Potent inhibitor of cabonic anhydrase 2 (CA2)

Negative allosteric modulator of human P2X7 and a positive allosteric modulator of rat P2X7

Potent inhibitor of adipocyte differentiation and weak partial agonist of

Novel Selective and Nonpeptidomimetic Proteasome Inhibitor As an Antimalarial, specifically inhibiting the proteasome activity in P. falciparum

Novel agonist for retinoid X receptor

Inhibotor of active Vaccinia-Related Kinases (VRK)

Novel inhibitor of CDK

Novel selective and soluble inhibitor of tumor necrosis factor-alpha converting enzyme (TACE)

Potent and selective full agonist for peroixisome proliferator-activated receptor-alpha

Novel potent RET kinase inhibitor

Potent TrkA kinase inhibitor

Novel agonist at the adenosine A1 receptor

Orally active, nonsteroidal tamoxifen derivative and a ligand for the estrogen receptors (ERs), steroid receptor members of the nuclear receptor superfamily of transcription factors

Inhibitor of Mer Kinase, also inhibiting EGFR

Novel VEGFR inhibitor, also a moderate inhibitor of BET proteins with an IC 50 value of 4.6 μM for BRD4(1)

Potent inhibitor of PfDHODH, showing greater than 4,000-fold selectivity for the malarial enzyme

Novel inhibitor of EGFR

Novel inhibitor of firefly luciferase derived from Photinus pyralis (FLuc), the most widely used luciferase

Selective cyclin dependent kinase inhibitor; Inhibitor of Yes1 kinase; Inhibitor of binding or entry into cells for Lassa Virus

Selective agonist of peroxisome proliferator-activated receptor-γ (PPARγ)

Potent and selective inhibitor of glycogen synthase kinase 3 (GSK3)

Novel and potent inhibitor of VEGFR2 tyrosine kinase, non-selectivey inhibiting AURKA and AURKB

Potent GSK-3 inhibitor, highly selective over CDK-2

Novel Inhibitor of GSK3beta

Novel inhibitor of mitosis and cytokinesis in T. brucei which causes human African trypanosomiasis (HAT)

Novel potent and selective inhibitor of the cytochrome bc1 complex of mitochondrial electron transport in P. falciparum

Novel polo-like kinase (PLK1) inhibitor

Novel NAD+-competitive Sirt2 inhibitor

Novel modulator of NF-Y transcription, inhibiting the binding of NF-Y to DNA, blocking cellular proliferation and cell cycle progression, interacting with a variety of CCAAT-containing promoters leading to p53-independent cell cycle arrest

Novel inhibitor of Nav1.7

Novel potent inhibitor of NaV1.7 and highly selective against NaV1.5, having limited selectivity against NaV1.1 and NaV1.2

GX-936 analog, antagonist of voltage-gated sodium 1.7 (Nav1.7) channels

AMPA antagonist

Novel bacterial DNA gyrase inhibitor, exhibiting antimicrobial activity and inhibiting bacterial cell division

Novel Rho-associated coiled coil-formed protein kinase (ROCK) inhibitor, exerting strong intraocular pressure (IOP)-lowering effects into the eyes of monkeys

Novel Rho-associated coiled coil-formed protein kinase (ROCK) inhibitor, exerting strong intraocular pressure (IOP)-lowering effects into the eyes of monkeys

Novel full H1 agonist

Novel class of selective diacylglycerol acyltransferase 2 (DGAT2) inhibitor

Novel class of selective diacylglycerol acyltransferase 2 (DGAT2) inhibitor

Novel water-soluble and biocompatible small-molecule near-infrared II (NIR-II) fluorescent dye

Inhibitor of acetic acid-induced writhing response

Novel inhibitor of STAT3 activation, inhibiting head and neck cancer cell proliferation in a dose dependent manner

Inhibitor of monoamine oxidase (MAO)

Novel hemagglutinin (HA) protein inhibitor, inhibiting entry and replication of diverse influenza viruses via the HA protein, showing potent antiviral activity against diverse H1N1, H5N1, and H3N2 influenza viruses encoding HA proteins from both groups 1

Herbicide, being used for the control of broad-leaved weeds in cereals and oilseed rape

