Natural activator of cryptic biosynthetic gene clusters (BGC), also acting as a potent inhibitor of monoamine oxidase B

Potent, highly selective, and orally bioavailable inhibitor of PIM-1 kinases

Novel potent PIM inhibitor

Antipsychotic agent

Inhibitor of PIP 4 Ks, efficiently killing transformed BJ cells, but not normal counterparts, displaying a strong selective lethality against Ras-activated or Ras-transformed cells

Partial agonist of benzodiazepine receptors

Antipsychotic prodrug, most notably used for schizophrenia

Antifungal antibiotic, showing inhibitory activity against fungi and yeasts, especially against Trichophyton

Novel potent in vitro and in vivo antifungal agent against azole-resistant Candida albicans

Natural nitric oxide (NO) production inhibitor

NSAID with better gastrointestinal (GI) tolerability

Inhibitor of the acetylcholinesterase activity from bovine erythrocytes and electric eel

Inhibitor of topoisomerase II, intercalating into DNA and inducing topoisomerase II-mediated DNA strand crosslinks, resulting in inhibition of DNA replication and tumor cell cytotoxicity

Potent ligand to target the Y220C pocket, stabilizing Y220C

Novel Protein Kinase C-iota (PKC-ι) Inhibitor, Binding Post-kinase Domain Residues

Novel selective inhibitor of protein kinase Cθ (PKCθ)

Novel highly potent and selective PKM2 inhibitor, blocking PKM2 mitochondrial translocation under nutritional stress and inhibits tumor growth in vivo

Novel potent and specific β5i inhibitor

Potent inhibitor of HipA toxin, inhibiting E. coli persistence

mRNA splicing inhibitor

Antilipidemic and antiplatelet agent

Novel Potent and Specific Inhibitor of Placental Alkaline Phosphatase (PLAP; IC 50 = 32 nM), Targeting Tumor of the Female Reproductive Tract

Novel Potent Activator of the Nonreceptor Protein Tyrosine Phosphatase Shp2

Gastroprotective agent, increasing the prostaglandin production in the gastric mucosa and accelerates ulcer healing

Broad spectrum aminoglycoside antibiotic typically used for moderate-to-severe urinary tract infections or pyelonephritis

Novel inhibitor of phospholipase C (PLC) isozyme

Novel enhancer of Reactive Oxygen Species (ROS), depleting glutathione levels in analogy to piperlongumine but with reduced cell death

Novel activator of AMPK, inducing apoptotic death in prostate cancer cells

Plk1 PBD-specific phosphopeptide inhibitor, effectively inhibiting mitotic progression and cell proliferation

Novel Inhibitor of the Polo-Box Domain of Polo-like Kinase 1 (Plk1 PBD)

Novel polo-like kinase 1 (PLK1) inhibitor

Slightly less potent inhibitor of FMS than PLX647 but has better aqueous solubility

Potent anticancer tetrahydroisoquinoline alkaloid, being able to form a covalent bond with the amino group of a guanine in selected triplets of DNA duplexes and eventually give rise to double-strand breaks

Novel inhibitor of β-catenin signaling, significantly reduced β-catenin activity in hepatoblastoma and several HCC cells

Novel potent irriversible dual inhibitor of tubulin and epidermal growth factor receptor (EGFR), inducing the apoptosis of A549 cells in a dose- and time-dependent manner, along with decrease in mitochondrial membrane potential (MMP), production of ROS an

Novel inhibitor of prenylated methylated protein methyl esterase (PMPMEase), a key enzyme in the reversible methylation/demethylation step in the protein prenylation pathway

Novel inhibitor of prenylated methylated protein methyl esterase (PMPMEase), a key enzyme in the reversible methylation/demethylation step in the protein prenylation pathway

Selective 5-HT1A serotonin receptor antagonist

Cell-permeable analog of pifithrin-α, potently blocking p53-mediated expression of p21/WAF1 and apoptosis

Novel G Protein-Biased Cannabinoid 1 (CB1) Receptor Agonist

Potent inhibitor of CDK2/cyclin A

Allosteric modulator of 5-HT(2C)R with no intrinsic agonist activity

The first small-molecule approach capable of detecting and controlling engineered cell-cell outputs

