Insecticide, acting as an EC 3.1.1.7 (acetylcholinesterase) inhibitor

Natural neuroprotective agent on glutamate-mediated HT22 cell death, controlling the amount of ubiquinone, up-regulating p21 expression in a p53-dependent manner, decreasing Akt phosphorylation and resulting in increased Fas ligand production and caspase-

Novel slow-releasing hydrogen sulfide (H2S) donor, inhibiting NF-κB activity and inducing cell apoptosis

Novel highly potent Factor XIa inhibitor with selectivity against most of the relevant serine proteases

Novel potent and selective inhibitor of FXIa, producing a robust and dose-dependent inhibition of both arterial thrombosis and MES

Novel, Potent, and Nonsteroidal Farnesoid X Receptor (FXR) Selective Antagonist

Novel antiviral agent against Rift Valley fever virus (RVFV) by blocking virus budding from the trans Golgi.

Novel potent and highly specific MEK inhibitor (MEKi)

Novel fluorescent specific ligand of human telomeric G-quadruplex DNA, binding to both G-tetrad and the lateral loop near the 5-end, reducing the telomere length and downregulating hTERC and hTERT mRNA expression in HeLa cells

Inhibitor of NLRP3 inflammasome

Novel antibacterial and anti-biofilm agent against antibiotic resistant clinical isolates

Novel G6PD inhibitor, revealing immune dependence on pentose phosphate pathway. depleting NADPH most strongly in lymphocytes, markedly decreasing inflammatory cytokine production in T calls, suppressing respiratory burst in neutrophils

Novel potent competitive γ-aminobutyric acid type A receptor (GABA A R) antagonist (K i = 180 nM), targeting extrasynaptic α4βδ subtype, showing efficiently rescue inhibition of T cell proliferation

Potent and selective

GAC0003A4 is an LXR inverse agonist that inhibits LXR transcriptional activity. GAC0003A4 also efficiently degrades LXRβ protein. GAC0003A4 has the potential to be used in advanced pancreatic cancer and other refractory malignancies.

Novel LXR inverse agonist, functioning as LXR a degrader, significantly reducing LXR protein levels in PDAC cell lines

Liver-specific magnetic resonance imaging (MRI) contrast agent

Novel viral RNA-dependent RNA polymerase (RdRP) inhibitor

Novel inhibitor of galactokinase (GALK)

First-in-class transforming growth factor-β receptor type I inhibitor

Novel male contraceptive agent, blocking spermatogenesis

Novel acid-tolerant green RSFP, exhibiting negative switching with especially high contrast in acidic conditions, and its off switching is caused by trans-to-cis isomerization of the chromophore hydroxyphenyl ring that accompanies protonation

Natural antibiotic, displaying potent and selective bactericidal activity against key Gram-positive pathogens (including Staphylococcus aureus and enterococci)

Mammalian metabolite, identified in plasma and cerebrospinal fluid from hyperammonaemic patients

Novel acetylcholinesterase inhibitor

Novel GAS41 YEATS inhibitor, blocking proliferation of NSCLC cells, and modulating expression of GAS41-dependent genes, demonstrating on-target inhibition of GAS41 in cancer cells

Novel allosteric activator and positive modulator of α7 nicotinic acetylcholine receptors (nAChR), more active (+)-enantiomer of 4BP-TQS

Novel potent CB1R ago-PAM

Novel CB1R allosteric agonist biased toward G protein- vs β-arrestin1/2-dependent signaling

Novel CB1R allosteric agonist-positive modulator (ago-PAM), exhibiting augmented allosteric-agonist and PAM activities in neuronal cultures, improved metabolic stability, and enhanced orthosteric agonist binding (CP55940)

Novel CB1R allosteric agonist-positive allosteric modulator (ago-PAM), exhibiting moderate ago-PAM potency and improved aqueous solubility with therapeutic reduction of intraocular pressure in murine glaucoma models

Novel CB1R allosteric agonist-positive modulator (ago-PAM), exhibiting augmented allosteric-agonist and PAM activities in neuronal cultures, improved metabolic stability, and enhanced orthosteric agonist binding (CP55940)

