Page last updated: 2024-11-13

CCT251545

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Description

CCT251545: a Wnt signaling inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

CCT251545 : A 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. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID77050682
CHEMBL ID3408213
CHEBI ID143114
SCHEMBL ID17113515

Synonyms (32)

Synonym
8-[3-chloro-5-[4-(1-methylpyrazol-4-yl)phenyl]pyridin-4-yl]-2,8-diazaspiro[4.5]decan-1-one
8-[3-chloro-5-[4-(1-methyl-1h-pyrazole-4-yl)phenyl]-4-pyridyl]-2,8-diazaspiro[4.5]decane-1-one
CHEBI:143114
1661839-45-7
cct251545
8-{3-chloro-5-[4-(1-methyl-1h-pyrazol-4-yl)phenyl]pyridin-4-yl}-2,8-diazaspiro[4.5]decan-1-one
S7981
8-(3-chloro-5-(4-(1-methyl-1h-pyrazol-4-yl)phenyl)pyridin-4-yl)-2,8-diazaspiro[4.5]decan-1-one
4tv ,
CS-5359
HY-12681
AC-31717
SCHEMBL17113515
gtpl8945
bdbm50073190
CHEMBL3408213 ,
AKOS030526639
BCP17378
cct-251545;cct 251545
EX-A2539
Q27075796
AMY16654
nsc-784591
nsc784591
cct 251545
MS-27406
cct-251545
2,8-diazaspiro[4.5]decan-1-one, 8-[3-chloro-5-[4-(1-methyl-1h-pyrazol-4-yl)phenyl]-4-pyridinyl]-
A902314
8-{3-chloro-5-[4-(1-methyl-1h-pyrazol-4-yl)-phenyl]-
pyridin-4-yl}-2,8-diaza-spiro[4.5]decan-1-one
8-{3-chloro-5-[4-(1-methyl-1h-pyrazol-4-yl)-phenyl]- pyridin-4-yl}-2,8-diaza-spiro[4.5]decan-1-one

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" Here we report the discovery of 109 (CCT251921), a potent, selective, and orally bioavailable inhibitor of CDK8 with equipotent affinity for CDK19."( Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
Adeniji-Popoola, O; Blagg, J; Burke, R; Busch, M; Calderini, M; Clarke, PA; Crumpler, S; Czodrowski, P; Dale, T; de Haven Brandon, A; Eccles, SA; Esdar, C; Mallinger, A; Musil, D; Ortiz-Ruiz, MJ; Poeschke, O; Raynaud, FI; Rink, C; Rohdich, F; Schiemann, K; Schneider, R; Schwarz, D; Stieber, F; Stubbs, M; Thai, C; Valenti, M; Wienke, D; Workman, P, 2016
)
0.43
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
Wnt signalling inhibitorA 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.
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
EC 2.7.11.22 (cyclin-dependent kinase) inhibitorAn EC 2.7.11.* (protein-serine/threonine kinase) inhibitor that interferes with the action of cyclin-dependent kinase (EC 2.7.11.22).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
chloropyridineCompounds containing a pyridine nucleus substituted with one or more chlorine atoms.
pyrazoles
azaspiro compoundAn azaspiro compound is a spiro compound in which at least one of the cyclic components is a nitrogen heterocyle.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (13)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency0.03700.00529.466132.9993AID1347411
Interferon betaHomo sapiens (human)Potency0.03700.00339.158239.8107AID1347411
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Poly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)IC50 (µMol)10.00000.00190.62935.0000AID1198325
Cyclin-CHomo sapiens (human)IC50 (µMol)0.00600.00500.67925.9000AID1295765
Cyclin-CHomo sapiens (human)Ki0.00900.00900.00900.0090AID1731776
Cyclin-dependent kinase 8Homo sapiens (human)IC50 (µMol)0.01690.00341.02755.9000AID1295749; AID1295764; AID1852092
Cyclin-dependent kinase 8Homo sapiens (human)Ki0.00900.00900.00900.0090AID1731776
Glycogen synthase kinase-3 alphaHomo sapiens (human)IC50 (µMol)0.46200.00101.22499.1000AID1198336
Glycogen synthase kinase-3 alphaHomo sapiens (human)Ki0.23100.00910.34681.6000AID1731798
Glycogen synthase kinase-3 betaHomo sapiens (human)IC50 (µMol)0.69000.00060.801310.0000AID1198337
Glycogen synthase kinase-3 betaHomo sapiens (human)Ki0.34500.00200.36681.6000AID1731799
Protein Wnt-3aHomo sapiens (human)IC50 (µMol)0.00700.00350.02950.0780AID1198342
Protein kinase C theta typeHomo sapiens (human)Ki0.06100.00150.65036.0000AID1731800
Cyclin-dependent kinase 19Homo sapiens (human)IC50 (µMol)0.00550.00500.40852.2000AID1295749; AID1295765
Poly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)IC50 (µMol)15.00000.00210.67505.1300AID1198326
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cyclin-dependent kinase 19Mus musculus (house mouse)EC50 (µMol)0.02000.02000.02000.0200AID1733982
Cyclin-dependent kinase 8Mus musculus (house mouse)EC50 (µMol)0.02000.02000.71001.4000AID1733982
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (224)