Topical corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictor activities, inducing phospholipase A2 inhibitory proteins, activating gene expression of anti-inflammatory proteins mediated via the corticosteroid receptor response element

Antimalarial, binding to plasmpesin, a haemoglobin degrading enzyme unique to the malarial parasites

Selective peroxisome proliferator-activated receptor gamma (PPAR-gamma) modulator with antilipidemic activity

Novel HaloPROTAC degrader, inducing degradation of HaloTag fusion proteins

Novel Wnt inhibitor, blocking Wnt signaling downstream of beta-Catenin

Novel inhibitor of cathepsin K (CatK)

Novel selective inhibitor of Hap2/3/4/5p mediated transcription in vivo.

Natural antiproliferative, antifungal, antitumor agent, suppressing the epithelial-mesenchymal transition (EMT) process and inhibiting activation of the FAK/Src/STAT3 signaling pathway in A375 cells, targeting RACK1 to suppress cancer cell migration

Novel p300/CBP HAT inhibitor

Precursor for HATRIC-based ligand receptor capture (HATRIC-LRC)

Hepatocellular carcinoma (HCC)-selective cytotoxin, suppressing AKT anti-apoptotic signaling

Novel Inhibitor of Mycobacterium tuberculosis DosRST signaling and persistence

Novel Inhibitor of Mycobacterium tuberculosis DosRST signaling and persistence

Novel inhibitor of DosRST, inhibiting DosR DNA binding in a dose-dependent manner by directly targeting DosR

Novel inhibitor of DosRST, inhibiting Mtb survival during hypoxia-induced NRP, directly targeting the sensor kinase heme, via a mechanism that is distinct from the oxidation and alkylation of heme previously observed with artemisinin (HC101A)

Novel inhibitor of human carbonic anhydrase XII (hCA-XII), demonstrating significant antiproliferative activity against hypoxic tumor cell lines

Novel selective dual carbonic anhydrase IX and XII inhibitor

Novel Nek2 inhibitor, successfully mitigating drug resistance in bortezomib-resistant multiple myeloma; Potent AXL kinase inhibitor

Novel inhibitor of human coronavirus 229E (hCoV 229E) replication with an EC50 value of 5.5 µM

Selective modulator of amyloid-beta peptide degradation, regulating Abeta levels.

Novel copper-dependent cytotoxic agent, being highly potent against a panel of pancreatic, small cell lung carcinoma, prostate cancer, and leukemia models, with IC50 values in the low-to-mid nanomolar range

Antiviral agent against HCV genotype 2a JFH-1 infected in human Huh7.5.1 cells

Novel Inhibitor of Hepatitis C Virus

High affinity and selective colchicine site tubuline inhibitor amenable to radiolabel with C-11, a positron emitting isotope

Novel PROTAC HDAC6 degrader, efficiently and selectively decreased HDAC6 levels in several cell lines, including activated THP-1 cells

Novel potent and selective PROTAC degrader of HDAC6 protein

Novel hHDAC6 inhibitor, having low inhibitory potency over hHDAC1 and hHDAC8, as potential pharmacological tools for idiopathic pulmonary fibrosis (IPF) treatment

Novel potent HDAC6 inhibitor with an IC 50 of 31 nM and excellent HDAC6 selectivity (SI = 338 for HDAC6 over HDAC3), displaying high antiproliferative activity against various cancer cell lines including the HDACi-resistant YCC3/7 gastric cancer cells (IC

Novel HDAC6 isoform-selective inhibitor, increasing the acetylation level of α-tubulin with little effect on the acetylation of histone H3, inducing apoptosis in HL-60 cell by activating caspase 3

Potent and selective HDAC6 inhibitor

Potent and selective HDAC6 inhibitor

Novel highly potent and selective HDAC6 inhibitor with an IC 50 of 2.54 nM and being more than 290- to 3300-fold selective over other HDAC isoforms

First-in-class proteolysis targeting chimera (PROTAC) for selective degradation of histone deacetylase 8 (HDAC8)

Novel Selective Histone Deacetylase 8 (HDAC8) Inhibitor with Anti-Neuroblastoma Activity

Novel HDAC inhibitor, targeting HDAC2, HDAC3, HDAC4, HDAC5, HDAC7, HDAC8, and HDAC9

Novel Histone deacetylase (HDAC) inhibotor, displays potent inhibitory activity towards human HDACs and several cancer cells lines

HDL376 is a scavenger receptor class B type I (SR-BI) inhibitor. HDL376 directly inhibits SR-BI-mediated lipid transport in cells and in liposomes reconstituted with purified SR-BI (IC50 = 0.22 μM). HDL376 can be used for the research of atherosclerotic coronary artery disease.

