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

Negative control for GSK4027

Novel specific inhibitor of polo-like kinase 1 (PLK-1), inducing cell death by causing cell cycle arrest at G2/M phase by competing with the ATP binding site of PLK-1 thus leading to apoptosis

Novel, Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitor

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

Novel highly potent and selective non-peptide oxytocin receptor antagonist

Novel potent EchA6 inhibitor

Novel inhibitor of the Ribonuclease H Activity of HIV-1 Reverse Transcriptase

Potent polo-like kinase 1 (PLK1) inhibitor

Novel ATM inhibitor with cancer cell specific radiosensitization activity

Novel, soluble, permeable, and selective BRD7/9 inhibitor

Novel PCAF/GCN5 degrader, modulating PCAF/GCN5 immune cell function through a PROTAC approach

Negative control for GSK699

Novel stabilizer of Zα 1 -antitrypsin, blocking Zα 1 -antitrypsin polymerisation in vitro, reducing intracellular polymerisation and increasing the secretion of Zα 1 -antitrypsin threefold in an iPSC model of disease

Novel potent inhibitor of EchA6

Novel Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitor

Negative control for GSK789

Novel potent and selective BET pan-BD2 inhibitor

Novel agonist of the orphan nuclear receptors steroidogenic factor-1 (SF-1, NR5A1) and liver receptor homologue-1 (LRH-1, NR5A2)

Selective glucocorticoid receptor agonist (SEGRA)

Negative control for GSK8814

Highly potent, selective, SAM-competitive, and cell-active EZH2 inhibitor

Antimalarial

Negative control for GSK073

Novel potent protein kinase C-related kinase 1 (PRK1) inhibitor with IC50 of 40±8.7 nM)

Novel potent inhibitor of bacterial type IIA topoisomerases

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

Potent inhibitor of bacterial type IIA topoisomerases

Novel potent transrepression-selective liver X receptor modulator with anti-inflammatory activity

Negative control as an inactive IDH1 inhibitor

Next-generation NSAID-like γ-secretase modulator (GSM) with improved in vitro potency and brain penetration, effectively lowering Aβ42 production in cells and in amyloid precursor protein transgenic mice

Novel hepatitis B surface antigen (HBsAg) inhibitor for the treatment of hepatitis B virus infection

Novel potent histamine H3 receptor antagonist

Novel broad-spectrum inhibitor of coronavirus and enterovirus replication, targeting the main protease (Mpro or 3CLpro)

First-In-Class Antagonist against the Adrenomedullin-2 (AM2) Receptor

Inhibitor of vasoconstrictor responses to sympathetic nerve stimulation, potentiating the actions of adrenaline and noradrenaline, increasing the blood glucose concentration and decreasing the appetite

Novel inhibitor of the activation of nuclear factor (NF)-κB signaling in bone marrow-derived dendritic cells, significantly inhibiting LPS-induced IL-12p40 and TNF-α gene expression, IκBα degradation, and NF-κB DNA binding activity in BMDCs, attenuating c

Acyl-CoA, inhibiting cholesterol acyltransferase

Natural inhibitor of 3C-like protease (3CLpro), targeting SARS-CoV-2 3CLpro, SARS-CoV 3CLpro and MERS-CoV 3CLpro

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)