Processvia Protein(s)Taxonomy
peptidyl-serine phosphorylationPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
peptidyl-threonine phosphorylationPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
protein polyubiquitinationPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
mitotic spindle organizationPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
protein transportPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
Wnt signaling pathwayPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
regulation of telomere maintenance via telomerasePoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
positive regulation of telomere maintenance via telomerasePoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
mRNA transportPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
spindle assemblyPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
cell divisionPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
positive regulation of telomerase activityPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
protein localization to chromosome, telomeric regionPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
protein poly-ADP-ribosylationPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
protein auto-ADP-ribosylationPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
positive regulation of canonical Wnt signaling pathwayPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
positive regulation of telomere cappingPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
negative regulation of telomere maintenance via telomere lengtheningPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
negative regulation of telomeric DNA bindingPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
negative regulation of maintenance of mitotic sister chromatid cohesion, telomericPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
G0 to G1 transitionCyclin-CHomo sapiens (human)
negative regulation of Notch signaling pathwayCyclin-CHomo sapiens (human)
positive regulation of transcription by RNA polymerase IICyclin-CHomo sapiens (human)
protein ubiquitinationCyclin-dependent kinase 8Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICyclin-dependent kinase 8Homo sapiens (human)
regulation of cell cycleCyclin-dependent kinase 8Homo sapiens (human)
negative regulation of triglyceride metabolic processCyclin-dependent kinase 8Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 8Homo sapiens (human)
regulation of systemic arterial blood pressureGlycogen synthase kinase-3 alphaHomo sapiens (human)
cardiac left ventricle morphogenesisGlycogen synthase kinase-3 alphaHomo sapiens (human)
glycogen metabolic processGlycogen synthase kinase-3 alphaHomo sapiens (human)
protein phosphorylationGlycogen synthase kinase-3 alphaHomo sapiens (human)
dopamine receptor signaling pathwayGlycogen synthase kinase-3 alphaHomo sapiens (human)
nervous system developmentGlycogen synthase kinase-3 alphaHomo sapiens (human)
insulin receptor signaling pathwayGlycogen synthase kinase-3 alphaHomo sapiens (human)
positive regulation of autophagyGlycogen synthase kinase-3 alphaHomo sapiens (human)
positive regulation of gene expressionGlycogen synthase kinase-3 alphaHomo sapiens (human)
positive regulation of peptidyl-threonine phosphorylationGlycogen synthase kinase-3 alphaHomo sapiens (human)
negative regulation of UDP-glucose catabolic processGlycogen synthase kinase-3 alphaHomo sapiens (human)
Wnt signaling pathwayGlycogen synthase kinase-3 alphaHomo sapiens (human)
cell migrationGlycogen synthase kinase-3 alphaHomo sapiens (human)
peptidyl-threonine phosphorylationGlycogen synthase kinase-3 alphaHomo sapiens (human)
viral protein processingGlycogen synthase kinase-3 alphaHomo sapiens (human)
positive regulation of protein ubiquitinationGlycogen synthase kinase-3 alphaHomo sapiens (human)
negative regulation of TOR signalingGlycogen synthase kinase-3 alphaHomo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processGlycogen synthase kinase-3 alphaHomo sapiens (human)
cellular response to insulin stimulusGlycogen synthase kinase-3 alphaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationGlycogen synthase kinase-3 alphaHomo sapiens (human)
cellular response to interleukin-3Glycogen synthase kinase-3 alphaHomo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processGlycogen synthase kinase-3 alphaHomo sapiens (human)
negative regulation of glycogen biosynthetic processGlycogen synthase kinase-3 alphaHomo sapiens (human)
positive regulation of protein catabolic processGlycogen synthase kinase-3 alphaHomo sapiens (human)
positive regulation of heart contractionGlycogen synthase kinase-3 alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIGlycogen synthase kinase-3 alphaHomo sapiens (human)