Antagonist of central cholecystokinin receptors

Novel non-toxic and mammalian-specific LINE-1 inhibitor

Selective inhibitor of carbonic anhydrase IX (CAIX)

Selective inhibitor of carbonic anhydrase IX (CAIX)

Highly potent non-nucleoside inhibitor of HIV-1 reverse transcriptase

Novel Potent and Selective Sodium Glucose Co-Transporter 2 (SGLT2) Inhibitor for the Treatment of Type 2 Diabetes

Novel glucosylceramide synthase (GCS) inhibitor, rescuing lysosomal deficits, α-synuclein pathology and neuron toxicity

Novel highly-selective oral checkpoint kinase 1 (Chk1) inhibitor

Novel potent, selective and orally bioavailable Chk1 inhibitor

Novel Bruton's tyrosine kinase (BTK) inhibitor

Novel SMAC mimetic and IAP antagonist

Inhibitor of the Wnt/beta-catenin signaling pathway, suppressing cell proliferation and enhancing radiosensitivity in A549/Wnt2 cells.

Novel Phosphodiesterase 4D (PDE4D) Inhibitor

MAO inhibitor

Novel antifungal agent

Metabolite of ganstigmine, a novel acetylcholinesterase inhibitor

Natural covalent Cys151-dependent NRF2 activator

Natural non-covalent NRF2 activator, activating NRF2 in A KEAP1-dependent but Cys151-independent manner, conferring greater protection than a Cys151-dependent analog, geopyxin C

GFB-12811 is a high selective and orally active CDK5 inhibitor with an IC50 of 2.3 nM. GFB-12811 is highly selective over the other tested kinases (CDK1/2/6/7/9).

Endogenous dipeptide, activating N-methyl-D-aspartate receptors

Novel nonpeptidic inverse agonist of the Ghrelin Receptor (GHSR)

Metalloproteinase inhibitor, specifically blocking TNF-alpha secretion both in vitro and in vivo

Potent EGFR/erbB2 dual inhibitor

Novel oral anti-nociceptive agent, showing peripheral opioid agonistic activity and hydrogen sulphide-releasing capacity

Potent mitochondrial benzodiazepine receptors (MBRs) ligand; Prodrug for its active metabolite bromo-nordazepam

Novel suppressor of endoplasmic reticulum (ER) stress and oxidative stress, preventing protein aggregate accumulation in vitro and in cultured hippocampal HT22 neuronal cells, as well as glutamate-induced oxytosis and erastin-induced ferroptosis

Novel suppressor of endoplasmic reticulum (ER) stress and oxidative stress, preventing protein aggregate accumulation in vitro and in cultured hippocampal HT22 neuronal cells, as well as glutamate-induced oxytosis and erastin-induced ferroptosis

Gilteritinib (ASP2215) hemifumarate is a potent and ATP-competitive FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively.

Natural suppressor of mesenchymal stem cell (MSC) differentiation

Natural Activator of the Nrf2-Regulated Antioxidant Defense System in SH-SY5Y Cells, Binding to the Subpockets of Keap1 Kelch Domain

First-in-Class, Potent, and Orally Bioavailable NADPH Oxidase Isoform 4 (Nox4) Inhibitor

Novel water solubile prodrug of ICRF-193, penetrating into NVCMs, reaching intracellular concentrations sufficient to induce cytoprotective effects against ANT toxicity

Novel Allosteric Activator of Human Glucokinase in the Absence of Glucose

Novel and potent glucokinase activator (GKA)

First-in-class liver-selective glucokinase activator for the treatment of type 2 diabetes

Novel inhibitor of the cell cycle progression in M-phase; Inhibotor of endosome maturation

Novel 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor

Novel Galactofuranosyltransferase 2 (GlfT2) inhibitor

Second-generation sulfonylurea, promoting the accumulation of fructose 2,6-bisphosphate in hepatocytes

Novel inhibitor of the acetyltransferase activity of Escherichia coli N-acetylglucosamine-1-phosphate-uridyltransferase/glucosamine-1-phosphate-acetyltransferase (GlmU).

