Novel potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis

First-in-class selective, partial CDK2 degrader against hearing loss and cancer, protecting against cisplatin ototoxicity and kainic acid excitotoxicity

Glucokinase activator, decreasing fasting and postprandial glucose in type 2 diabetes mellitus patients

Novel Fibrinolysis Inhibitor, Acting via Interference of a Protein-Protein Interaction

Novel selective inhibitor of 5-Lipoxygenase Activating Protein (FLAP) for the treatment of inflammatory diseases

Novel, potent and selective inhibitor of p38α MAP kinase

Novel potent smoothened inhibitor, demonstrating in vivo activity in abrogating the Hh paracrine pathway as well as anti- tumor effects

Antimicrobials, active against methicillin resistant S. aureus (MRSA)

Potent and selective ATP-competitive Dyrk1B kinase inhibitor

Potent, second-generation, selective histamine-H1-receptor antagonist and mast cell stabilizer

Novel CNS penetrant potent inverse agonist of GHS-R1a (IC 50 (affinity) = 0.77 nM)

Azide-A-DSBSO crosslinker is a mass spectrometry (MS)-cleavable, membrane-permeable, homobifunctional, azide-labeled, acid-cleavable cross-linked peptide. Azide-A-DSBSO crosslinker enables the study of protein-protein interactions via cross-linking mass spectrometry (XL-MS).

Mitochondria-luciferin releasing agent, reacting with mitochondria-activatable luciferin (MAL-Probe), such as TPP-CL2, to release luciferin

Macrolide antibiotic, binding to the 50S subunit of the bacterial ribosome and thus inhibiting translation of mRNA

Excellent photoswitchable agonist for neuronal α7 nAChRs

Novel photoswitchable agonist for peroxisome proliferator-activated receptor γ (PPARγ)

Novel photoswitchable ligand for the cannabinoid receptor 2 (CB2)

Novel photoswitchable agonist for peroxisome proliferator-activated receptor γ (PPARγ)

Potent and selective PFKFB3 inhibitor

Natural potent HDAC inhibitor

Novel chimeric inhibitor of dimeric RAF, inhibiting B-Raf V600E mutan

Novel CCR5 antagonist-based HIV-1 entry inhibitor

Novel HBV core protein allosteric modulator (CpAM), bing to the HAP pocket and modulating HBV capsid assembly in a distinct manner

Novel activator of Pyrin inflammasome

Novel potent nonbrain-penetrant BACE1 inhibitor

Allosteric Inhibitor of the NS2B-NS3 Protease from Dengue Virus

Novel inhibitor of BAG-1-mediated protein interactions, targeting the RAF-MEK-ERK signaling pathway, transformed cells

Selective Dopamine D3 Receptor Antagonist

Novel microtubule inhibitor as the prodrug of BAL27862, activating spindle assembly checkpoint, exerting antiproliferative effects and dose-dependent vascular disruption

Potent ATP-competitive inhibitor of Protein Kinase C (PKC) and Protein Kinase A (PKA)

Antibacterial; Antimicrobial; Inhibitor of DNA gyrase and intracellular accumulation of quinolones

Novel BAM complex inhibitor, interferring with BamA-related processes and affect folding and insertion of OMPs

Novel BAM complex inhibitor, interferring with BamA-related processes and affect folding and insertion of OMPs

Hypoxia-activated prodrug of topoisomerase II inhibitor

Antimalarial; Novel Chloroquine analog against Chloroquine-Resistant Parasites

Natural anti-breast cancer and anti-angiogenic agent

Inhibitor of tumor angiogenesis, growth and metastasis in melanoma

Bile acid transporter inhibitor

The first small molecule inhibitor of Lipid II

Novel fluorescent Bortezomib-GV1001 conjugate for monitoring the delivery of the proteasome inhibitor bortezomib (Btz) to HT-29 cancer cells, exhibiting an improved cytoplasmic availability

Anticancer agent; inhibitor of BMP2K (BIKE) and DRAK1

Bavisant dihydrochloride hydrate (JNJ31001074AAC) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H3 receptor. Bavisant dihydrochloride hydrate can be used for attention-deficit hyperactivity disorder (ADHD) research.