Novel microtubule destabilizing natural product from the Podophyllum species

Novel RNA polymerase I inhibitor, targeting ribosomal DNA G-quadruplexes, potently and selectively inhibiting cell growth by high-affinity binding to G4s in ribosomal DNA, impairing RNA polymerase I (Pol I) elongation, inducing a rapid inhibition of Pol I

Novel macrocycle antibiotic with selective and potent activity against P. aeruginosa

Novel modulator of protein-protein interactions of the mitotic polo-like kinases, targeting KRAS mutant xenografts, indicate avenues, acting synergistically with Crizotinib, an inhibitor of the c-MET receptor, against mutant KRAS-expressing cancer cells

Pan-Specific Inhibitor of the Polo-Box Domains of Polo-like Kinases Arrests Cancer Cells in Mitosis

Used for the transfection of a broad variety of cell lines; Antimicrobial; Novel binding agent of diffusive gradients in thin-films (DGT) technique (PEI-DGT)

Novel activator of Adenosine monophosphate (AMP)-activated protein kinase (AMPK)

Antibiotic as a last-line therapy to treat infections caused by these life-threatening 'superbugs'

Novel pan-inhibitor of KCa3.1/KCa2 channels

Potent Activator of Vγ9Vδ2 T-Lymphocytes; HMBPP ananlog prodrug

Hypobetalipoproteinemic and Lipid decreasing agent

Novel pan-human EGF receptor (HER) inhibitor

Novel iNOS homodimerization inhibitor

The first reported PPARα/δ dual antagonist

Novel dual PPARα/γ agonist, ameliorating insulin resistance and gluconeogenesis in vivo and vitro

Novel inhibitor of protein-protein interaction (PPI), blocking #212121; font-family: BlinkMacSystemFont, -apple-system, "Segoe UI", Roboto, Oxygen, Ubuntu, Cantarell, "Fira Sans", "Droid Sans", "Helvetica Neue", sans-serif; font-size: 14px; font-style: no

Novel insulin mimetic

Novel pan-RAS-effector PPI inhibitor

Novel PPK1 inhibitor, preventing UTI effectively through the disruption of the PPK1 function

Novel PPK1 inhibitor, preventing UTI effectively through the disruption of the PPK1 function

Potent and selective antagonist of melanocortin-4 receptor (MC4R)

Novel anti-influenza agent, interrupting the crucial RNP trafficking, resulting in influenza replication inhibition, preventing virus-induced cytopathic effects

Novel Modulator of Water-Heme Interactions in Low-Spin P450 Complexes of CYP2C9d and CYP125A1

Novel inhibitor of budding of mVP40 and eVP40 VLPs, blocking mVP40-795 Nedd4 protein-protein interaction.

Specific blocker of the MARV VP40 PPxY-host Nedd4 interaction and subsequent PPxY-dependent egress of MARV VP40 VLPs.

Novel potent neuroprotectant, inhibiting glutamate-induced cell death, caspase-3 activation, and amyloid β1-42-induced cell death, also suppressing mitogen-activated protein kinase kinase 4 (MKK4) and c-jun N-terminal kinase (JNK) signaling activated by n

Novel inhibitor of IMPDH enzyme

Novel human double minute 2 (HDM2) inhibitor

Quorum sensing modulator as a PqsR antagonist

Pradigastat (LCQ-908) is a potent, selective and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor. Pradigastat has anti-obesity and anti-diabetic effects.

Inhibitor of prostaglandin (PG) synthesis

Inverse agonist at alpha-1 adrenergic receptors

Novel inhibitor of checkpoint kinase 1 (CHK1)

Inducer of Functional Neurorestoration Via the Sigma-1 Receptor

Allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3)

Potent and selective inhibitor of protein arginine methyltransferase 3 (PRMT3)

Novel potent and selective inhibitor of PRMT4 (also known as CARM1)

Novel potent PRMT5 inhibitor, exhibiting potent anti-proliferative activity against a panel of leukemia and lymphoma cells

Novel potent, selective, and cell active protein arginine methyltransferase 5 (PRMT5) inhibitor

Potent inhibitor of protein arginine methyltransferases (PRMTs)

Potent inhibitor of protein arginine methyltransferases (PRMTs)

