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Wnt signalling inhibitor

A substance that inhibits any of the Wnt signalling pathway, a group of signal transduction pathways made of proteins that pass signals from outside of a cell through cell surface receptors to the inside of the cell.

ChEBI ID: 78031

Members (6)

MemberDefinitionClass
6-cyclohexyl-3-furan-2-yl-(1,2,4)triazolo(3,4-b)(1,3,4)thiadiazoleA triazolothiadiazole that is [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole which is substituted at positions 3 and 6 by 2-furyl and cyclohexyl groups, respectively. A cardiomyocyte promoter and an inhibitor of Wnt/beta-catenin dependent transcriptional activity, it induces cardiac cell formation in murine stem cells and zebrafish embryos, expanding cardiac progenitor cells. A biphasic modulator of cardiogenesis, it can act as either a promotor or inhibitor of heart formation, depending on the stage of treatment.cardionogen-1
6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acidA chromanol that is 6-hydroxychromane which is substituted by a carboxy group at position 2 and by methyl groups at positions 2, 5, 7, and 8. A cell-permeable, water-soluble analogue of vitamin E, it is used as a standard for measuring the antioxidant capacity of complex mixtures.Trolox
CCT251545A chloropyridine that is 3-chloropyridine substituted by a 1-oxo-2,8-diazaspiro[4.5]decan-8-yl group and a 4-(1-methyl-1H-pyrazol-4-yl)phenyl group at positions 4 and 5, respectively. It is an orally bioavailable inhibitor of Wnt signaling (IC50 = 5 nM) and a potent and selective chemical probe for cyclin-dependent kinases CDK8 and CDK19.CCT251545
iwr-1 endoA dicarboximide having an endo bridged phthalimide structure, substituted at nitrogen by a 4-(quinolin-8-ylcarbamoyl)benzoyl group.IWR-1-endo
lgk974A carboxamide, the structure of which is that of acetamide substituted on carbon by a 2',3-dimethyl-2,4'-bipyridin-5-yl group and on nitrogen by a 5-(pyrazin-2-yl)pyridin-2-yl group. It is a highly potent, selective and orally bioavailable Porcupine inhibitor (a Wnt signalling inhibitor).LGK974
toxoflavinA pyrimidotriazine that is 1,6-dimethyl-1,5,6,7-tetrahydropyrimido[5,4-e][1,2,4]triazine with oxo groups at positions 5 and 7.toxoflavin

Research

Studies (1,635)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199028 (1.71)18.7374
1990's249 (15.23)18.2507
2000's565 (34.56)29.6817
2010's672 (41.10)24.3611
2020's121 (7.40)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials18 (1.06%)5.53%
Reviews26 (1.53%)6.00%
Case Studies0 (0.00%)4.05%
Observational1 (0.06%)0.25%
Other1,659 (97.36%)84.16%

