Novel NOP receptor-mu opioid receptor ligand

Novel potent and selective partial agonist of human and rat α3β4 nicotinic cholinergic receptors

High affinity, selective alpha3beta4 nAChR ligand

Novel dual μ-opioid and nociceptin receptor partial agonist (K i = 16.49 and 3.67 nM, respectively)

Nucleosidic antibiotic

Novel selective nociceptin receptor (NOP) agonist

Novel inhibitor of cyclin-dependent kinases 1, 2, 4, 5, and 9 with in vitro activity against lymphoid malignancies

Novel degrader of MTH1 fusion proteins for use within the aTAG system

aTAG 4531 (CFT-4531) is a potent, selective, and onmechanism tool degrader of MTH1 with DC50 value of 0.28 nM and Ki value of 1.8 nM. degradation activity is due to the intricate formation of the ternary complex between the MTH1 aTAG, CRBN E3 ligase, and aTAG tool degrader .

Hydrogen sulfide-releasing cyclooxygenase inhibitor

Potent cytotoxic agent for both prostate cancer and melanoma

Novel ROS generator, permeating mycobacteria to reliably enhance endogenous ROS including superoxide radical

Selective ß1 receptor antagonist

Potent JAK2 inhibitor

Novel selective A2BR antagonist

Novel inhibitor of the cancer-associated tropomyosin 3.1 (Tpm3.1), suppressing glucose-stimulated insulin secretion (GSIS) from the pancreatic islets

Novel non-toxic contrast agent for micro-CT imaging

Novel potent inhibitor of nucleotide pyrophosphatase/phosphodiesterase-1 (NPP1)

Novel antitimor agent, exhibiting superior anti-proliferative activity, excellent chemo-sensitizing activity against pancreatic cancer in vitro and in combination with Gemcitabine

Natural potent apoptosis inducer in U937 cells, inducing caspase-3 processing, PARP, and DNA fragmentation

Novel Potent Dual Inhibitor of MDM2 and MDMX (Ki =1 nM)

Novel potent and selective dual inhibitor of MDM2 (Ki = 0.9 nM) and MDMX (Ki = 7 nM)

Novel potent, highly selective, orally bioavailable CDK9/P-TEFb inhibitor

Novel Potent Autotaxin (ATX) Ligand

Novel selective Autotaxin (ATX) inhibitor

Novel inhibitor of JAK/STAT signaling, inhibiting both constitutive and interleukin-6-induced STAT3 phosphorylation, selectively affecting cell viability only of cancer cells harboring aberrant JAK/STAT signaling

Potent inhibitor of HCV RdR

Novel AURKA inhibitor, reducing clonogenicity, arresting the cell cycle at the G2/M phase, and inducing caspase-mediated apoptotic cell death in HCT116 human colon cancer cells

Natural antibiotic

Novel inhibitor of AChE, suppressing Aβ aggregation, protecting Caenorhabditis elegans against Aβ- and 6-OHDA-induced neurotoxicities dose-dependently

Potent inhibitor of HCV RdR

Novel small 4 integrin antagonist, preventing the development of experimental colitis in mice.

Novel potent ATP-competitive inhibitor of Aurora A/B/C (5.6/18.4/24.6 nM)

Novel DNA damage inducer during G0/G1, S, and G2 cell cycle phases via a mechanism unique from other DNA damaging agents

Novel autophagy inhibitor, targeting mitochondrial complex I directly, leading to the potent inhibition of mitochondrial respiration as well as autophagy

Unique signaling molecule used in quorum sensing

Novel inhibitor of autophagy, promoting metabolic stress within the tumour microenvironment and potentiating the effect of cytostatics in combination therapy

Novel anticancer agent, exhibiting potential cytotoxicity and inhibiting autophagy in hepatocellular carcinoma (HCC) cells

Monoselective agonist of the S1P(1) receptor

Novel USP30 inhibitor

Novel USP28 inhibitor

Novel, highly potent p53-MDM2 inhibitor with an IC50 value of 0.08 nmol/L, displaying excellent oral efficacy in the human SJSA1-based xenograft model.