Novel, Reversible Covalent BTK Inhibitor for Rheumatoid Arthritis

Novel reversible covalent selective LMP7 inhibitor

Antagonist at the NR1/NR2A subtype but an agonist at the NR1/NR2D subtype

Potent inhibitor of tumor metastasis, inhibiting calmodulin, sialic acid, lipoperoxidation, fibrinogen, cell-movement and the cell-cycle arrest

Novel selective procaspase-8 (Pro-C8) Inhibitor covalently binding the zymogen, or inactive precursor (pro-form), of caspase-8, but not other caspases

Prodrug of NBDHEX, selectively inhibiting glutathione transferase (GST P1-1) with better water solubility, and more potent anticancer activities

Novel potent cereblon degrader with DC50 of 200 nM, and 64% protein degradation, as quantified by western blot

Novel highly potent degrader against EGFRL858R/T790M and EGFRdel19, reaching the lowest DC 50 values among all reported EGFR-targeting PROTACs

Novel SLC-targeting chimeric degrader, targeting SLC9A1 and other SLC9 family members, effectively impairing pH homeostasis and differentially killing cancer cell lines

Novel noncovalent CDK12/13 dual inhibitor, inducing potent and selective CDK12-CycK degradation without affecting CDK13, suppressing DDR-associated genes and induced synthetic lethality with Olaparib

Novel PI3K degrader, showing a significant and complete degradation effect on PI3K kinase at a concentration of 10 μM within 8 h

Novel potent and selective p38α and p38β degrader

Novel degrader of HMGCR protein, potently blocking cholesterol biosynthesis with less compensatory upregulation of HMGCR

Novel potent epidermal growth factor receptor (EGFR) degrader, inducing EGFRdel19 and EGFRL858R/T790M degradation with DC50 values of 0.51 and 126 nM, showing potent anti-proliferative activity against HCC827 and H1975 cell lines with IC50 values of 0.83

Novel potent degrader of H-PGDS protein via the ubiquitin-proteasome system and in the suppression of prostaglandin D2 (PGD2) production

Proteolysis targeting chimeras (PROTAC), providing broad tissue distribution and knockdown of the targeted ERRalpha protein in tumor xenografts

Proteolysis targeting chimeras (PROTAC), providing broad tissue distribution and knockdown of the targeted RIPK2 protein in tumor xenografts

Novel SirReal-based PROTAC, inducing isotype-selective Sirt2 degradation, resulting in the hyperacetylation of the microtubule network coupled with enhanced process elongation

Novel selective and potent Fak degrader

The most potent and selective ERRα degrader

Novel PROTAC, targeting steroid hormone receptors for ubiquitination and degradation

Novel bacterial polyyne contributing to the antioomycete and plant-protective effects of P. protegens

Novel selective CB2 agonist (CB2: 17.4 nM and CB1: 5585 nM)

Novel potent and selective inhibitor of SETD2

Selective 5-HT4 agonist

Novel selective 5-HT6 receptor antagonist, enhancing cognition and memory and potently decreasing food intake and body weight in rodents

Novel potent and selective 5-HT2B receptor antagonist

Novel inhibitor of upstream IκB kinase (IKK), specifically inhibiting the IκB phosphorylation and degradation and the subsequent nuclear translocation of NF-κB

Highly potent and selective VDR-coactivator inhibitor

Naturally occurring inhibitor of FOXO1a nuclear export

Unique inhibitor of bacterial chromosomal partitioning, increasing the efficacy of bortezomib and sorafenib through regulation of stress granule formation

Potent competitive antagonist and positive modulator of the P2X2 receptor with >100-fold selectivity versus P2X4, P2X7, and several investigated P2Y receptor subtypes (P2Y(2,4,6,12))

Positive modulator of ATP effects at P2X2 receptors

Potent competitive antagonist and positive modulator of the P2X2 receptor

Novel fluorescent-labeled selective adenosine A2B receptor antagonist

Highly potent, selective, competitive, and reversible inhibitor of monoamine oxidase B (MAO-B)

Highly potent, selective, competitive, and reversible inhibitor of monoamine oxidase B (MAO-B)

Highly potent, selective, competitive, and reversible inhibitor of monoamine oxidase B (MAO-B)