Protein Targets (131)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency25.118911
4-(cytidine 5'-phospho)-2-C-methyl-D-erithritol kinaseArabidopsis thaliana (thale cress)Potency1.187311
Adenosine receptor A1Rattus norvegicus (Norway rat)Potency1.258911
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency26.200012
alpha-galactosidaseHomo sapiens (human)Potency31.622811
ATAD5 protein, partialHomo sapiens (human)Potency6.513111
Bloom syndrome protein isoform 1Homo sapiens (human)Potency1.122011
Caspase-1Homo sapiens (human)Potency2.366133
caspase-1 isoform alpha precursorHomo sapiens (human)Potency7.292322
Caspase-7Homo sapiens (human)Potency3.763633
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency2.903122
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency3.981111
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency5.011911
Chain A, Beta-lactamaseEscherichia coli K-12Potency15.165212
Chain A, CruzipainTrypanosoma cruziPotency1.585533
Chain A, Ferritin light chainEquus caballus (horse)Potency28.183811
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency100.000011
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency44.668411
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency5.417233
chromobox protein homolog 1Homo sapiens (human)Potency89.125111
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency21.317411
DNA polymerase betaHomo sapiens (human)Potency89.125111
DNA polymerase eta isoform 1Homo sapiens (human)Potency3.033122
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency5.323311
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency10.087613
EWS/FLI fusion proteinHomo sapiens (human)Potency19.924244
eyes absent homolog 2 isoform aHomo sapiens (human)Potency741.511322
fructose-bisphosphate aldolase AOryctolagus cuniculus (rabbit)Potency4.466811
galactokinaseHomo sapiens (human)Potency1.158622
gemininHomo sapiens (human)Potency7.326623
glp-1 receptor, partialHomo sapiens (human)Potency9.333612
GLS proteinHomo sapiens (human)Potency7.943311
glyceraldehyde-3-phosphate dehydrogenase isoform 1Homo sapiens (human)Potency2.511911
Guanine nucleotide-binding protein GHomo sapiens (human)Potency10.000011
Histamine H3 receptorRattus norvegicus (Norway rat)Potency3.981113
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency10.000011
huntingtin isoform 2Homo sapiens (human)Potency5.011911
IDH1Homo sapiens (human)Potency0.517411
Integrin alpha-IIbHomo sapiens (human)Potency0.794311
Integrin beta-3Homo sapiens (human)Potency0.794311
Interferon betaHomo sapiens (human)Potency0.037013
lamin isoform A-delta10Homo sapiens (human)Potency5.011911
lethal factor (plasmid)Bacillus anthracis str. A2012Potency1.258911
lethal(3)malignant brain tumor-like protein 1 isoform IHomo sapiens (human)Potency0.501212
Microtubule-associated protein tauHomo sapiens (human)Potency11.220222
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency2.238711
neuropeptide S receptor isoform AHomo sapiens (human)Potency1.503134
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency11.294712
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency1.412511
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency0.183611
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency0.527944
P53Homo sapiens (human)Potency79.432811
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency0.766711
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency0.891311
phosphoglycerate kinaseTrypanosoma brucei brucei TREU927Potency1.289322
phosphopantetheinyl transferaseBacillus subtilisPotency49.288512
plasminogen precursorMus musculus (house mouse)Potency1.122011
PPM1D proteinHomo sapiens (human)Potency0.037012
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency19.952611
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency63.095711
ras-related protein Rab-9AHomo sapiens (human)Potency1.122012
regulator of G-protein signaling 4Homo sapiens (human)Potency79.432811
serine-protein kinase ATM isoform aHomo sapiens (human)Potency0.891311
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency15.906812
Smad3Homo sapiens (human)Potency0.112211
TAR DNA-binding protein 43Homo sapiens (human)Potency26.632012
TDP1 proteinHomo sapiens (human)Potency12.546524
thioredoxin reductaseRattus norvegicus (Norway rat)Potency48.022422
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency0.100011
thyroid stimulating hormone receptorHomo sapiens (human)Potency25.118922
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency1.122011
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency1.122011
USP1 protein, partialHomo sapiens (human)Potency0.031611

