Novel non-ATP competitive allosteric inhibitor of Aurora B kinase, binding in the allosteric site F

Anti-HIF-1alpha agent, inhibiting HIF-1alpha and cellular VEGF proteins

Novel inhibitor of STAT3 activation and dimerization through targeting the phosphotyrosine binding site within the SH2 domain

Stimulator of the production of growth hormone (GH) from the pituitary gland

Long-lasting stimulator of the production of growth hormone (GH) from the pituitary gland

Novel CK2 inhibitor, showing potent CSC inhibitory effects in A549 cells

Novel potent PfNDH2 inhibitor

Novel selective allosteric modulator of the protein kinase CK2, inducing apoptosis and cell death in 786-O renal cell carcinoma cells (EC50 = 5 µM) and inhibiting STAT3 activation even more potently than the ATP-competitive drug candidate CX-4945

Potent, reversible, and ATP-competitive inhibitor of casein kinase-2 (CK2)

Novel potent CK2 inhibitor

Novel CK2 inhibitor, targeting an allosteric pocket, exhibiting an IC50 of 3.4 μM against purified CK2α in combination with a favorable selectivity profile

Novel potent and selective inhibitor of CK2. modulating the aforementioned signaling cascades and counteracting 17-AAG-mediated up-regulation of HSP70 in brain cancer cells

Novel cell-permeable and selective inhibitor of human protein kinase CK2, inducing apoptosis in the prostate cancer cell line LNCaP

Novel inhibitor of CK2α, binding in the ATP pocket

Inhibitor of vascular adhesion molecule-1 (VCAM-1), HMGB1 phosphorylation, iNOS expression, NFkB activation; Antiinflammatory

Natural Dual Inhibitor for Wild Type and D816V Mutant of c-KIT Kinase

Negative control for CK156

Inhibitor of H5N1 avian influenza A virus infection

Inhibitor of respiratory syncytial virus (RSV)

Novel potent inhibutor of HIV-1 integrase

Novel protein tyrosine phosphatase-1B (PTP1B) inhibitor, neutralizing the toxicity of α-hemolysin, inhibiting β-secretase 1 (BACE1)-mediated insulin receptor cleavage

The most potent clathrin terminal domain-amphiphysin inhibitor reported to date

Natural modulator of voltage-gated sodium (NaV) channels

Novel two-photon polarity-sensitive lipid membrane probe

Antibiotic, acting as a mechanism-based β-lactamase inhibitor

Novel hypoxia-inducible factor (HIF)-1 inhibitor

Prostaglandin I2 analogue, dose-dependently inhibiting human and rabbit platelet aggregation and human platelet adhesion in vitro

Potent CLK1 and CLK2 inhibitor, also inhibiting SRPK1 and SRPK2

Potent and selective CLK1 and CLK2 inhibitor

Novel inhibitor of the human enzyme dimethylarginine dimethylaminohydrolase-1 (DDAH-1)

Corticosteroid Hormone Receptor Agonist

Hypolipaemic agent, reducing hypertriglyceridemia and hypercholesterolemia

Herbicide safener that is added to various herbicide formulations to reduce crop damage

Long-acting benzodiazepine, producing the active metabolite desmethyl-diazepam, which is a partial agonist of the GABAA receptor

Full agonist of GABAA receptors, acting as anxiolytic, sedative, hypnotic, amnesic, anticonvulsant and muscle relaxant agent

Precursor for tumor selective PET imaging (124I-CLR1404) or therapeutic radiation (131I-CLR1404)

Novel chromophore-linked metallo-β-lactamase (MBL) substrate as potential inhibitor against a panel of clinically relevant MBLs

Novel inhibitor of

Novel potent and selective dual inhibitor of c-Met and ALK, potently abrogating hepatocyte growth factor (HGF)-induced c-Met phosphorylation and cell migration, phosphorylation of ALK, EML4-ALK, and ALK resistance mutants in transfected cells

Novel selective agonist of cannabinoid CB2 receptors

Novel Matrix Metalloproteinase Inhibitor As a Potent Antihemorrhagic Agent

First-in-class dual PDE5 and HDAC6-selective inhibitor

Novel Epigenetic Inhibitor Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with In Vivo Efficacy in Multiple Myeloma