Potent antifungal agent, hosting defense peptide mimic through a membrane-active mechanism

Potent inhibitor of the ErbB receptor family (IC50 values are 0.3, 0.5 and 1.1 nM for ErbB1 (EGFR), ErbB4 and ErbB2 respectively)

Anti-inflammatory and anti-cancer agent, disrupting the cooperation of CCAAT-box/enhancer-binding protein beta (C/EBPß) and co-activator p300

Natural anti-inflammatory and anti-cancer agent

Inhibitor of interleukin-1β-induced MIP-1β production

Cytotoxic peptide, inducing mitotic arrest and abnormal spindle formation

The biosynthetic precursor of gossypol

Heparan sulfate antagonist

Heparin derivative for treatment of thrombotic diseases

Master regulator of iron homeostasis, contributing to Swedish mutant APP-induced osteoclastogenesis and trabecular bone loss

Novel inhibitor of Tau aggregation against Tau-related neurodegenerative diseases including Alzheimer's disease (AD)

Novel LsrK inhibitor (ID 50 119 μM) agaist antimicrobial resistance (AMR)

Novel TGF-β Signaling Inhibitor

Novel orally bioavailable, non-peptide thrombopoietin (TPO) receptor agonist

Novel inhibitor of the phosphorylation of DRP1, stimulating a phenotype suggestive of respiration through mitochondrial normalization and demonstrating activity in Vemurafenib-resistant melanoma in vivo

Novel potent inducer of hexamethylene bis-acetamide inducible protein 1 (HEXIM1)

Potent inducer of oxidative stress as well as cell cycle arrest in the S-phase, significantly decreasing intracellular ATP level

Insulin-regulated aminopeptidase (IRAP) inhibitor, mprovin memory in control and memory-deficient mice models

Novel type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRalpha, Kit, and Src kinases

Fragment 177-191 of human growth hormone, regulating fat metabolism but without the adverse effects on blood sugar or growth, stimulating lipolysis (the breakdown or destruction of fat) and inhibiting lipogenesis (the transformation of nonfat food materia

Novel sulfur-triazole exchange (SuTEx) covalent probe with ~5-fold enhanced chemoselectivity for tyrosines over other nucleophilic amino acids

Positive allosteric modulator at the barbiturate/picrotoxin site of the GABAA receptor

Non-nucleoside reverse transcriptase inhibitor

Potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus (HIV)

Potent inhibitor of multidrug-resistant human immunodeficiency virus-1 (HIV-1)

Hexapeptide sequences of hIAPP, being sufficient for the formation of beta-sheet-containing amyloid fibrils and coiling around each other in a typical amyloid fibril morphology

Pentapeptide sequences of hIAPP, being sufficient for the formation of beta-sheet-containing amyloid fibrils and self-assemble laterally into unusually broad ribbons

CNS active anticonvulsant and ultra-short acting hypnotic

Novel HIF-1alpha inhibitor

Novel HIF-1alpha-p300 Protein Protein Interaction inhibitor

Novel hypoxia inducible factor hydroxylase modulator

Novel hypoxia inducible factor hydroxylase modulator

Novel HIF Pathway Inhibitor

Natural muscarinic receptor antagonist

Novel Potent Inhibitor of HIPK1/HIPK2 Kinase

Natural alkaloid, demonstrating significant cytotoxicity against a panel of human and murine tumor cell lines

Allosteric inhibitor of ATP phosphoribosyltransferase (ATPPRT), binding to the ATPPRT:ATP complex via a two-step binding mechanism, inhibiting ATPPRT competitively and likely uncompetitively, respectively, against PRPP and ATP

Novel enhancer of catalytic efficiency of neurolysin

Novel enhancer of catalytic efficiency of neurolysin

Novel photoaffinity-labeled probe for full-length human immunodeficiency virus-1 integrase (HIV-1 IN)