Novel potent Lp1NTPDase inhibitor

Novel Potent and Selective Antagonist for the UTP-Activated P2Y4 Receptor

Novel Potent Agonist of the Orphan G Protein-Coupled Receptor GPR17 (EC 50 12 nM)

Novel potent and selective agonist of the orphan G protein-coupled receptor 84 (GPR84)

Fluorescent Probe for Ecto-5'--nucleotidase (CD73)

Novel Potent Agonist of the Orphan G Protein-Coupled Receptor GPR17 (EC 50 27.9 nM)

Novel Potent Agonist of the Orphan G Protein-Coupled Receptor GPR17 (EC 50 32.1 nM)

Fluorescent Probe for Ecto-5'--nucleotidase (CD73)

The first potent and selective inhibitor of human nucleoside triphosphate diphosphohydrolase-2 (NTPDase2)

Novel Agonist of the Cannabinoid-Activated Orphan G-Protein-Coupled Receptor GPR18, being selective versus the CB-sensitive receptors CB1, CB2, and GPR55

Novel Agonist of the Cannabinoid-Activated Orphan G-Protein-Coupled Receptor GPR18, being selective versus the CB-sensitive receptors CB1, CB2, and GPR55

Potent GPR55 antagonist

Novel Selective, competitive GPR55 antagonist

Novel Highly Sensitive PSMA Probe for NIR-II Imaging and Intraoperative Tumor Resection, Visualizing Tumors in Real Time

Novel PSMA ligand conjugated with fluorescent dye SulfoCy7, demonstrating good visualization of PSMA-expressing tumors and the absence of any explicit toxicity up to 87.9 mg/kg

Na-K ATPase inhibitor, stimulating SERCA2a and accelerating calcium cycling in heart failure by relieving phospholamban inhibition

Novel Bovine Viral Diarrhea (BVD) Inhibitor, specifically blocking BVDV cell entry

Novel inhibitor of hypoxia-induced VEGF expression

Natural antifungal agent, against postharvest fruit pathogenic fungi

Novel CFTR modulator, increasing CFTR protein expression across different mutations, including F508del, by increasing CFTR mRNA levels by ~1.5 to ~2-fold in HBE cells

Novel CFTR modulator, binding to the poly-r(C) binding protein 1 (PCBP1), showing an affinity for RNA-bound PCBP1 higher than that of free PCBP1

Novel Brk/PTK6 kinase inhibitor

Novel Inhibitor of the PTK7/β-Catenin Interaction Targeting the Wnt Signaling Pathway in Colorectal Cancer

Novel Inhibitor of the PTK7/β-Catenin Interaction Targeting the Wnt Signaling Pathway in Colorectal Cancer

Novel Potent Multi-target PTK Inhibitor for the Treatment of Idiopathic Pulmonary Fibrosis (IPF)

Unique promoter of SMN2 exon 7 splicing, acting by directly stimulating splicing of exon 7

Novel NIR fluorescent probe for the detection of Aβ oligomers

Novel non-competitive potent and selective inhibitor of protein tyrosine phosphatase 1B (PTP1B)

Novel PTEN-like mitochondrial phosphatase PTPMT1 inhibitor

Novel thermally activated delayed fluorescence (TADF) molecule that exhibits high external quantum efficiency (EQE) in non-doped organic light-emitting diodes (OLEDs) at high luminescence

Hsp90α- and Hsp90ß-selective inhibitor

Novel specific inhibitor of tumor Hsp90

Hsp90α- and Hsp90ß-selective inhibitor

Novel specific Hsp90b1 inhibitor

Dual inhibitor of PDE3 and PDE4

Natural heat shock protein 90 (Hsp90) inhibitor, potentiating the echinocandin drug caspofungin in caspofungin-resistant fungal pathogens, blocking the induction of caspofungin-responding genes required for the adaptation to cell wall stress through the c

Novel Grp94-selective inhibitor PU-WS13 biotin probe

Novel potent and selective CHEK2>Chk2 inhibitor

Novel potent anticancer agent, disturbing microtubule formation at the centrosomes and inhibiting the growth of tumors dose-dependently in the HCT116 human colon cancer xenograft model in vivo