First-in-class allosteric inhibitor of respiratory syncytial virus (RSV), blocking RNA elongation by the respiratory syncytial virus polymerase complex

Novel USP28 inhibitor

Novel selective USP7 inhibitor (USP7 IC50 9 μM; USP8 >50μM)

Novel USP28 inhibitor

The fifth-generation fluoroquinolone with in vitro coverage of community-acquired bacterial pneumonia (CABP) pathogens, atypical respiratory pathogens, multidrug-resistant Streptococcus pneumoniae and methicillin-resistant Staphylococcus aureus

Novel non-peptide Ang-(1-7) mimetic, inhibiting perivascular inflammation, through the reduction of chemokine expression in pVAT, as well as through direct actions on monocytes/macrophages inhibiting their activation

Novel angiotensin-(1-7) Mas receptor agonist

Novel antistaphyloccocal agent, attenuating inhibition of hERG potassium channel current

Cancer chemoprevebtive agent

Natural potent antienterovirus D68 (anti-EV-D68) agent

Novel cytosolic phospholipase A2 group IVA (cPLA2α) inhibitor, displaying potent anti-inflammatory activity and disease-modifying properties in cellular and in vivo models

Potent broad spectrum antibacterial agent, particularly against drug-resistant Staphylococcus pathogens

Novel potent and selective αvβ3 integrin inhibitor

The first potent and selective αvβ5 integrin inhibitor

Novel PDE4 inhibitor

Novel specific inhibitor of HIV-1 entry through interaction with the Env spike by virtue of the incorporation of a guandinium group

Novel potent dual inhibitor of Ax1 and Mer

Zn -dependent inhibitor of human plasma Lp-PLA2

Highly specific JNK inhibitor #212121; font-style: normal; font-variant-ligatures: normal; font-variant-caps: normal; font-weight: 400; letter-spacing: normal; text-align: start; text-indent: 0px; text-transform: none; white-space: normal; word-spacing: 0

Novel dual ERK5 and BRD4 inhibitor

Novel potent and selective ERK5 inhibitor

Novel potent dual ERK5 and BRD4 inhibitor

Novel highly potent and orally bioavailable Axl inhibitor

Novel integrin-binding peptide, inhibiting hepatocyte growth factor (HGF) signaling through Met-integrin interactions, also being an antiangiogenic agent by reducing phosphorylation of VEGR2, IGFR, and PDGFR, stabilizing vessels by disrupting α5β1 signali

Cyclooxygenase Inhibitor;

Second Generation

Novel transient receptor potential cation channel subfamily V member 1 (TRPV1) antagonist

Novel transient receptor potential cation channel subfamily V member 1 (TRPV1) antagonist

Novel orally bioavailable inhibitor of Hedgehog signaling

Novel transient receptor potential cation channel subfamily V member 1 (TRPV1) antagonist

Novel potent EphB4 inhibitor

Novel tankyrase inhibitor, enhancing irinotecan activity in tumors that exhibit elevated tankyrase and irinotecan resistance

Novel covalent ERK1/2 inhibitor

Novel weak PAR2 antagonist

Novel selective Cdc42 inhibitor, suppressing primary colon cancer growth and prolonging survival in a preclinical mouse xenograft model by downregulation of PAK1 activity

Near-IR probe for detecting conformational changes of Aβ1-42 soluble oligomers in vitro

Inducer of Death Receptors and Sensitizer of Human Cancer Cells to TRAIL through a p53-Independent Mechanism

Inhibitor of hepatic cholesterol biosynthesis, inhibiting the cytochrome P450 enzyme lanosterol 14alpha-demethylase

Novel selective GABA-C antagonist

Novel CXCR2 antagonist with 200 times improvement in solubility than AZD8309

Selective alpha7 nicotinic receptor activator

Novel transient receptor potential vanilloid 1 (TRPV1) antagonist

AZD1897 is a PIM1, PIM2, and PIM3 inhibitor with IC50 values of less than 3 nM for these three PIM kinases. AZD1897 exhibits anticancer activity and synergistically inhibits the activity of acute myeloid leukemia (AML) cells in combination with Capivasertib (HY-15431). This synergistic inhibitory effect is achieved through the inhibition of the mTOR and MCL1 pathways.

Novel peroxisome proliferator-activated receptor alpha (PPARalpha) agonist, inducing alanine aminotransferase-1 gene and protein expression in human, but not in rat hepatocytes

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)