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
90-kda heat shock protein beta HSP90 beta, partialHomo sapiens (human)IC501.056622
AcetylcholinesteraseHomo sapiens (human)IC502,090.700022
Adenomatous polyposis coli proteinHomo sapiens (human)Ki118.000022
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC500.000911
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC500.000911
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC500.000911
Cadherin-1Homo sapiens (human)Ki16.500022
Catenin beta-1Homo sapiens (human)IC5082.960055
Catenin beta-1Homo sapiens (human)Ki4.775044
Cathepsin BHomo sapiens (human)IC500.046722
cathepsin S isoform 1 preproproteinHomo sapiens (human)IC500.176511
Cyclin-CHomo sapiens (human)IC500.006011
Cyclin-CHomo sapiens (human)Ki0.009011
Cyclin-dependent kinase 19Homo sapiens (human)IC500.005522
Cyclin-dependent kinase 8Homo sapiens (human)IC500.016933
Cyclin-dependent kinase 8Homo sapiens (human)Ki0.009011
Dehydrogenase/reductase SDR family member 9Homo sapiens (human)IC501,000.000011
dual specificity protein phosphatase 3Homo sapiens (human)IC501.170022
dual specificity protein phosphatase 6Rattus norvegicus (Norway rat)IC502.320011
Glycogen synthase kinase-3 alphaHomo sapiens (human)IC500.462011
Glycogen synthase kinase-3 alphaHomo sapiens (human)Ki0.231011
Glycogen synthase kinase-3 betaHomo sapiens (human)IC500.690011
Glycogen synthase kinase-3 betaHomo sapiens (human)Ki0.345011
green fluorescent protein, partialAequorea victoriaIC5067.549012
heat shock protein HSP 90-alpha isoform 2Homo sapiens (human)IC501.056622
Lysine-specific demethylase 4AHomo sapiens (human)IC502.500022
Lysine-specific demethylase 4CHomo sapiens (human)IC500.520522
NAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)IC500.870011
NAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)IC5014.400011
nuclear receptor corepressor 2 isoform 2Homo sapiens (human)IC5039.841011
peroxisome proliferator-activated receptor gamma isoform 2Homo sapiens (human)IC5039.841011
photoreceptor-specific nuclear receptorHomo sapiens (human)IC5039.841011
Poly [ADP-ribose] polymerase 1Homo sapiens (human)IC5055.612544
Poly [ADP-ribose] polymerase 2Homo sapiens (human)IC5053.490055
Poly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)IC5020.973377
Poly [ADP-ribose] polymerase tankyrase-1Mus musculus (house mouse)IC500.131011
Poly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)IC5016.856589
Poly [ADP-ribose] polymerase tankyrase-2Mus musculus (house mouse)IC500.056011
Polyphenol oxidase 2Agaricus bisporusIC50200.000011
procathepsin L isoform 1 preproproteinHomo sapiens (human)IC5025.112922
Prostaglandin G/H synthase 1Homo sapiens (human)IC500.130011
Prostaglandin G/H synthase 2Homo sapiens (human)IC506.625022
Protein kinase C theta typeHomo sapiens (human)Ki0.061011
Protein Wnt-3aHomo sapiens (human)IC500.007011
Protein-serine O-palmitoleoyltransferase porcupineHomo sapiens (human)IC500.000422
Protein-serine O-palmitoleoyltransferase porcupineMus musculus (house mouse)IC500.000733
ReninHomo sapiens (human)IC500.980011
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC501,000.000011
Transcription factor 4Homo sapiens (human)IC500.800011
Transcription factor 7-like 2Homo sapiens (human)Ki46.416766
tyrosine-protein phosphatase non-receptor type 22 isoform 1Homo sapiens (human)IC501.295022
tyrosine-protein phosphatase non-receptor type 7 isoform 2Homo sapiens (human)IC501.240011
Xanthine dehydrogenase/oxidaseHomo sapiens (human)IC501,000.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Cyclin-dependent kinase 19Mus musculus (house mouse)EC500.020011
Cyclin-dependent kinase 8Mus musculus (house mouse)EC500.020011
glycogen synthase kinase-3 beta isoform 1Homo sapiens (human)EC5062.740011
mitogen-activated protein kinase kinase kinase 3 isoform 1Homo sapiens (human)EC5030.000011
mitogen-activated protein kinase kinase kinase kinase 2 isoform 1Homo sapiens (human)EC5030.000022
Poly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)EC502.500011
Poly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)EC501.350022
recombinase AMycobacterium tuberculosis H37RvEC500.054122

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
DNA repair and recombination protein RAD54-like isoform 1Homo sapiens (human)AC501.100011
jumonji domain containing 2AHomo sapiens (human)AC502.541011
jumonji domain containing 2C, partialHomo sapiens (human)AC500.541411
recombinase AMycobacterium tuberculosis H37RvIC902.870011
replicative DNA helicaseMycobacterium tuberculosis H37RvAC500.070422