Novel modulator of the PIN1 accumulation, selectively modifying PIN1 basal plasma membrane targeting in Arabidopsis with minimal effects on apical plasma membrane proteins

Novel modulator of the PIN1 accumulation, selectively modifying PIN1 basal plasma membrane targeting in Arabidopsis with minimal effects on apical plasma membrane proteins

Sodium/hydrogen exchange inhibitor

Novel potent inhibitor of eleven-nineteen leukemia (ENL) protein, selectively targeting the ENL YEATS domain

Novel oral inhibitor of angiogenic and proliferation kinases, having activity in recurrent, platinum resistant ovarian cancer

Novel potent inhibitor of ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1 or NPP1), showing good in vitro potency, stability in SGF/SIF/PBS, selectivity, ADME properties and pharmacokinetic profile and finally potent anti-tumor response in viv

PGE2 analog, inhibiting gastric acid secretion

Dopamine D2-receptor agonist for the treatment of extrapyramidal disorders, also being an antiparkinson agent

Entasobulin is a β-tubulin polymerization inhibitor with potential anticancer activity.

Novel inhibitor of Ectonucleoside Triphosphate Diphosphohydrolase 5 (ENTPD5)

Novel inhibitor of Ectonucleoside Triphosphate Diphosphohydrolase 5 (ENTPD5)

Unnatural verticilide enantiomer, inhibiting type 2 ryanodine receptor-mediated calcium leak and being antiarrhythmic.

Novel, potent, and selective Factor XIa inhibitor

Vitamin E derivative, suppressing inflammation during hepatic ischemia-reperfusion injury and exerting hepatoprotective effects

Novel potent and selective leucyl-tRNA synthetase inhibitor

Novel agonist of EphA2 receptor tyrosine kinase

Potent and selective covalent inhibitor of receptor tyrosine kinase EphB1

Novel clickable potent and specific inhibitor of EphB3

The first potent and specific inhibitor of a single Eph isoform EphB3

Novel selrctive SETD8 inhibitor without inhibiting G9a, SETD7, RmtA, and PRMT1

Novel stabilizer of 14-3-3 PPIs, Diastereoepimer of aminopeptidase inhibitor bestatin

Second-generation antihistamine and mast cell stabilizer, being highly selective for the H1 receptor

The precursor of the nocardicins

Mucolytic and bronchospasm relieving agent

Novel inhibitor of extracellular polymeric substances (EPS)

Potent, selective, high efficacy 5-HT1A receptor agonist

Inactive isomer of EPZ005687 and can be used as the negative control for EPZ005687

Novel selective SMYD3 inhibitor

Novel selective SMYD2 inhibitor

Novel SMYD2 inhibitor

Novel Oral Selective Estrogen Receptor Degrader with Highly Improved Antitumor Effect and Favorable Druggability

Selective squalene synthase (SQS) inhibitor

Retinoic acid receptor (RAR) subtype α-selective agonist

Novel Selective ERAP1 Inhibitor

Novel competitive inhibitor of ERAP1 aminopeptidase activity

Novel ErbB type I receptor tyrosine kinase inhibitor for the treatment of hyperproliferative diseases

Novel potent inhibitor of ERCC1-XPF activity, targeting DNA repair in tumor cells

Natural Nsp15 inhibitor against SARS-COV2

Novel ATP-competitive Selective c-Jun N-terminal kinase (JNK) inhibitor

Analogue of the lipid A portion of the endotoxin lipopolysaccharide (LPS) with potential immunomodulating activity, binding to the Toll-like receptor (TLR)/CD14/MD2 receptor complex, inhibiting the activation of the receptor complex by LPS

Negative control for ERK Inhibitor II AOB6420

Novel degrader of ERK1/2, eliciting downregulation of phospho-ERK1/2 signal.