Novel inhibitor of

Novel Hedgehog pathway inhibitor, revealing the receptor GPR39

Novel Potent and Specific Target Of Rapamycin Complex 2 (TORC2) Inhibitor

Novel ultrapotent and selective inhibitor of of human β-Factor XIIa

Novel peptide STAT5 inhibitor, blocking IL-2/sIL-2Rα signaling and inhibiting T reg cell development

Novel SARS-CoV Mpro inhibitor which has its P1-phenylalanine residue bound to the relatively hydrophilic S1 pocket of the enzyme and yet exhibits a high inhibitory activity against SARS-CoV Mpro, with Ki = 2.24 ± 0.58 μM

Potent dual 5-lipoxygenase (5-LOX) inhibitor and platelet-activating factor (PAF) receptor antagonist

Inhibitor of DprE1, an epimerase required for cell wall biosynthesis

Novel allosteric modulator of the β2 adrenergic receptor (β2AR), binding to a pocket formed primarily by the cytoplasmic ends of transmembrane segments 1, 2, 6 and 7 as well as intracellular loop 1 and helix 8

Selective and potent potentiator of nAChRs containing an α4

Novel TRPV1 modulator, also modulating both CB1 and CB2 receptors

Novel Inhibitor for RNA-Dependent RNA Polymerase of Norovirus

Novel Potent Inhibitor of the HIV-1 Nucleocapsid Protein

Novel Zika virus (ZIKV) NS2B-NS3pro protease inhibitor

Novel blocker of binding of CXCL12 to CXCR4

Novel partial blocker of GluK1, with GluK2 being unaffected

Novel potent and selective blocker of the calcineurin-NFAT interaction (KD=16nM), preventing acute lung injury, being a promising novel treatment for ARDS and other inflammatory diseases

N-methyl-D-aspartate (NMDA) receptor ligand, selectivity targeting the intrachannel PCP/ketamine/MK-801 site of NMDA receptor

Novel and selective noncompetitive antagonist of the NMDA

Novel potent RIPK1/necroptosis ligand, penetrate the blood-brain barrier

Novel inhibitor of mitogen-activated protein kinase (MAPK)

Bioluminescent probe

Natural lariat depsipeptide, inhibiting VEGFA/VEGFR2 expression and suppressing tumor growth in glioblastoma xenografts, targeting Sec61 to prevent biogenesis of secretory and membrane proteins

Novel potent and selective inhibitor of the interaction between Hsp47 and collagen

Novel potent and selective inhibitor of the interaction between Hsp47 and collagen

Novel potent and selective inhibitor of the interaction between Hsp47 and collagen

Natural differentiation inducer of human promyelocytic leukemia cells

Inhibitor of tubulin polymerization, preventing cancer cells from producing microtubules

Inhibitor of tubulin polymerization; vascular disrupting agent (VDA)

Inducer of G2/M-phase cell cycle arrest and cell death in cancer cell lines

Dual inhibitor of phospholipid transfer protein and microsomal triglyceride transfer protein

Novel inducer of Klotho (KL) expression

Natural triketide pyrone, functioning as a sulfate shuttle and its sulfated derivative being accepted as donor molecules by the PAPS-independent arylsulfate sulfotransferase (ASST) Cpz4 to yield sulfated caprazamycin intermediate

A mixture of estrogen hormones used to treat menopause symptoms such as hot flashes and vaginal changes, and to prevent osteoporosis (bone loss) in menopausal women, being also used to replace estrogen in women with ovarian failure or other conditions tha

Novel fluorescent copper probe

Novel potent and selective melanocortin-4 receptor inhibitor, possessing 15-fold selectivity for the MC4R versus the MC3R

Novel positive allosteric modulator of the GABA(B) receptor

Novel positive allosteric modulator of the GABA(B) receptor

Natural potent cytotoxic agent against multiple cancer cell lines, acting on cells as a protein synthesis inhibitor, targeting the eukaryotic translation elongation factor 1A (eEF1A), a target shared by other lipophilic cyclic peptide natural products

Novel photoCORM, exhibiting good cellular uptake and real-time monitoring ability of CO uncaging by a color change approach in cancerous B16F10 cells

