Novel boron-containing dopa-derivative, acting as a bladder relaxant through non-catecholamine receptors

Novel Dual PROTAC for Simultaneous Degradation of EGFR and PARP

First Potent Small Molecule Ligand for MALAT1

Novel highly selective agonist for the δ-opioid receptor, producing less convulsions than most drugs from this family and having antidepressant-like effects

Novel inhibitor of dipeptidyl peptidase 7 (DPP7)

Novel selective DPP8/9 inhibitor, blocking AML progression in vivo

Substrate of CYP3A and inhibitor of P-glycoprotein

Novel DprE1 inhibitor, killing M. tuberculosis

Click chemistry tool molecule in probing peptidoglycan (PG)

Novel Dual PROTAC for Simultaneous Degradation of EGFR and PARP

Novel inhibitor of the interaction of hACE2 with the spike proteins of SARS-CoV-2 as well as SARS-CoV

Novel inhibitor of the interaction of hACE2 with the spike proteins of SARS-CoV-2 as well as SARS-CoV

Oral non-opioid anti-tussive agent for treatment of cough

Inhibitor of the growth of estrogen receptor-presenting breast cancers

Novel potent PTHR1 antagonist

Novel selective PPARγ modulator, resulting in robust plasma glucose reductions with excellent DMPK profiles

Novel potent orally active hepcidin production inhibitor

Novel and orally bioavailable PTHR1 antagonist

Novel non-macrolide GPR38 agonist

Novel potent orally active hepcidin production inhibitor

Novel Potent, Orally Available G9a/GLP Inhibitor for Treating β-Thalassemia and Sickle Cell Disease

Pathogen motility inhibitor of EcDsbA

Non-toxic human papillomavirus E6 inhibitor

Novel Plasmodium falciparum Dihydroorotate Dehydrogenase (PfDHODH) Inhibitor (Pfalcip cells: 0.0018 μM)

Novel potent inhibitor of dihydroorotate dehydrogenase (DHODH)

Novel potent Dihydroorotate Dehydrogenase (DHODH) inhibitor

Novel selective mGlu5 receptor negative allosteric modulator (NAM) with potent antidepressant and antimanic activity

Agonist of S1P receptors

Novel potent and orally active activator of PP2A

Negative control for DT2216

Potent and selective degrader of mutant FKBP12F36V fusion proteins

Antiviral agent against influenza A, parainfluenza Sendai, coxsackie A21, and rhinovirus

Irreversible DNA minor groove binding alkylating agent, disrupting the nucleic acid architecture and leading to tumor cell death

Anthracycline antibiotic from Streptomyces

Selective 5-HT2A receptor antagonist

Potent and selective 5-HT 2A receptor antagonist

Novel potent and highly selective inhibitor of VEGFR, exhibiting antitumor activities both in vitro and in vivo.

Novel and potent leukotriene B(4) receptor antagonist

Novel Hsp70 agonist, showing no cellular toxicity and induced cellular stress response pathways

Novel allosteric inhibitor of the tumor-promoting interaction between the oncogenic factor AIMP2-DX2 and HSP70

Antitumor antibiotic

Novel Selective and Potent EGFR Inhibitor, Overcoming T790M-Mediated Resistance in Non-Small Cell Lung Cancer

Novel potent Inhibitor of PI3Kalpha

Novel OPG/RANKL upregulator, increasing OPG expression without affecting RANKL expression, promoting osteoblast differentiation while inhibiting osteoclast differentiation, regulating OPG expression through canonical Wnt/β-catenin signaling

γ-Secretase modulator (GSM) photoaffinity probe, revealing distinct allosteric binding sites on presenilin

Potent Activator of P53-Independent Cellular Senescence

Novel XIAP BIR2 domain-binding degrader of E3 ubiquitin ligases

Sigma1 receptor ligand and potential atypical antipsychotic

Novel degrader of GST-α and GST-α-EGFP fusion proteins as well as endogenous GST-π in cells and lysates

Highly potent and selective activator of isozymes CA-VA and CA-VII

Highly potent and selective activator of isozymes CA-VA and CA-VII

Novel Oral and Selective Prostaglandin F 2α (PGF 2α ) Receptor Antagonist

Novel PP1-targeting Ebola Virus (EBOV) inhibitor with improved pharmacological properties

Novel dose-dependent inhibitor of HDAC1, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, and HDAC9, inhibiting Pseudomonas aeruginosa alginate synthesis

Novel EBV activator, well-performing EBV lytic cycle inducer

Novel potent specific inhibitor of EcDsbB, targeting disulfide bond forming enzyme

Novel specific inhibitor of EcDsbB, targeting disulfide bond forming enzyme DsbB of Gram-negative bacteria

Novel marine-derived anticancer saponin, targeting topoisomerase2alpha by unique interference with its DNA binding and catalytic cycle

Lipo-pro-prostaglandin E1, preventing hearing disturbance and equilibrium dysfunction due to inner ear microcirculatory disorders

An impurity of Edoxaban, a novel inhibitor of factor Xa

Novel eEF2K inhibitor, inducing significant apoptosis through classical apoptotic pathways

Potent agonist of peroxisome proliferator-activated receptor gamma (PPAR-gamma) with potential antineoplastic activity