Novel potent Glyoxalase 1 (GLO1) inhibitor, demonstrating to penetrate the blood-brain barrier, elevating levels of methylglyoxal in the brain, and reducing depression-like behavior in mice

Novel inhibitor of glyoxalase 1 (Glo1), increasing the cellular methylglyoxal levels in human cells and suppressing the osteoclast formation of mouse bone marrow-derived macrophages

Enteroendocrine hormone, stimulating the growth of intestinal epithelium

Ago-allosteric modulator of human GLP-2R

The first-in-class, ATP-competitive inhibitor of MAPKAPK5

Novel inhibitor of glutaminase 1 (GLS1) with high binding affinity (SPR, Kd = 24 nM; ITC, Kd = 37 nM), exhibiting a similar in vivo antitumor activity as CB839

Novel potent glucose transporter type 4 (GLUT4) translocation activator, showing a significant blood glucose lowering effect in the severe diabetic mice model

Selective inhibitor of human glucose transporter subtype 1/4 (hGLUT1/4)

Selective inhibitor of human glucose transporter subtype 1/4 (hGLUT1/4)

Glucose transporter inhibitor linker for insulin conjugate

Novel glucose transporter (GLUT) inhibitor, exhibited high antitumor potency through the suppression of glucose uptake (IC 50 : 2.5 μM), while not cytotoxic to prostate and mammary epithelial cells

Metabolite of soy isoflavones, promoting the proliferation of bone marrow stromal cells and osteoblasts and suppresses bone turnover

Novel GM3 derivative, showing excellent migration and invasion inhibitory effects in cells and marked antitumor activity in C57BL/6 mice, involving focal adhesion and ECM-receptor interaction signaling pathways

Selective modulator of gamma-aminobutyric acid(A) receptors

Novel potent BCR-Abl PROTAC, inducing degradation and demonstrating in vivo activity

Negative control for GMB-805

Novel Tubulin Polymerization Inhibitor

Novel GluN2A subunit-selective and brain-penetrant positive allosteric modulator (PAM) of The N-methyl-d-aspartate receptor (NMDAR)

Novel potent and selective RORc inverse agonist

Novel Met inhibitor

Novel GluN2A-selective NMDA receptor positive allosteric modulator (PAM)

Novel NMDAR PAM with both an improved pharmacokinetic profile and increased selectivity against AMPARs

Novel inhibitor of nicotinamide phosphoribosyl transferase (NAMPT)

Negative control for GNE-2256

Novel GluN2A-selective NMDA receptor positive allosteric modulator (PAM)

Novel selective CHK1 inhibitor

Novel potent aryl hydrocarbon receptor (AHR) antagonist with the capacity to inhibit both DRE-dependent and -independent activity

Novel Inhibitor of EGF-EGFR Interactions

Novel inhibitor of Plasmodium falciparum, killing both blood- and sexual-stage P. falciparum parasites

Dose dependent up-regulator of the level of E-cadherin in SW620 cells

Natural highly potent HIV latency-reversing agent

Novel inhibitor of Gram-negative lipoprotein trafficking

Novel potent GNMT inducer, inhibiting Huh7 cell growth in vitro and xenograft in vivo

Dual Glycolate Oxidase/Lactate Dehydrogenase A (GO/LDHA) Inhibitor for Primary Hyperoxaluria

Agonist of the GnRH receptor, inducing the secretion of the gonadotropins follicle-stimulating hormone and luteinizing hormone from the pituitary gland and to increase sex hormone production by the gonads

Natural inhibitor of Musashi family of RNA-binding proteins

Antipsychotic and cognitive enhancer; Dopamine D1 and D2 receptor modulator

Natural potent inducer of apoptosis in MCF-7 cell lines

Curcumin analog, exhibiting potent growth suppressive activity in human colorectal carcinoma cells

Novel selective non-steroidal agonist of G-protein bile acid receptor 1 (GPBAR1, also known as TGR5 or M-BAR)