Novel PROTAC Estrogen-related Receptor α (ERRα) Degrader

Novel Activator of the Anticipatory Unfolded Protein Response with Enhanced Selectivity for Estrogen Receptor Positive Breast Cancer

The first ERβ-targeted near-infrared (NIR) inherently fluorescent probe, showing the advantages of high ERβ selectivity, good optical properties, and excellent ERβ imaging capability in living cells

Carbapenem antibiotic, inhibiting cross-linking of the peptidoglycan layer of bacterial cell walls by blocking penicillin-binding proteins (PBPs)

Novel thermosensitive fluorescent dye, visualizing thermogenesis in stimulated single-cell brown adipocytes

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Novel potent inhibitor of recombinant human and mouse Transglutaminase enzyme activity, mainly TG2 and the close related enzyme TG1

Anti-HBV agent, showing activities on HepG 2.2.15 cell line in vitro

Precursor of adrenaline, suppressing the locomotor stimulation by MAO inhibitor

Broad-spectrum, topical macrolide antibiotic, diffusing through the bacterial cell membrane and reversibly binding to the 50S subunit of the bacterial ribosome

Serotonin 5-HT2A Agonist

Novel Highly Soluble σ1 Receptor Antagonist for Pain Management

Selective estrogen receptor modulator (SERM), exhibiting estrogen agonism in certain tissues and estrogen antagonism in others

Non-Peptidic, potent, and orally active stromelysin inhibitor, blocking cartilage degradation

H-89 analog as PKA and AKT1 inhibitor with specificity on no longer inhibiting CAMK2B and neither affecting viability of mice nor causing any detectable tissuedamage at the dose given

Novel inhibitor of PORCN, inhibiting ß-catenin reporter activity in a dose-dependent manner

Cell-impermeant viability indicator, as high-affinity nucleic acid stain that is weakly fluorescent until bound to DNA and emits red fluorescence (excitation/emission maxima ~528/617).

Novel anticancer agent

Natural potent antiviral agent, significantly inhibiting coxsackievirus group B (CVB) replication both in vivo and in vitro

Novel selective FTO inhibitor

TRPA1 channel agonist

Activator of β2 and β3 subunit containing channels of the GABAA receptor complex, stimulating the production of GABA(A) active neurosteroids

Novel enhancer of the religation reaction of human topoisomerase I

Partial agonist at the glutamate binding site of the GluN2 subunits

Pesticide, acting as antibiotics or growth regulators to kill mites and ticks

Potent and selective inhibitor of Pim 1, inhibiting the phosphorylation of Bad and 4EBP1 in cells and suppresses the proliferation of several non-solid and solid human tumor cell lines.

Novel broad-spectrum β-lactamase inhibitor

Novel Biased modulator of NMDA receptors, controlling channel opening and ion selectivity

Novel negative allosteric modulator (NAM) of NMDA receptors, reducing both the overall current that flows following receptor activation and the flux of Ca2+ ion relative to monovalent cations

Scavenger for oxidative species such as peroxynitrite, superoxide, and hydrogen peroxide

The first plant cyclic peptide with antibacterial and antifungal activity

Novel potent gamma-secretase modulator

Novel GluN2B antagonist, binding at the same GluN1/GluN2B dimer interface as ifenprodil but adopting a remarkably different binding mode involving a distinct subcavity and receptor interactions

Novel partial positive allosteric GABAA receptor modulator

Novel ALK5 inhibitor

Novel glucagon-like peptide 1 (GLP-1) receptor agonist, displaying significantly elongated half-lives and improved long-acting antidiabetic activity in the presence of endogenous anti-DNP antibodies

Potent and selective SIRT1 inhibitor

Potent and selective SIRT1 inhibitor

Topoisomerase I inhibitor

Novel Dual-Analyte Fluorescent Chemosensor for Visualizing Neurotransmitter Exocytosis

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

Polyethylene glycol conjugate of SN38, acting as a topoisomerase I inhibitor,, exerting significant anti-leukaemia activity, overcoming ABCG2-mediated topotecan resistance

Novel influenza A hemagglutinin (HA) fusion inhibitor (EC 50 = 1.9 ± 0.3 μM), preventing HA from transitioning to the postfusion state at pH 5.0

Novel antifungal agent against Candida albicans persister cells

Novel potent and selective MAP4K4 inhibitor

Novel bactericidal, killing Mycobacterium tuberculosis by targeting iron-sulfur protein Rv0338c (IspQ), a putative redox sensor