Calcium channel blocker, blocking both T-type and L-type calcium channels

Natural alpha-aminobutyric acid-rich secondary metabolite of fungi, strongly inhibiting the BBMV V-ATPase, acting as a mitochondrial complex V inhibitor, showing antitumor activity in vivo

Antibiotic, inhibiting bacterial protein synthesis

Novel third-generation EGFR tyrosine kinase inhibitor, targeting EGFR T790M mutation in advanced non-small cell lung cancer

Novel EGFR inhibitor, attenuating Ang II-induced Kidney Fibrosis

Novel EGFR inhibitor, significantly reducing myocardial inflammation, fibrosis, apoptosis, and dysfunction, showing promises to the treatment on obesity-induced cardiac complications

Novel EGFR inhibitor, attenuating Ang II-induced Kidney Fibrosis

Potent inhibitor of adrenergic alpha1, alpha2c, 5-HT2a, 5HT7 receptors; Relatively selective blocker of adrenergic alpha2c over adrenergic alpha2a receptors.

Selective, non-competitive AMPA receptor antagonist, improving motor co-ordination

Antibacterial agent

Arginase Inhibitor, activating EPO-mediated mitochondrial function and haemoglobin expression, stimulating melanogenesis by MAP kinase activation and tyrosinase upregulation

Potent and bio-stable inhibitor of the chicken sEH (chxEH)

Potent and bio-stable inhibitor of the chicken sEH (chxEH)

Potent and bio-stable inhibitor of the chicken sEH (chxEH)

Novel Mirk kinase inhibitor, inhibiting DYRK1A-induced Tau phosphorylation at multiple AD-relevant sites, blocking the in vivo growth of pancreatic cancer cells

Novel water-soluble analog of progesterone

Novel water-soluble analog of progesterone, reducing cerebral edema and lesion size and improving functional recovery, decreasing glial fibrillary acidic protein expression immunoreactivity

Novel RNA-competitive, ATP-uncompetitive eIF4A Inhibitor, decreasing BJAB Burkitt lymphoma cell viability, engaging a novel pocket in the RNA groove of eIF4A and inhibiting unwinding activity by interfering with proper RNA binding and suppressing ATP hydr

Novel anti-bacterial agent, targeting the MmpL3 transporter in Mycobacterium abscessus

Novel Cell-active Inhibitor of the Undrugged Oncogenic PTP4A3 Phosphatase

Novel Cell-active Inhibitor of the Undrugged Oncogenic PTP4A3 Phosphatase

Novel etomidate analogue, enhancing GABA A receptors currents with a concentration for 50% of maximal effect (EC 50 ) of 0.98 {plus minus} 0.02 μM, which was about three times more potent than etomidate (3.07 {plus minus} 1.67 μM), retaining the favorable

Novel inhibitor of Aurora B kinase

Novel ligand of the apelin receptor (APJ), possessing high affinity for APJ (Ki 4.6 nM) and producing cardiorenal effects in vivo similar to those of ELA

Oleoylethanolamide-modelled PPAR

Novel γ-secretase inhibitor

Novel highly potent, selective, and CNS-penetrant inhibitor of elongation of very long chain fatty acid 1 (ELOVL1) enzyme

Eukaryotic Ribosomal Selective Glycoside (ERSG), inducing read-through of premature stop codons (PSCs) and resulting in translation of full-length protein

Novel BCL-2 inhibitor, neutralizing the antiapoptotic activity of overexpressed BCL-2 toward staurosporine and sensitizing BCL-2-expressing cells from leukemic patients to the killing effects of staurosporine, chlorambucil, and fludarabine

High affinity ligand for estrogen receptor-

Novel potent antitumor agent, inducing apoptosis in a panel of tumor cell lines

Novel potent and highly selective c-Met inhibitor

PDE 3 inhibitor

Non-peptide angiotensin II receptor antagonist

Novel peptide endomorphin (EM) degradation blocker

Novel peptide endomorphin (EM) degradation blocker

Novel peptide endomorphin (EM) degradation blocker

Novel corticotropin-release factor 1 antagonist

5-FU derivative, with various anticancer agents against human cancer xenografts

Novel PRMT inhibitor, preventing arginine methylation of cellular proteins, being essentially inactive against the lysine methyltransferase SET7/9

Novel Potent and Selective Inhibitor of Protein Arginine Methyltransferase 4 (PRMT4)

Antioxidant, inhibiting free radical oxidation of biomembrane lipids, modulating the activity of membrane-bound enzymes and the receptor complexes of the brain membranes

Novel non-steroidal CYP17 inhibitor. reducing androgen synthesis for treatment of castration-resistant prostate cancer

Novel butyrylcholinesterase inhibitor against Alzheimer's disease

Novel Potentiator of α7 Receptor Signaling

Useful pharmceutical building block

Antimalarial

Natural vesicle trafficking inhibitor

Specific inhibitor of trafficking pathways, disrupting recycling at the PM via interference with ROP6/RIC1 signalling

Novel inhibitor of eukaryotic ARF-GEFs (ADP-ribosylation factor guanine nucleotide exchange factors)

Specific inhibitor for plant callose deposition during cytokinesis without affectting endomembrane trafficking during interphase or cytoskeletal organization

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