrosis factor-α (TNF-α)

Emivirine analog with improved activity against drug-resistant HIV mutants

Novel non-nucleoside reverse transcriptase inhibitor of HIV-1

Novel selective inhibitor of TNKS-USP25 interaction, effectively reducing prostate cancer cell proliferation and tumor growth

Novel highly potent and selective TNKS2 inhibitor with antiproliferative effects in a colorectal cancer cell line (DLD-1) where the Wnt pathway is constitutively activated

Highly potent and selective tankyrase inhibitor

Novel potent and selective tankyrase (TNKS) inhibitor

Unique multitargeting drug conjugate with extremely low propensity for development of resistance, targeting RNA polymerase, DNA gyrase, and DNA topoisomerase IV

Novel Human Toll-like Receptor 8-Selective Agonist

Stimulator of metabolism, preventing diseases associated with parturition and peri-partum period, developmental and nutritional disorders in young animals, and bone growth disorders and tetany or paresis caused by calcium, magnesium, and phosphorus metabo

Natural agonist of TPRC1/4/5 channels, also acting as a dual PKCα and PKCθ activator, inducing an insulin resistant phenotype by inhibiting IRS1 and the PI3K/Akt pathway, activating the heat shock factor 1 (HSF1) transcription factor driving glucose depen

Novel dual TOP1 and TDP1 inhibitor, inducing both cellular TOP1cc, TDP1cc formation and DNA damage, resulting in cancer cell apoptosis at a sub-micromolar concentration

Novel narrow spectrum kinase inhibitor, potently inhibiting P38a, Src, and Syk kinase activities

Novel Selective Inhibitor of Endoplasmic Reticulum α-Glucosidase II, Exhibiting Antiflaviviral Activity

Novel highly specific fluorescent TOPK inhibitor

Nucleic acid stain, acting on viable, early apoptotic and necrotic cells differentially, showing specific staining of nuclei without any staining of the cytoplasm

Natural psychoactive agent

Chromogenic peptide substrate for the rapid and specific photometric assay of recombinant hirudin (r-hirudin)

Selective CA IX inhibitor

Novel ToxT inhibitor, reducing Vibrio cholerae virulence in vivo and effectively inhibiting intestinal colonization in the infant mouse

Novel probe for activin receptor-like kinase (ALK4 and ALK5)

Novel inhibitor of O-GlcNAcase (OGA)

Novel probe for CECR2/BPTF bromodomains

First-in-class fluorescent drug delivery vesicle that can efficiently load both water-soluble and -insoluble anticancer drugs

Novel Peripheral Selective Tryptophan Hydroxylase 1 (TPH1) Inhibitor (IC 50 : 42nM) for Obesity and Fatty Liver Disease

Inhibitor of tyrosine recombinases and Holliday junction-resolving enzymes; Antibacterial

Promising amyloid reducing agent by lowering the levels of Aβ.

Novel Specific Inhibitor of Type I Collagen Production in Fibrosis

Novel taxane family member, reducing the brain metastatic colonization of breast cancer cells

Novel tumour progression locus 2 (Tpl2) kinase inhibitor

Enhancer of the cytotoxic effect of immunotoxins (ITs) which results in increased apoptosis in different cancer cells

Mitochondria-activatable luciferin (MAL-Probe)

Novel Type-I Inhibitor of TIE-2

Potent I 2 -imidazoline receptor agonist

Metabolite of Resveratrol

Potent and selective NMDA agonist

Novel HuR binder, modulating HuR-RNA interactions

Novel KGA allosteric inhibitor

Natural resveratrol trimer, acting as a protein kinase C inhibitor

Natural specific inhibitor of γ-secretase, decreasing amyloid-beta levels without influencing cleavage of Notch, showing strong growth inhibitory effects on cancer cell lines and significant anti-complement activity, also acting as a PTP1B inhibitor

Metabolite of Resveratrol

Metabolite of Resveratrol

Novel Highly Selective β2-Adrenoceptor Agonist as an Oral Antiasthmatic Agent

Inhibitor of histone deacetylases

Novel TGR5 agonist, reducing glycemic and dyslipidemic cardiovascular risk in animal models of diabesity

Central sugar signal in plants, regulating sucrose use and allocation, underpinning crop growth and development

Potent and long-acting derivative of the hormone Trenbolone

EC 3.1.1.7 (Acetylcholinesterase) inhibitor, acting as an insecticide, an acaricide, an agrochemical, and a nematicide

AKT Inhibitor, Enhancing Gemcitabine Activity in Pancreatic Cancer Cells

Potent NAE-hydrolyzing acid amidase (NAAA) inhibitor

Metabolite of Trifluoperazine; Antidepressant and antipsychotic

Novel Bromodomain Binding Mimic of Lysine Acetylation