Novel class I mutation corrector, rescuing CFTR mutations in nucleotide-binding domain 1 (NBD1) by modulating proteostasis

Selective glucocorticoid receptor antagonist

Preformed water-soluble complex of corticosterone and 2-hydroxypropyl-β-cyclode​xtrin

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Novel Dual Covalent Inhibitor and Potential Fluorescent Label of HadA in Mycobacterium tuberculosis

Novel Potent Mitochondria-Targeted Photodynamic Therapy Anticancer Agent

Novel viral propagation inhibitor, binding to the revised attenuator hairpin structure of the SARS-CoV-2 frameshifting element (FSE), stabilizing the hairpin's folded state and reducing frameshifting efficiency in cells

Potent and selective leukotriene B4 antagonist

Novel potent and selective p38alpha inhibitor

Inhibitor of glycogen phosphorylase; Antidiabetic

Inhibitor of Kv1.3 potassium ion channels

Novel selective α5 GABA A receptor agonist

Novel Mdr1 P-glycoprotein substrate

Potent PPARα agonist with a Ki of 10.8 nM

Novel nonnucleoside reverse transcriptase inhibitor (NNRTI)

Novel inhibitor of against human liver FBPase (IC50, 0.029±0.006 μM) and high selectivity relative to the other six AMP-binding enzymes, producing significant glucose-lowering effects on both type 2 diabetic KKAy mice and ZDF rats

Novel non-RBD binding modulator to inhibit SARS-CoV-2 by prohibiting the conformational change of the spike (S) protein

Novel potent inhibitor of CpFIKK catalytic activity

Novel selective inhibitor of the CREB binding protein (CBP)

Unique inhibitor of MDM2, inhibiting MDM2-p53 interaction and promoting MDM2 degradation

Novel CpIMPDH inhibitor

Novel selective NADPH oxidase 2 (Nox2) inhibitor, attenuating endothelial cell inflammation and vessel dysfunction and restoring mouse hind-limb flow

Novel selective NADPH oxidase 2 (Nox2) inhibitor, attenuating endothelial cell inflammation and vessel dysfunction and restoring mouse hind-limb flow

Novel positive allosteric modulator (PAM) of metabotropic glutamate receptor 5 (mGlu5)

Novel inhibitor of death-associated protein kinase 1 (DAPK1), also inhibiting VEGF-receptor 2 and tyrosine-protein kinase SRC

Novel endothelin receptor antagonist, suppressing the upregulation of matrix metalloproteinases and connexin 43 in hyperthyroid myocardium

Novel potent and selective fluorescent inhibitor of glutaminase (GLS1)

Liposomal-encapsulated combination of daunorubicin and cytarabine for the treatment of newly diagnosed tAML or AML with myelodysplasia-related changes (AML-MRCs)

Novel RORγt inhibitor, suppressing Th17 cell differentiation, reducing the severity of experimental autoimmune disease models such as EAU, EAE, and type 1 diabetes

Novel RORγt inhibitor, suppressing Th17 cell differentiation, reducing the severity of experimental autoimmune disease models such as EAU, EAE, and type 1 diabetes

Novel NIR-II probe, noninvasively and dynamically visualizing and monitoring many physiological and pathological conditions of circulatory systems, including lymphatic drainage and routing, angiogenesis of tumor, and vascular deformity such as arterial th

Novel potent HDAC8 inhibitor

Novel probe for selectively detecting sAβ species in Alzheimer's disease (AD)

Foster Resonance Energy Transfer (FRET) pair for Aβ40 aggregates

Substrate for the assay of creatine kinase, providing a quick source of energy for muscle fibers to contract when they need an initial burst of energy

Novel potent and cell-permeable inhibitor of cAMP-response element binding protein (CREB)

Novel CREBBP Bromodomain Inhibitor

Natural antiangiogenic homoisoflavanone, inhibiting the proliferation, migration and tube formation ability of human retinal microvascular endothelial cells

Antineoplastic and Antibacterial; Inducer of death in cancer cells through a reactive oxygen species (ROS)-mediated mechanism; Dark blue cancer cell growth inhibitor

