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

Local anaesthetic agent, blocking voltage-gated Na(+) currents in neurons

Impurity of Lenalidomide

Natural antibiotic, acting as an inhibitor of DOXP reductoisomerase

Novel dipeptidyl peptidase IV (DPP4) inhibitor

Novel Dipeptidyl Peptidase-4 (DPP-4) Inhibitor

Novel Photochromic Ion Channel Blocker

Novel NO-donating antimicrobial peptide, exhibiting Staphylococcus aureus and Escherichia coli biofilm dispersion and eradication, and potent antibacterial activities in vitro

Novel agonist of the formyl peptide receptor (FPR), protecting against myocardial ischaemia-reperfusion injury in mice

Selective ET(A) receptor antagonist

Natural specific inhibitor of mammalian NSDHL and yeast Erg26p, inhibiting an artificial Hepatitis C viral replicon, and showung broad antifungal activity

Nonprostanoid PGI2 agonist

Potent and nonadrenotoxic ACAT inhibitor

Novel Nonpeptide Bradykinin B2-Receptor Partial Agonist

Potent, selective, and orally active antagonist for central adenosine A1 receptors

Novel Potent and Selective Covalent Inhibitor of KRAS G12C

Potent ligand for a protein site governed largely by van der Waals interactions, producing excitatory activity in tadpoles and mice; also antagonizing propofol-induced hypnosis

Novel N-Methyl-d-aspartate receptor (NMDAR) positive allosteric modulator (PAM) with potential antidepressant effects

Novel highly potent and selective inhibitor (type 1.5 binding mode) of MAPK14 [IC50 = 0.2 nM (ELISA, cell free); KD = 1.5 nM (DiscoverX)]

Novel Anabolic Selective Androgen Receptor Modulator (SARM)

Novel inhibitor of protein farnesyltransferase (FT), inhibiting the growth of P. falciparum in red blood cells and suppressing parasitemia

Farnesyltransferase inhibitor, inhibiting both H- and K-Ras oncogenic signaling

Novel fat mass- and obesity-associated protein (FTO) inhibitor, preventing neurosphere formation in patient-derived glioblastoma stem cells (GSCs) without inhibiting the growth of healthy neural stem cell-derived neurospheres

Novel specific high-affinity fluorescent probe for FtsZ antibacterial inhibitor

FTY720 analog as novel potent stimulator of the activity of the protein phosphatase 2A (PP2A)

FTY720 analog as novel stimulator of the activity of the protein phosphatase 2A (PP2A), targeting mitochondria

Direct inhibitor of the p53 transactivation domain from binding to replication protein A

Natural antimicrobial agent, showing neuroprotective, expectorant, and antioxidant activities

Chemosensitizing agent, selectively reversing BCRP-mediated multidrug resistance to mitoxantrone, doxorubicin, and topotecan

Highly potent dopamine D2 modulator

Anti-bacterial metabolite of Nitrofuran

Novel potent Hepatitis C virus (HCV) NS3/4A protease inhibitor

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