Novel Plasmodium vivax Hypoxanthine-Guanine Phosphoribosyltransferase Inhibitor

Novel selective FGF14:Nav1.6 PPI modulator

Inhibitor of cell death induced by oxidative stress and inhibitor of AB1-40 aggregation induced by Cu2+ ion

Novel potent inhibitor of collagen prolyl-4-hydroxylases (CP4H)

Novel suppressor of cancerous cell growth and proliferation

Bacterial siderophore, acting as an iron-chelating growth promoter for Pseudomonas aeruginosa

Novel inhibitor of p53-MDM2 interaction

Novel inhibitor of the PyrD protein (a dihydroorotate dehydrogenase (DHODase) involved in pyrimidine biosynthesis), suppressing bacterial cytotoxicity, biofilm formation and antibiotic resistance

Natural phytotoxin, inducing monopolar spindle formation and suppressing proliferation of cancer cells

Novel highly potent agonist of the apelin receptor (APJ) receptor (APJ cAMP EC50: human 0.023nM; rat 0.024nM; dog 0.030nM; monkey 0.080nM)

Novel KMD5A inhibitor

Novel BBB-permeable substrate of pyrilamine-sensitive proton-coupled organic cation antiporter (PYSOCA), acting as a selective class I HDAC inhibitor

Y2/Y5 Neuropeptide Y receptor agonist, reducing food intake in normal-weight and obese individuals and the plasma levels of the hunger-promoting hormone ghrelin

Novel inverse agonist of 5-HT6 receptor

Novel class of bright near infrared window II (NIR-II, 1,000 - 1,700 nm) probe, being successfully used to achieve high spatial and temporal resolution imaging of hind limb vasculature, lymphatic system, and small tumor metastasis, as well as precise NIR-

Selective PAR1 negative allosteric modulator

Novel Heme Oxygenase-1 Inhibitor (HO-1 IC 50 =0.27μM; HO-2 IC 50 =0.46μM)

Novel reactive oxygen species (ROS) inducer, showing significant cytotoxicity in pancreatic cancer cells

Novel Nav1.7 channel blocker (IC 50 at 3.5±1.5 μM). being efficacious on chronic pain in mice

Novel fluorescent molecular rotor for the selective detection of the hybrid-conformation 22AG G-Quadruplex

Novel potent inhibitor of quorum sensing (QS) pathways, strongly blocking agr-type QS in S. aureus

Novel potent inhibitor of quorum sensing (QS) pathways, strongly blocking agr-type QS in S. aureus

Novel multitarget anti-AD agent, significantly increasing in adult neurogenesis and remyelination through Prox1/NeuroD1 and Wnt/β-catenin pathways, demonstrating beneficial effects in preclinical models of AD

Novel photodynamic antitumor agent

Modulator of specific GABAA receptors via the benzodiazepine site on the GABAA receptor

Potent, orally active fungal Cyp51 (lanosterol 14-α-demethylase) inhibitor

Natural disrupter of DNA replication and transcription via DNA intercalation, reducing oxygen intake and carbohydrate metabolism and the excitability of muscle fibers, inhibiting the drug efflux pump P-glycoprotein

Novel antivirulence agent against Vibrio vulnificus, inhibiting the quorum-sensing signaling pathway by controlling the DNA-binding affinity of SmcR and thus effectively alleviating the virulence of V. vulnificus in vitro and in vivo

Novel microtubule destabilizer

Second-Generation GluN2C- and GluN2D-selective positive allosteric modulator (PAM) of the N-methyl-d-aspartate (NMDA) receptor

Novel Potent and Specific Ligand of r(CCUG)exp, Targeting r(CCUG) Repeats in Myotonic Dystrophy Type 2, Facilitating Degradation by RNA Quality Control Pathways

Novel scavenger receptor class B type I blocker

Novel inhibitor of HDL uptake induced by overexpression of scavenger receptor BI (SR-BI)

Novel Antiviral agent for Enterovirus D68

Efficient stabilizer of Mahoney procapsids

Potent and selective antagonist of 5-HT2A receptors

Novel inhibitor of PI3Kβ and PI3Kδ, inhibiting growth of PTEN deficient breast and prostate tumor

Prodrug of Racemetirosine, an inhibitor of tyrosine 3-monooxygenase

Novel potent DNA-alkylating agent, inhibiting TBP/DNA interaction