Selective dopaminergic reuptake inhibitor

Novel potent, selective, and reversible inhibitor of human monoamine oxidase B (hMAO-B)

Novel potent, selective, and reversible inhibitor of human monoamine oxidase B (hMAO-B)

Novel potent and mycobacteria-specific antimycobacterial agent, targeting MmpL3, improving the antimycobacterial activity and being also potent against Mtb

Novel potent and mycobacteria-specific antimycobacterial agent, targeting MmpL3, a mycobacterial mycolic acid transporterr, demonstrating MIC = 0.03, 2, and ≤ 0.12 μg/mL against Mabs, Mycobacterium avium complex (MAC), and Mtb respectively

Potent and selective inhibitor of AKR1C3

Potent and selective inhibitor of AKR1C3

Potent and selective CRTH2 antagonist

TLR4 antagonist, protecting against advanced diabetic nephropathy

Novel potent powerful lipid A analogue as a conjugation-ready TLR4 ligand

Novel TRPM8 agonist

Novel water-soluble, potent, and selective TRPM8 receptor agonist

Inhibitor of gene products associated with cell survival, proliferation, invasion, and angiogenesis, targeting NF-κB pathway, showing antiproliferative activity and unique mode of action

Novel photoisomerizable potent and selective M1 ligand, mimicing the tricyclic chemical structure and display reversibly controlled activity, showing stronger inhibition upon illumination both in vitro and in cardiac atria ex vivo

Novel modulator of PI3K and NF-κB activities, blocking migration and production of inflammatory mediators

Novel substrate-competive c-Src inhibitor

Novel G9a (EHMT2) inhibitor, binding tightly inside the active site cavity of G9a, inhibiting the activity of G9a in both enzyme and cell based assays with much lesser toxicity than BIX-0129

Dual inhibitor of angiogenesis and lysophosphatidic acid acyltransferase

Novel potent dual inhibitor of ALK and c-Met

Novel cell permeable degrader of BRD4

Novel anticancer agent, effectively killing multi-drug resistant cancer cells and a panel of different cancer cells originated from a variety of different tissues including breast and skin, preventing tubulin polymerization, leading to the cell cycle arre

Novel anticancer agent, effectively killing multi-drug resistant cancer cells and a panel of different cancer cells originated from a variety of different tissues including breast and skin, preventing tubulin polymerization, leading to the cell cycle arre

Inhibitor of prostate-specific membrane antigen (PSMA)

Novel Serotonin 5-HT 2C Receptor Positive Allosteric Modulator (PAM) with Enhanced Drug-like Properties

Novel fluorescent RXR agonist

Novel r(CUG) repeat expansion cleaver, specifically recognizing the 3-dimensional structure of r(CUG)exp, cleaving it more selectively among transcripts containing short, nonpathogenic r(CUG) repeats than an oligonucleotide that recognizes RNA sequence vi

5-HT1A receptor agonist

Agonist for the cannabinoid receptors, with Ki values of 59.21 nM at CB1 and 136.38 nM at CB2 and EC50 values of 11.98 nM at CB1 and 16.2 nM at CB2

Inducer of demyelination and motor dysfunction via upregulation of IGF-1

Potent anti-cancer agent

Novel dual PXR and AhR agonist

Novel potent pregnane X Receptor (PXR) agonist

Inhibitor of PIM, suppressing cyclin-Dependent Kinase 2 (CDK2)

Novel potent and selective inhibitor of PI5P4Ks

Direct thrombin inhibitor, preventing occlusive arterial and venous thrombosis in a canine model of vascular injury

Potent serine protease inhibitor, targeting the S 2 S 3 thrombin and FXa subsites

Novel orally efficacious antimalarial agent against P. falciparum 3D7 ( IC50: 51 nM)

Potent antimalarial agent against Plasmodium falciparum 3D7

Potent antimalarial agent against Plasmodium falciparum 3D7

Novel Wnt/β-Catenin Inhibitor, Preferentially Inhibiting the Growth of Breast Cancer Stem-like Cells

Novel potent and substrate-competitive PTP1B and TCPTP dual inhibitor

Potent LTB4 receptor antagonist

Novel low-impact ampakine that can safely activate AMPA receptors without causing excito-neurotoxicity, rapidly crossing the blood-brain barrier (T max = 2 min), protecting against respiratory depression