Potent PARP inhibitor

Novel potent GPR120 agonist, exhibiting significant glucose-lowering effect and high selectivity over GPR40

Novel potent GPR52 agonist, dose-dependently suppressing methamphetamine-induced hyperlocomotion in mice

The first orally active GPR52 agonist

Highly potent and specific GPR52 antagonist

Novel, potent, efficacious, and brain-penetrant GPR88 agonist (cAMP EC 50 = 14 nM)

Novel potent GPR88 agonist (EC 50 = 59 nM)

Novel HIV replication blocker (EC 50 = 1.66 μM), being actively against a panel of HIV mutant strains displaying resistance to individual drugs used in antiretroviral therapy

Novel potent and selective ferroptosis inducer, inhibiting glutathione peroxidase 4 (GPX4)

Novel high affinity, potent, and selective stabilizer of the MYC G-quadruplex (G4)., inducing cytotoxicity with corresponding decreased MYC mRNA and altering protein binding to the NHE III1 region

Novel dual G-quadruplex/i-motif binder, binding to and stabilizing both G-quadruplex and i-motif, being effective in both oncogene replication and transcription

Potent TrkA kinase inhibitor

Negative control for GI181771X

Selective and brain penetrant NK1-receptor antagonist

Novel inhibitor of the EGFr and C-erbB-2.

5-HT1B/5-HT1D serotonin receptor antagonist

5-HT3 receptor antagonist

Bacterial siderophore with a diazeniumdiolate ligand system

Potent 5HT3 antagonist

Novel Nrf2 modulator via a thus far uncharacterized mechanism

Natural blocker of the voltage-gated sodium channels located in the cell membrane of neurons

Novel orally available, potent and selective inhibitor of Transient Receptor Potential Ankyrin 1 (TRPA1) with IC50 value less than 10 nM

Novel oral specific TRPV1 antagonist, decreasing bladder overactivity and noxious bladder input in cystitis animal models

Natural Potent Inhibitor for Glioblastoma Stem Cell via Targeting RHOA and PI3K/AKT

Novel potent G-protein-coupled receptor kinase 5 (GRK5) inhibitor

Novel, potent, and selective G protein-coupled receptor kinase 6 (GRK6) inhibitor with an IC50 value of 6 nM against GRK6 and selectivity against a panel of 85 kinases

Novel CCR5 inhibitor, inhibiting the replication of wild-type R5-HIV-1

Novel β-Secretase BACE1 Inhibitor, reversing memory impairments and rescuing age-related cognitive decline

Novel allosteric inhibitor of respiratory syncytial virus (RSV)

Novel potent inhibitor of feline infectious peritonitis (FIP) virus in tissue culture and experimental cat infection studies

Novel Inhibitor of Hepatitis C Viral Infectivity

Novel oral prodrug of GS-441524, inhibiting SARS-CoV-2, including variants of concern (VOC) in cell culture and human airway epithelium organoids

Potent and selective inhibitor of HIV-1 protease, effectively inhibiting protease mutants with amino acid insertions, also inhibiting major aspartyl peptidase 1 (May1), a secreted Cryptococcus neoformans protease

Novel high potent and selective stabilizer of the MYC G-quadruplex (G4)

Glutamate receptor antagonist and radical scavenging agent

Novel allosteric HIV-1 integrase (IN) inhibitor, disrupting formation of mature HIV particles

Novel potent EchA6 inhibitor

Potent inhibitor of AKT kinase

Novel dual H1 and H3 receptor antagonist with a long duration of action

Potent inhibitor of AKT kinase, showing activity against auxotrophic M. tuberculosis and being potentiated with meropenem

Novel inhibitor of polo-like kinase

Novel inhibitor of polo-like kinase

Potent and selective GPR119 agonist

Novel selective inhibitor of MmpL3 mutation

Novel allosteric inhibitor of human immunodeficiency virus (HIV) integrase, blocking viral replication and abnormal multimerization involving specific protein domains