negative regulation of glucose importGlycogen synthase kinase-3 alphaHomo sapiens (human)
negative regulation of insulin receptor signaling pathwayGlycogen synthase kinase-3 alphaHomo sapiens (human)
excitatory postsynaptic potentialGlycogen synthase kinase-3 alphaHomo sapiens (human)
negative regulation of cell growth involved in cardiac muscle cell developmentGlycogen synthase kinase-3 alphaHomo sapiens (human)
cellular response to lithium ionGlycogen synthase kinase-3 alphaHomo sapiens (human)
cellular response to glucocorticoid stimulusGlycogen synthase kinase-3 alphaHomo sapiens (human)
positive regulation of adenylate cyclase-activating adrenergic receptor signaling pathwayGlycogen synthase kinase-3 alphaHomo sapiens (human)
negative regulation of canonical Wnt signaling pathwayGlycogen synthase kinase-3 alphaHomo sapiens (human)
extrinsic apoptotic signaling pathwayGlycogen synthase kinase-3 alphaHomo sapiens (human)
extrinsic apoptotic signaling pathway in absence of ligandGlycogen synthase kinase-3 alphaHomo sapiens (human)
positive regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwayGlycogen synthase kinase-3 alphaHomo sapiens (human)
autosome genomic imprintingGlycogen synthase kinase-3 alphaHomo sapiens (human)
positive regulation of mitochondrial outer membrane permeabilization involved in apoptotic signaling pathwayGlycogen synthase kinase-3 alphaHomo sapiens (human)
regulation of mitophagyGlycogen synthase kinase-3 alphaHomo sapiens (human)
positive regulation of amyloid-beta formationGlycogen synthase kinase-3 alphaHomo sapiens (human)
positive regulation of protein targeting to mitochondrionGlycogen synthase kinase-3 alphaHomo sapiens (human)
negative regulation of glycogen synthase activity, transferring glucose-1-phosphateGlycogen synthase kinase-3 alphaHomo sapiens (human)
negative regulation of type B pancreatic cell developmentGlycogen synthase kinase-3 alphaHomo sapiens (human)
negative regulation of glycogen (starch) synthase activityGlycogen synthase kinase-3 alphaHomo sapiens (human)
positive regulation of glycogen (starch) synthase activityGlycogen synthase kinase-3 alphaHomo sapiens (human)
cell differentiationGlycogen synthase kinase-3 alphaHomo sapiens (human)
regulation of microtubule cytoskeleton organizationGlycogen synthase kinase-3 alphaHomo sapiens (human)
regulation of neuron projection developmentGlycogen synthase kinase-3 alphaHomo sapiens (human)
positive regulation of gene expressionGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of gene expressionGlycogen synthase kinase-3 betaHomo sapiens (human)
ER overload responseGlycogen synthase kinase-3 betaHomo sapiens (human)
peptidyl-serine phosphorylationGlycogen synthase kinase-3 betaHomo sapiens (human)
intracellular signal transductionGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of apoptotic processGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of protein export from nucleusGlycogen synthase kinase-3 betaHomo sapiens (human)
epithelial to mesenchymal transitionGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of cell-matrix adhesionGlycogen synthase kinase-3 betaHomo sapiens (human)
glycogen metabolic processGlycogen synthase kinase-3 betaHomo sapiens (human)
protein phosphorylationGlycogen synthase kinase-3 betaHomo sapiens (human)
mitochondrion organizationGlycogen synthase kinase-3 betaHomo sapiens (human)
dopamine receptor signaling pathwayGlycogen synthase kinase-3 betaHomo sapiens (human)
circadian rhythmGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of autophagyGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of gene expressionGlycogen synthase kinase-3 betaHomo sapiens (human)
peptidyl-serine phosphorylationGlycogen synthase kinase-3 betaHomo sapiens (human)
peptidyl-threonine phosphorylationGlycogen synthase kinase-3 betaHomo sapiens (human)
viral protein processingGlycogen synthase kinase-3 betaHomo sapiens (human)
hippocampus developmentGlycogen synthase kinase-3 betaHomo sapiens (human)
establishment of cell polarityGlycogen synthase kinase-3 betaHomo sapiens (human)
maintenance of cell polarityGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of cell migrationGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of axon extensionGlycogen synthase kinase-3 betaHomo sapiens (human)
neuron projection developmentGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of protein-containing complex assemblyGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of protein-containing complex assemblyGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of protein ubiquitinationGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of protein bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of phosphoprotein phosphatase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of microtubule-based processGlycogen synthase kinase-3 betaHomo sapiens (human)