Novel inhibitor of CXCL8-mediated chemotaxis through selective regulation of CXCR2-mediated signaling

Nonsteroidal dermatologic and anti-inflammatory agent, blocking the MEK1/2-Erk1/2 pathway, inhibiting chronic contact hypersensitivity responses (CHRs) and the rebound phenomenon following withdrawal of corticosteroid therapy without immunosuppression

Novel potent CXCR2 antagonist

Novel CXCR2 selective antagonist with a low CXCR1 antagonism preference

Selective D1 agonist with anti-Parkinsonian activity

Novel ABA receptor agonist, preferentially activating Pyrabactin Resistance 1 (PYR1) with low nanomolar potency

Androgen receptor (AR) antagonist, inhibiting AR function in castrate-resistant prostate cancer (CRPC)

Blue fluorescent amino acid, exhibiting blue fluorescence (λ max ~ 405 nm) with a high quantum yield and long lifetime

Novel Effective Aminoluciferin Derivative for Deep Bioluminescence Imaging

Natural antibacterial peptide, activating the AAA+ protease ClpC/ClpP, causing cell death by uncontrolled protein degradation

Novel PD-1/PD-L1 inhibitor, binding two PD-L1 and efficiently block the PD-1/PD-L1 interaction

Natural irreversible inhibitor of acetylcholinesterase (AChE)

Novel bicyclic peptidyl pan-Ras inhibitor, binding selectively to the GTP-bound forms of wild-type and mutant Ras isoforms (K D = 21 nM for KRasG12V-GppNHp) and being highly cell-permeable and metabolically stable (serum t1/2 > 24 h)

Novel Cyclic Peptide Inhibitor of the p6/UEV Protein-Protein Interaction, disrupting the p6/UEV interaction with an IC50 of 6.17 ± 0.24 μM by binding to UEV with a Kd of 11.9 ± 2.8 μM.

Immunosuppressant

Immunosuppressant

Macrocyclic immunosuppressive peptide, exhibiting a higher plasma concentration than Cyclophilin A

immunosuppressive agent

Cyclic alkylaminoluciferin substrate for firefly luciferase

Cyclic alkylaminoluciferin substrate for firefly luciferase, emitting 4.7-fold more light than aminoluciferin, and 2.6-fold more light than D-luciferin

Non-peptidic, potent, and orally active stromelysin inhibitor;

Cyclic alkylaminoluciferin substrate for firefly luciferase

Novel S1PR4 antagonist

Novel non-peptidic NPBWR1 (GPR7) antagonist

Novel short-acting KOR antagonist

Potent and selective human CYP11B1 inhibitor

Novel potent and selective CYP1A1 inhibitor, antagonizing B[a]P mediated activation of aromatic hydrocarbon receptor (AhR) in yeast cells, and protecting human cells from CYP1A1-mediated B[a]P toxicity in human cells

Novel covalent allosteric CYP3A4-effector

Novel fungal lanosterol 14α-demethylase (CYP51)/histone deacetylase dual inhibitor, blocking ergosterol biosynthesis and HDAC catalytic activity in fungus, suppressing the function of efflux pump, yeast-to-hypha morphological transition, and biofilm forma

Novel CypD inhibitor, binding strongly to CypD and attenuating mitochondrial and cellular perturbation insulted by Aß and calcium stress

Novel non-peptidic inhibitor of cyclophilin D as neuroprotective agents in Aβ-induced mitochondrial dysfunction

Novel potent tri-vector cyclophilin inhibitor

Inhibitor of Pentaglycine Interpeptide Bridge Synthesis

NRAS inhibitor, targeting the post-translational S-palmitoyl modification of NRAS, causing a dose-dependent decrease in NRAS palmitoylation and inhibiting downstream signaling in melanoma cells with an activating mutation in NRAS

Inhibitor of cholinesterase activity, β-amyloid aggregation and Ca overload; Novel multi-target-directed ligand (MTDL); Activator of kinase 1 and 2 (ERK1/2) and Akt/protein kinase B (PKB) pathways