Non-peptidic snail toxin; Activator of the Kv1.1 potassium ion channel

Novel specific P2X(7) receptor antagonist

Novel dual inhibitor of BPTF and Brd4

Potent non-cytotoxic inhinitor of Mycobacterium tuberculosis H37Rv

Potent non-cytotoxic inhinitor of Mycobacterium tuberculosis H37Rv

Novel noncompetitive inhibitor of rTbIPMK

Novel Inhibitor of the Mycobacterium tuberculosis Demethylmenaquinone Methyltransferase MenG

Potent non-cytotoxic inhinitor of Mycobacterium tuberculosis H37Rv

Potent and selective H3 histamine receptor inverse agonist

Novel inhibitor of EPHX2 (epoxide hydrolase 2, alias soluble epoxide hydrolase or sEH), up-regulating cytoprotective genes and down-regulating proinflammatory cytokine production

Novel potent, metabolically stable and centrally penetrant PPARγ partial agonist

Novel competitive inhibitor of rTbIPMK with respect to Ins(1,4,5)P3

Novel selective non-imidazole histamine H 3 receptor antagonist

Novel AKT Inhibitor, Enhancing Anti-Tumor Effects in Combination with the MEK Inhibitor

Novel insulin-like growth factor 1 receptor inhibitor, binding to a novel region of the GRK active site cleft that could likely be exploited to achieve more selectivity

Novel inhibitor of T. brucei IPMK, partially inhibiting rTbIPMK activity

Inhibitor of insulin receptor, also tageting IGF-1R and ALK

Selective inhibitor of iE-DAP-stimulated IL-8 release via the NOD1 signaling pathway

Novel highly potent, reversible soluble epoxide hydrolase (sEH) inhibitor, exhibiting potent cell-based activity, a concentration-dependent inhibition of the conversion of 14,15-EET to 14,15-DHET, attenuating cigarette smoke-induced inflammation by both i

Novel S1P1 receptor agonist

Novel I-kappa-B kinase-3 (IKK3) inhibitor

Novel selective histamine H3 receptor antagonist

Specific ATPase competitive kinesin-5 inhibitor

Betulin derivative as antitumor agent

Novel selective inhibitor of G protein-coupled receptor kinase 2 (GRK2)

Novel potent and selective, SAM-competitive inhibitor of SMYD3

Novel human immune virus (HIV) maturation inhibitor

Novel inhbitor of protein kinase GRK1/2/5 and PKA

Novel quaternized GSK-3008348 derivative, acting as a highly selective αvβ6 Integrin Inhibitor

Novel potent RORγ inverse agonist

Potent and selective antagonist of P2X7 receptor

Novel selective inhibitor of G protein-coupled receptor kinase 2 (GRK2)

Promiscuous kinase inhibitor, a close analog of CTx-0294885

Novel agonist of toll-like receptor 2 (TLR2), stimulating the release of G-CSF in activated THP-1 cells, peripheral blood mononuclear cells, and human umbilical vein endothelial cells

Novel selective non-imidazole histamine H 3 receptor antagonist

Novel lysine specific histone demethylase 1 (LSD1) inhibitor, exhibiting high selectivity to LSD1 over MAOs

Novel inhibitor of prolyl hydroxylase (PHD) domain-containing enzyme

Novel anti-TB agent against Mycobacterium tuberculosis and Mycobacterium bovis BCG, targeting MmpL3 and inhibiting EchA6

Novel DNMT1-selective inhibitor (IC 50 = 0.11 ± 0.02 µM)

Novel highly potent cell-permeable, reversible, ATP-competitive inhibitor of GSK-3 (IC50 = 0.4 and 0.6 nM for GSK-3α and GSK-3β, respectively)

GSK3-IN-3 is a mitophagy inducer, inducing Parkin-dependent mitophagy. GSK3-IN-3 is also a GSK-3 inhibitor with an IC50 value of 3.01 μM. GSK3-IN-3 is non-ATP nor substrate competitive and is neuroprotective against 6-OHDA.

Potent and irreversible inhibitor of GSK3

First-in-Class GSK-3β/HDAC Dual Inhibitor as a Disease-Modifying Agent To Combat Alzheimer’s Disease