Novel cell-permeable synthetic peptide inhibitor of Bax, blocking apoptosis

Novel glucagon receptor antagonist

Negative control for BAY-091

Novel MNK1 inhibitor, targeting oncogenic protein expression and showing potent anti-tumor activity

Negative control for BAY-3153

Novel potent interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor (IC 50 of 3 nM)

Negative control for BAY299

Control compound for BAY-598, a novel potent inhibitor of SMYD2

Novel allosteric MEK inhibitor with long half-lives, high bioavailabilities, low brain penetration potential and high efficacy in a K-Ras-mutated A549 xenograft model

Negative control for BAY-549

Negative control for BAY-678, a potent and selective human neutrophil elastase (HNE) inhibitor

Novel allosteric MEK inhibitor with long half-lives, high bioavailabilities, low brain penetration potential and high efficacy in a K-Ras-mutated A549 xenograft model

Negaitve control for BAY-390

Novel potent and selective acetyl-CoA carboxylase (ACC) inhibitor

Novel potent and selective acetyl-CoA carboxylase (ACC) inhibitor, blocking WNT3A lipidation, secretion, and signaling

Selective inhibitor of type A monoamine oxidase with dopaminergic properties

Novel inhibitor of prion replication

Novel potent TRPM8 antagonist (IC 50 1.25 ± 0.26 μM)

Potent inhibitor of LpxC

BB-83698 is a peptide deformylase inhibitor and potent antimicrobial with excellent activity against streptococci and Moraxella catarrhalis strains.

Novel inhibitor of SARS-CoV-2 main protease (MPro)

Novel potent apoptotic inducer of human leukaemia cells by activation of the extrinsic pathway and the generation of reactive oxygen species

Novel potent inhibitor of IL-2 secretion, demonstrating potent immunomodulatory activity

Novel FBXO7/PINK1 interaction antagonist, abrogating FBXO7 and PINK1 association, leading to increased cellular PINK1 concentrations and activities, and limiting mitochondrial damage

Memory Enhancer and Free Radical Scavenger

Novel butyrylcholinesterase inhibitor (BChEi) for the treatment of canine cognitive dysfunction

Novel inhibitor of the KRS-67LR interaction

Novel potent and selective degrader of Bcl-2

Novel efficient Bcl-2 inhibitor, exhibiting high specificity and stabilizing effect toward G-quadruplexes

Novel pan-Bcl-2 family inhibitor, upregulating the BH3-only protein Noxa, which inhibits Mcl-1, inducing autophagy through (ER) stress and disruption of the interaction of Beclin 1 with Bcl-2

Novel B-Cell Lymphoma 6 (BCL6) PROTAC

Novel Cell-Permeable Probe for the Identification of Protein Sulfenic Acids

Clearing cycloalkyne for click reaction with Azido-Warfarin WN3 or other Azido-containing drugs

Novel highly potent inhibitor of breakpoint cluster region-abelson kinase (Bcr-Abl) including the T315I mutant

Novel Bcr-Abl inhibitor, potently inhibited Bcr-AblWT and Bcr-AblT315I kinases with IC 50 of 0.043 μM and 0.17 μM, respectively

Potent and selective

Novel small molecule PTP1B inhibitor

Sodium channel enhancer

Potent and selective hydroxamate PfAM1 inhibitor

Novel EthR inhibitor, boosting antituberculous activity of ethionamide

Novel activator of ethionamide

Novel EthR inhibitor and ethionamide booster

Novel specific bona fide EthR-inhibitor, boosting ETH 4 times in an intravenously infected TB mice model

Novel CBP/p300 Bromodomains inhibitor, binding BRD4 almost identical to SGC-CBP30

Active metabolite of beclomethasone dipropionate

Fatty Ester for Lipid Research

Novel potent and specific inhibitor of dog gastric lipase (DGL)

Inhibitor of monoamine oxidase; Anti-serotonin agent

Inhibitor of angiotensin-converting enzyme (ACE); Prodrug of benazeprilat

Novel potent PI3K inhibitor, suppressing metastasis of non-small cell lung cancer cells by modulating β-catenin/ZEB1 regulatory loop, blocking AKT phosphorylation

Novel inhibitor of HIV-1 Rev function, also acting as a cytostatic agent with substantial antiretroviral activity

Irreversible and nonselective Monoamine_oxidase_inhibitor>monoamine oxidase inhibitor (MAOI)

Antiandrogen, being effective in the treatment of acne, seborrhea, and hirsutism in women

Potent D2/D4 dopamine receptor antagonist, neuroleptic and antipsychotic

anti-HSV agent

Inhibitor of 4-hydroxyphenylpyruvate dioxygenase (HPPD), acting as a herbicide

Anorectic, primarily promoting weight loss through reduced appetite

Useful pharmaceutical building block

Long-acting calcium-blocking agent with significant anti-anginal activity

Novel antibacterial agent against multidrug-resistant Escherichia coli at low concentrations as 0.007 mM, disintegrating membrane, accelerating ROS accumulation, reducing bacterial metabolism, and intercalating into DNA groove

Novel antibacterial agent against multidrug-resistant Escherichia coli at low concentrations as 0.007 mM, disintegrating membrane, accelerating ROS accumulation, reducing bacterial metabolism, and intercalating into DNA groove