Novel bactericidal, killing Mycobacterium tuberculosis by targeting iron-sulfur protein Rv0338c (IspQ), a putative redox sensor

Selective, potent inhibitor of the late current mediated by the cardiac isoform of the sodium channel (NaV1.5)

Novel and potent inhibitor of PCAF catalytic domain

Novel matrix metalloproteinase inhibitor, reducing secretion of very low density lipoprotein-triacylglycerol, lowering TAG levels in serum and the liver, VLDL-TAG secretion, de novo FA synthesis in the liver, and serum levels of insulin and glucose

Novel pyrimidine synthesis inhibitor, exhibiting low micromolar antiviral activity against various influenza A and B virus strains, including the highly pathogenic influenza A strains H5N1 and H7N9, enterovirus A71, respiratory syncytial virus, human rhin

Novel clickable fumarate-competitive chemoproteomic probe

Novel FabH Inhibitor, showing potent antibacterial activity with a MIC value of 3.89–7.81 μM−1 against the tested bacterial strains and exhibiting potent E. coli FabH inhibitory activity with an IC 50 value of 1.6 μM

Novel inhibitor of β-ketoacyl-(acyl-carrier-protein) synthase III (FabH).

Novel FABP4/5 inhibitor, inhibiting lipolysis in 3T3-L1 adipocytes and in primary human adipocytes, reducing plasma triglyceride and free fatty acid levels, ameliorating dyslipidemia but not insulin resistance in mice with diet-induced obesity

Novel dual inhibitor of fatty acid binding protein 4 (FABP4) and fatty acid binding protein 5 (FABP5)

Novel dual inhibitor of fatty acid binding protein 4 (FABP4) and fatty acid binding protein 5 (FABP5)

Novel factor VIIa inhibitor

Novel factor VIIa inhibitor

Novel antileukaemic alkaloid; Inhibitor of reverse transcriptase activity of RNA-tumor viruses; Inhibitor of topoisomerase I

Novel Folate Receptor Targeting and Cathepsin B-Sensitive Drug Delivery System for Selective Cancer Cell Death and Imaging, exhibited strong cytotoxicity against FR-overexpressing SK-Hep-1, HeLa, and Siha cells, with IC50 values of 2-3 μM, but had no effe

Novel folate-appended 2-hydroxypropyl-ß-cyclodextrin (HP-ß-CyD), showing strong anti-leukemia and cell-binding activities, inhibiting the growth of FR-expressing cells, enterjng CML cells through endocytosis and inducing both apoptosis and autophagy via m

Novel inhibitor of fungal fatty acid biosynthesis, demonstrating broad-spectrum activity against Candida auris and mucormycetes and retained the activity against azole-resistant candida isolates

Novel blocker of focal adhesion kinase (FAK) autophosphorylation

Novel highly potent FAK-targeting PROTAC degrader, showing a rapid and reversible FAK degradation

Novel Fluorescent HIF-1α peptide

Potent and bioavailable irreversible inactivator of PAD4

Nonsteroidal anti-inflammatory drug (NSAID)

Inhibitor of neutrophil superoxide production

Novel FAP-targeted Fluorescein dye conjugate

Novel FAP-targeted NIR dye conjugate

Inducer of apoptosis via regulation of L11 and c-Myc with combinational potential with anticancer drugs in non-small-cell lung cancers

Stable and persistent PKC activator

Novel folate-caged pomalidomide-based anaplastic lymphoma kinase (ALK) PROTAC, effectively degrading ALK fusion proteins in cancer cells in a FOLR1-dependent manner

Novel inhibitor of C. difficile's FASII pathway

Novel potent and specific fatty acid synthase (FASN) inhibitor

Novel fatty acid synthase (FASN)

Novel folate-targeted TLR7 agonist, selectively accumulating in profibrotic macrophages and suppressing fibrosis-inducing cytokine production, reprograming M2-like fibrosis-inducing macrophages into fibrosis-suppressing macrophages, resulting in dramatic

Dopamine D4 receptor antagonist

Novel irreversible dopamine D2 receptor ligand, covalently binding the L94C mutant of the dopamine D2 receptor