Novel highly potent HIV-1 inhibitor with broad-spectrum activity (EC50 = 2.0-57 nM) against resistant strains, exhibiting good solubility and safety profiles and a good PK profile with an oral bioavailability of 59% in rats

AMPA Receptor Positive Allosteric Modulator

Novel orally bioavailable STAT3 inhibitor

Novel potent orally bioavailable inhibitor of signal transducer and activator of transcription 3 (STAT3)

Novel apigenin analogue, suppressing pancreatic stellate cell proliferation

Novel inhibitor of YycG histidine kinase (HK), showing potent antibiofim activity against Staphylococcus epidermidis

Novel allosteric hexokinase 2 (HK2) modulator, selectively detaching HK2 from the mitochondria

Novel Metformin Derivative; Inhibitor of Proliferation and Invasion of Triple-Negative Breast Cancer Cells

Novel SARS-CoV-2 Main Protease (Mpro) inhibitor, binding to Subsites S1 and S2 (K d =0.69 µM)

Selective Acetylcholinesterase Inhibitor

Novel phosphoramidate prodrug of ddhCTP, effectively reducing titers of Zika and West Nile viruses in cell culture with minimal nonspecific toxicity to host cells

First-in-class inhibitor of protein arginine methyltransferase 5 (PRMT5)

Novel Nerve Agent Reactivator

Potent and highly selective FABP4 inhibitor

Novel antagonist to the inhibitors of apoptosis (IAPs), potentiating cell death in EGFR-overexpressing non-small-cell lung cancer cells

Novel highly potent, selective, and competitive hMAO-B inhibitor with high BBB permeability profile and neuroprotective action (IC 50 = 42 nM; SI > 2375)

Potent stimulator of gamma delta T cells

Protein kinase C partial agonist, targeting the C1 domain, inhibiting cell proliferation, decreasing cell viability and inducing an apoptotic response

Irriversible inhibitor of GSK3

Potent inhibitor of nicotinamide phosphoribosyltransferase (Nampt)

Potent and specific integrin α4ß1 or very late antigen 4 (VLA-4) receptor antagonist, binding to vascular cell adhesion molecule-1 (VCAM-1) and fibronectin

Novel food intake-reducing agent

Potent and selective I ks channel blocker

Novel sialidase-activatable fluorescence probe with improved stability for the sensitive detection of sialidase

Novel Hexosaminidase-Targeting Fluorescence Probe for Visualizing Human Colorectal Cancer.

Novel chemical probe for heterochromatin formation and function, disrupting of heterochromatin-mediated transcriptional gene silencing

Novel chemical probe for heterochromatin formation and function, disrupting of heterochromatin-mediated transcriptional gene silencing

Novel Blinking Fluorescent Probe for Tubulin Nanoscopy in Living and Fixed Cells

Novel selective inhibitor of the lymphocytic leukemia (LL) cell survival , Selectively Enhancing the Killing Effect through STAT3 Binding on Lymphocytic Leukemia Cells In Vitro and In Vivo

Novel strobilurin acaricide, exhibiting larvicidal and ovicidal activities against various acarids

Highly potent and selective ligand for the GHB binding sites, binding with 27 times better affinity than GHB itself and acrossing the blood brain barrier in vitro and in vivo

Fluorescent indicator of apoptosis, binding the minor groove of DNA at A and T rich regions

Novel specific Aurora B inhibitor

Antibiotic

Natural inhibitor of dietary fat absorption and showing strong anti-obesity activity

Histamine H1 receptor antagonist

Novel c-Met inhibitor, markedly reducing tumor growth, showing excellent pharmacodynamics, and suppressing cell proliferation and microvessel density in an orthotopic model of triple negative breast cancer

Novel highly selective switch-on fluorescence sensor, targeting telomeric dimeric G-quadruplex, discriminating the telomeric dimeric G-quadruplex TTA45 against other types of DNA structures accompanied by a drastic enhancement of the emission intensity wi

Novel silanol-based human pregnane X receptor (PXR) agonist

Loxoprofen active metabolite, acting as a safe intravenous NSAID with superior anti-inflammatory and analgesic activities

Novel Probe of the hras-1Y i-motif , selectively and directly interacting with the hras-1Y i-motif.