Novel inhibitor of plasma kallikrein

Novel selective inhibitor of plasma kallikrein, blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE

Novel negative allosteric modulator of the ß2-adrenergic receptor (ß2AR), inhibiting cAMP production through the ß2AR, but not that mediated by other Gs-coupled receptors, also inhibiting ß-arrestin recruitment to the activated ß2AR

Potent ligand of the serotonin (5-HT) and dopamine (DA) transporters used in diagonisis of Parkinson's disease as SPECT imaging precursor

Phytoestrogen, possessing typical curare-like action

Natural antibiofilm agent and adjuvant on the antifungal therapy related to resistant infections caused by C. glabrata

Selective beta-1 adrenergic receptor antagonist with antihypertensive and anti-glaucoma activities and devoid of intrinsic sympathomimetic activity

Novel Dual BET-BRD7/9 Bromodomain Inhibitor, showing a strong antiproliferative effect on various cancer cell lines that could not be observed for BD family selective inhibitors

Novel BET inhibitor, selectively targeting BRD4-BD1 bromodomain

Novel HIF Prolyl Hydrolase Inhibitor, preventing colonic inflammation and fibrosis in murine models of inflammatory bowel disease

Novel probe for neurofibrillary tangles (tau fibrils)

Novel potent and selective inhibitor of kynurenine aminotransferase II

Novel, systemically active kynurenine aminotransferase 2 (KAT2) inhibitor, significantly decreased escape latency in the Morris water maze, indicating improved performance in spatial and contextual memorynovel

Potent inhibitor of centrosomal clustering in malignant cells

Novel Aldose_reductase_inhibitor>aldose reductase (ALR2) inhibitor

Novel dual inhibitor of norepinephrine transporter (NET) function and thyrointegrin αvβ3 receptor

The first small-molecule substrate identified with high selectivity for BGT1 over the three other GAT subtypes; M1 muscarinic agonist

Cell-permeable apoptosis inducer, specifically preventing BH3 domain-mediated interactions between pro-apoptotic and anti-apoptotic members of the Bcl-2 family

Reactive dark quencher used in a variety of Fluorescence Resonance Energy Transfer (FRET) DNA detection probe.

Novel photoactivatable form of serotonin

Novel PROTAC (proteolysis-targeting chimera) as a PTK2 protein degerader

Novel fluorophore substrate of the protease Cathepsin C (CatC), being highly selective versus the related proteases CatB, CatF, CatH, CatK, CatL and CatS

Novel potent inhibitor of human chymase with >100 fold selectivity against Cathepsin G

Novel highly selective, soluble and cellular permeable inhibitor of the P. falciparum protease dipeptidyl aminopeptidase 1 (DPAP1)

Novel inhibitor of HIV replication, preventing the formation of the capsid core structure that encapsulates the viral genome and its associated enzymes, reversing transcriptase and integrase

Novel potent and selective inhibitor of Alk5 (TGFßR1), blocking the phosphorylation of Smad2 and Smad3 in HaCaT cells

Novel potent and selective ATP-competitive inhibitor of glycogen synthase kinase (GSK-3), targeting both isoforms GSK-3α and GSK-3β

Novel highly potent dual inhibitor of BRD9/BRD7

Novel RORγ antagonist for the treatment of autoimmune diseases

Non-ATP competitive inhibitor of JNK, targeting the JNK-JIP interaction

Novel potent, highly selective, and orally bioavailable CATHEPSIN C (CTSC, CatC) inhibitor

Novel nonpeptide angiotensin II receptor antagonist

Novel, highly selective and potent irreversible BTK inhibitor

Potent, selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase

Triple reuptake inhibitor (TRI)

Antilipidemic agent

GABAA receptor antagonist

Novel inhibitor of the TGF-β pathway, blocking the epithelial to mesenchymal transition

Partial agonist at dopamine D2 and serotonin 1A receptors

Novel selective heat shock protein 90 inhibitor, prodrug of CF2772

Selective Syk inhibitor

Novel, Selective, Potent, Reversible Bruton's Tyrosine Kinase (BTK) Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases

Novel potent blocker of the NMDA receptor ion channel

Novel potent blocker of Nav1.2 sodium channels, protecting of brain tissue from ischemia

Natural Biliary Toxin, causing extrahepatic biliary atresia

Potent HNF4α antagonist

Novel USP28 inhibitor

Novel selective RORgamma inhibitor, selectively inhibiting Th17 differentiation and RORgamma signature gene expression

Novel heparanase inhibitor

Potent inhibitor of SHIP-2 catalytic activity; Novel inositol polyphosphate surrogate modulating Ca responses in rat hepatocytes

Potent peptide opioid receptor agonist, alleviating LPS-Induced activation in rat primary microglial cultures in opioid receptor-dependent and receptor-independent manners