Dopamine D4 receptor antagonist

Highly potent and selective dopamine D4 receptor agonist

Potent and selective dopamine D3 receptor partial agonist

First-in-class covalent allosteric inhibitor of fructose-1,6-bisphosphate aldolase (FBA) from Candida albicans (CaFBA)

Novel potent αvβ3 antagonist. reducing GBM tumor growth and viability by up to 98%

Novel CAIX inhibitor, inhibiting breast cancer invasion and metastasis

Specific inhibitor of inflammasome assembly, targeting the NLRP3 inflammasome by interfering with the proximity-induced autocleavage of procaspase-1

Novel phosphodiesterase 4 (PDE4) inhibitor with little emetic potential, blocking MPP+ induced oxidative damage in SH-SY5Y cells and neurons via AMPK-dependent autophagy

Novel rapamycin derivative, targeting polycystic kidneys due to the high expression of the folate receptor (FRα), lacking the extra-renal effects of unconjugated rapamycin, in particular immunosuppressive effects

Novel potent antimalarial agent, binding to ferriprotoporphyrin-IX (FeIII-PPIX) (Kd = 33 nM) against chloroquine-resistant and sensitive strains of Plasmodium falciparum

Potent, selective, noncompetitive glutamate mGluR5 receptor antagonist

Non-steroidal anti-inflammatory drug, being used for symptomatic relief for rheumatoid arthritis, osteoarthritis, and mild to moderate pain

Non-steroidal antiinflammatory agent

Novel oral iron therapy agent, being effective in correcting iron deficiency anemia in patients with inflammatory bowel disease

Novel ferroptosis inducer, killing selected cancer cell lines by harnessing reactive oxygen species (ROS)

Iron chelator, mediating iron transport in Streptomyces pilosus

Natural potent colchicine site binding microtubule-destabilizing agent with anti-proliferation and anti-metastasis activity via PAK1 and p21-mediated signaling in breast cancer cells

Selective orthosteric agonist of human FFA2

Selective and moderately potent positive allosteric modular (PAM)-agonist of the FFA3 receptor

Novel PAM-antagonist of the function of C3 at FFA3

Novel fluorescent probe as an excellent VMAT2 substrate capable of detecting VMAT2 activity in intact cells using fluorescence microscopy

Potent, reversible, ATP-competitive inhibitor against PDGFRβ, FGFR-1, and VEGFR-2 (IC50 = 20, 90, and 240 nM, respectively) and effectively suppresses VEGF-stimulated proliferation of HMVECs (EC50 = 420 nM).

Novel, covalent, highly potent, and exquisitely specific FGFR4 inhibitor

Novel potent and selective covalent inhibitor of FGFR4 kinase

Novel highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4, exhibiting excellent potency against FGFR4, FGFR4V550L, and FGFR4V550M with nanomolar activity in both the biochemical and cellular assays while sparing FGFR1/2/3

Novel potent and selective FGFR4 inhibitor, covalently binding to FGFR4 protein

Novel potentl and selective covalent FGFR inhibitor, inhibiting proliferation of FGFR-amplified cancer cell lines with low nM IC50 values

Novel regulator of transcription factor PU.1-DNA binding interactions, acting as a weak agonist that recruits PU.1 to DNA

Novel inhibitor of the Wnt/β-catenin transcriptional activity, demonstrating significant increased rate of apoptosis in Huh7 and PLC/PRF

Novel light-regulated diltiazem derivative, photoswitching LTCC in pancreatic β cells, cardiomyocytes and mouse hearts

Fibroblast growth factor fragment

Potent macrophage activator, enhancing interleukin 12-dependent interferon gamma production by lipopolysaccharide-stimulated mouse splenocytes, exerting an antiviral action against HSV-1 with the independent pathways of IFN-alpha

Cell-adhesive octapeptide as the authentic sequence within intact fibronectin, mediating OSCC cell spreading, migration, and invasion, regulating IL-17A levels and mechanical allodynia after peripheral nerve injury

Antibacterial agent, expressing enhanced activity at acidic pH

Natural potent cytotoxic agent

Fluorescent protein-protein interaction (PPI) inhibitor

Highly potent membrane-permeable ligand of the immunophilin FKBP12, creating a new composite FKBP12-FK506 surface and inactivating calcineurin, a Ca calmodulin-dependent protein phosphatase