Inhibitor of human rhinoviruses serotype 14 (HRV-14)

Novel inhibitor of imatinib-resistant BCR-ABL T315I mutation in chronic myeloid leukemia

μ-Opioid Receptor Agonist

Novel anticancer Gold(III) agent with remarkable cytotoxicity to gastric cancer cells

Novel potent inhibitor of the recombinant FLT3 kinase and its mutant forms, blocking the proliferation of AML cell lines, harboring oncogenic FLT3-ITD mutations with remarkable IC50 values, which were comparable to the approved FLT3 inhibitor quizartinib,

Novel inhibitor of lipoteichoic acid (LTA) biosynthesis, potently inhibiting S. aureus and E. faecalis growth and biofilm formation

Novel Peripherally-Restricted Kappa Opioid Receptor (KOR) Agonist with Antinociceptive and Antipruritic Effects

Novel inhibitor of heat shock 27 kDa protein (HSP27), significantly inducing AR degradation in GBM cells via the proteasomal pathway, selectively inhibiting AR-overexpressed GBM cell growth with IC 50 values around 5 nM

Novel Hsp90-Aha1 chaperone complex formation inhibitor, enhancing F508del-CFTR channel activity

Novel potent inhibitor of heat shock protein 90 (Hsp90), effectively reducing the expression levels of Hsp90 client proteins including Her2, EGFR, Met, Akt, and c-Raf

Novel heat shock protein 90 (Hsp90) inhibitor

Novel heat shock protein 90 (Hsp90), more potent enantiomer

Novel macrocyclic calcitonin gene-related peptide (CGRP) receptor antagonist

Novel macrocyclic calcitonin gene-related peptide (CGRP) receptor antagonist

Novel allosteric antagonist of the glucagon-like peptide-1 receptor (GLP-1R)

Novel, potent, selective, and orally efficacious dual antagonist of the orexin receptors

Novel activator of PC2

Novel analgesic agent, activating TRPA1 and subsequently desensitizing the channel, exhibiting higher inhibitory activity than resveratrol

Adhesive peptide (sequence 351-359 mapped on the Human Vitronectin Protein), covalent and selective functionalizing on glass and titanium surfaces, increasng osteoblast attachment and adhesion strength and to promoting osseointegration

Novel human antigen R (HuR) ligand, acting as a HuR-RNA interferer

Novel CK2-Specific Pt(II) Compound, Reversing Cisplatin-Induced Resistance by Inhibiting Cancer Cell Stemness and Suppressing DNA Damage Repair in Non-small Cell Lung Cancer Treatments

Inhibitor of apurinic endonuclease-1 (APE1) by direct protein binding

Activable Probe for Noninvasive Hydroxyl Radical Imaging, emitted in 1000-1400 nm after responding to ·OH

Novel multitarget Fasudil derivative, inducing the NRF2 signature, promoting the expression of the antioxidant response enzymes HO-1 and NQO1, via a KEAP1-dependent mechanism

Novel potent and selective inhibitor of Schistosoma mansoni dihydroorotate dehydrogenase (SmDHODH)

Novel selective r(CGG)exp probe, improving pre-mRNA splicing defects, inhibiting formation of nuclear inclusions and RANT in a FXTAS cellular model

Natural antioxidant and anti-cancer agent, blocking the MAPK/NF-κB and activating Nrf2/HO-1

Novel anticancer agent, inhibiting lung cancer cell proliferation via a PKCa and ERK1/2 dependent mechanism

Natural antagonist of serotonergic receptors and inhibitor of CDK5/p25 and GSK-3ß

Novel analogue of combretastatin A-4, enhancing connexin43 expression

Novel potent and selective inhibitor of fat mass obesity-associated protein (FTO), being selectively over alkylation repair homologue 5 (ALKBH5), another DNA/RNA demethylase

Novel potent and selective inhibitor of human DNA polymerase kappa (hpol κ)

Selective kynurenine-3-hydroxylase inhibitor

Antibiotic enhancer against resistant Gram-negative bacteria

Antibiotic enhancer against resistant Gram-negative bacteria

Antibiotic enhancer against resistant Gram-negative bacteria

Novel antagonist of IAP (inhibitor of apoptosis protein)