Novel adjuvant to repurpose azithromycin for use against Pseudomonas aeruginosa, exhibiting a 1024-fold reduction in the minimum inhibitory concentration of azithromycin in vitro and displays activity in a Galleria mellonella model of infection

Novel anti-HIV active dimeric prodrug of 2‘,3‘-dideoxy-2‘,3‘-didehydrothymidine monophosphate (d4TMP)

Class I antiarrhythmic agent with chronotropic, inotropic, dromotropic and coronary vasodilator effects, potently blocking sodium channel

Novel anti-HIV active dimeric prodrug of 2‘,3‘-dideoxy-2‘,3‘-didehydrothymidine monophosphate (d4TMP)

Selective hAMCase Inhibitor

Novel inhibitor of angiogenesis by regulating STAT3 and VEGF in breast cancer cells

Novel and selective Wnt signaling inhibitor

Novel inhibitor of LPS-induced inflammation in macrophages, improving survival in sepsis

UV stabilizer

Potent activator of the Neh2-luc reporter

Novel Orally Efficacious Pan-HDAC Inhibitor

Inactivator of GSTP1>GST P1-1 through the covalent modification of two Cys47 residues per dimer and one Cys101

Novel potent antagonist of RORγt function, displaying an increased selectivity for RORγt over RORα and PPARγ compared to the purely orthosteric and allosteric non-PEG-linked parent compounds

Potent and selective dual inhibitor of MEK5 and ERK5

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

Novel potent and selective covalent Pin1 inhibitor

Novel Bumped-Kinase Inhibitor (BKI) for Cryptosporidiosis Therapy

Novel Bumped-Kinase Inhibitor (BKI) for Cryptosporidiosis Therapy

Novel potent and selective bumped kinase inhibitor (BKI) CpCDPK1 IC 50 0.0025 µM

Novel potent and selective bumped kinase inhibitor (BKI) CpCDPK1 IC 50 0.005 µM

Novel inhibitor of survivin transcription through a signal transducer and activator of transcription 3 (Stat3)-dependent mechanism, inhibiting tissue expression of survivin and inducing apoptosis in C4-2 skeletal tumor

Novel effective inhibitor of survivin expression at both the mRNA and protein levels in vitro, significantly reducing survivin in bone metastatic C4-2 tumors

Novel inhibitor of the expression of anti-apoptotic protein survivin and membrane-bound efflux pump ATP binding cassette B 1 (ABCB1, p-glycoprotein), presumably via signal transducer and activator of transcription 3 (Stat3), inhibiting human prostate canc

Bradykinin antagonist, causing impressive growth inhibition of lung and prostate tumors, displaying superior in vivo inhibitory effects than convential chemotherapeutic drugs

Natural anti-coronavirus agent

Natural Potent 14-3-3 inhibitor

Potent 14-3-3 inhibitor

Novel ERK inhibitor, inducing breast cancer cell apoptosis via mitochondrial pathway but independent on Ras/Raf/MEK pathway

Inhibitor of calpain, cathepsin L and cathepsin B

Inhibitor of Marburg virus (MARV) growth at noncytotoxic concentrations

Original TXA2 modulator, inhibiting the action of thromboxane A2 and 8-iso-prostaglandin F2alpha

Dual thromboxane synthase inhibitor and thromboxane receptor antagonist

Novel potent EGFR inhibitor

Novel LRP5/6-sclerostin interaction inhibitor, recovering the downregulated activity of the Wnt/β-catenin signaling pathway by competitive binding to the LRP5/6-sclerostin complex

Novel inhibitor of RNA polymerase I, causing nucleolar stress and showing potent anticancer activity across many tumor types

Novel potent cyclin-dependent kinases (CDK) inhibitor, inducing a strong cell cycle alteration

Potent and selective inhibitor of Cdk5/p25, protecting large population of cells against non-A

Metabolite of BML277 which is a selective checkpoint kinase 2 inhibitor

Novel activator of BMP signaling, enhancing osteoblast differentiation, targeting HECT domain of ubiquitin ligase Smurf1, up-regulating the protein level of Smad1/5

Novel activator of BMP signaling, enhancing osteoblast differentiation, targeting HECT domain of ubiquitin ligase Smurf1, up-regulating the protein level of Smad1/5

Novel Highly Selective LRRK2 Inhibitor

Novel PD-L1 Inhibitor

Novel PD-1/PD-L1 Inhibitor

Novel potent, selective inhibitor of AAK1 (adaptor associated kinase 1), having the appropriate combination of solubility and charge required for microiontophoresis

5HT1B/1D agonist

Novel K channel opener; Glyburide-Reversible Cardioprotective Agent with Minimal Vasodilator Activity