Novel non-peptide bradykinin (BK)-B2 receptor antagonist

Novel Inhibitor of FKBP12

Specific inhibitor of several viruses belonging to the family of flaviviridae

Natural anticancer and antioxidant

Novel, potent, orally active, and nonsteroidal farnesoid X receptor (FXR) antagonist with propensity for accumulation and responsiveness in ileum

Novel inhibitor of general secretion in early stage; FLI-06 analogue twice as active as FLI-06

Curcumin analogue, exhibiting enhanced growth-suppressive activity and inhibiting AKT and signal transducer and activator of transcription 3 phosphorylation in breast and prostate cancer cells

Curcumin analogue, exhibiting enhanced growth-suppressive activity and inhibiting AKT and signal transducer and activator of transcription 3 phosphorylation in breast and prostate cancer cells

Inhibitor of STAT3 phosphorylation and apoptotic promoter of human renal cell carcinoma and melanoma cell lines

Tumour hypoxia probe

Novel FLT3 inhibitor, displaying potent inhibitory activity against the FLT3-ITD mutant (IC 50 = 0.8 nM) and good selectivity over c-KIT kinase (over 500-fold), selectively inhibiting the proliferation of FLT3-ITD-positive AML cell lines MV4-11 (IC 50 = 2

Novel potent ATP-competitive inhibitor of Flt3

Novel selective and efficacious inhibitor of FLT3 mutations

Novel STAT3 activation inhibitor, induces cell cycle arrest and apoptosis in cancer cells harboring constitutively-active STAT3

The first phthalic acid diamide insecticide, impairs neuronal calcium signalling in the honey bees antennae

Novel photolabile NO donor

Herbicide, inhibiting very-long-chain fatty acid elongase (VLCFAE) synthesis

Green-fluorescent intracellular calcium indicator

Green-fluorescent intracellular calcium indicator

Monoamine oxidase A (MAO-A) specific inhibitor

Novel potent neuroprotective agent for treatment of Alzheimer's disease (AD), targeting NMDA receptor

Novel potent neuroprotective agent for treatment of Alzheimer's disease (AD), targeting NMDA receptor

Fungicide for the control of fungal diseases such as early blight, late blight, leaf spots, leaf rust, and Rhizoctonia solani.

Atypical antipsychotic agent and ligand for the serotonin receptors 5-HT6/5-HT7

Antipsychotic agent, blocking postsynaptic dopamine D2 receptors in the limbic, cortical system and basal ganglia

Antipsychotic agent, blocking postsynaptic dopamine D2 receptors in the limbic, cortical system and basal ganglia

Benzodiazepine with sedative, muscle relaxant, anticonvulsant, and anxiolytic activities

alpha2-Adrenergic receptor agonist

Fluorescent probe for monitoring synaptic activity at neuromuscular junctions

Negative control for FM-381

Negative control for Skepinone-L

Novel highly selective inhibitor of Aurora kinases A, B and C, with potent cellular activity and minimal off-target activity (PLK4)

Novel potent and selective Dual inhibitor of PI3K-δ and PI3K-γ

Novel potent dual CDK14 and CDK16 inhibitor

Novel concentration-dependent inhibitor of CRF1R-pPL cotranslational translocation at the level of the Sec61 complex

Novel AMPK activator, inhibiting growth and induces apoptosis in colon cancer and increasing apoptosis in triple negative and estrogen-receptor positive breast cancers

First in class anti-tubercular agent against sensitive and drug-resistant Mycobacterium tuberculosis (Mtb)

Novel fluorescent near-infrared (NIR) linker for building brighter labeled biomolecules, exhibiting no evidence of H-aggregation even at high labeling density when appended to monoclonal antibodies or virus-like particles

Inhibitor of IspD and IspE enzymes isolated from bacteria

Novel BRD PROTAC, being capable of degrading BRDs in a folate receptor-dependent manner in cancer cells

Novel ALK PROTAC, being capable of degrading ALK in a folate receptor-dependent manner in cancer cells