intracellular signal transductionGlycogen synthase kinase-3 betaHomo sapiens (human)
cellular response to interleukin-3Glycogen synthase kinase-3 betaHomo sapiens (human)
regulation of circadian rhythmGlycogen synthase kinase-3 betaHomo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of GTPase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of cell differentiationGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of osteoblast differentiationGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of glycogen biosynthetic processGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of cilium assemblyGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of protein catabolic processGlycogen synthase kinase-3 betaHomo sapiens (human)
protein autophosphorylationGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of protein export from nucleusGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of dendrite morphogenesisGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of axonogenesisGlycogen synthase kinase-3 betaHomo sapiens (human)
canonical Wnt signaling pathwayGlycogen synthase kinase-3 betaHomo sapiens (human)
excitatory postsynaptic potentialGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of microtubule cytoskeleton organizationGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of calcineurin-NFAT signaling cascadeGlycogen synthase kinase-3 betaHomo sapiens (human)
superior temporal gyrus developmentGlycogen synthase kinase-3 betaHomo sapiens (human)
cellular response to retinoic acidGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of canonical Wnt signaling pathwayGlycogen synthase kinase-3 betaHomo sapiens (human)
extrinsic apoptotic signaling pathwayGlycogen synthase kinase-3 betaHomo sapiens (human)
extrinsic apoptotic signaling pathway in absence of ligandGlycogen synthase kinase-3 betaHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionGlycogen synthase kinase-3 betaHomo sapiens (human)
neuron projection organizationGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of microtubule anchoring at centrosomeGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of cellular response to heatGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of protein localization to nucleusGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of long-term synaptic potentiationGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of mitochondrial outer membrane permeabilization involved in apoptotic signaling pathwayGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of protein acetylationGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway via death domain receptorsGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of protein localization to ciliumGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of dopaminergic neuron differentiationGlycogen synthase kinase-3 betaHomo sapiens (human)
cellular response to amyloid-betaGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of protein localization to centrosomeGlycogen synthase kinase-3 betaHomo sapiens (human)
beta-catenin destruction complex disassemblyGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of type B pancreatic cell developmentGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of glycogen (starch) synthase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of mesenchymal stem cell differentiationGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of TOR signalingGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of neuron projection developmentGlycogen synthase kinase-3 betaHomo sapiens (human)
cell differentiationGlycogen synthase kinase-3 betaHomo sapiens (human)
insulin receptor signaling pathwayGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of cardiac muscle cell differentiationProtein Wnt-3aHomo sapiens (human)
osteoblast differentiationProtein Wnt-3aHomo sapiens (human)
in utero embryonic developmentProtein Wnt-3aHomo sapiens (human)
positive regulation of cytokine productionProtein Wnt-3aHomo sapiens (human)
positive regulation of protein phosphorylationProtein Wnt-3aHomo sapiens (human)
heart loopingProtein Wnt-3aHomo sapiens (human)
positive regulation of receptor internalizationProtein Wnt-3aHomo sapiens (human)
transcription by RNA polymerase IIProtein Wnt-3aHomo sapiens (human)
axon guidanceProtein Wnt-3aHomo sapiens (human)
heart developmentProtein Wnt-3aHomo sapiens (human)
protein localizationProtein Wnt-3aHomo sapiens (human)
cell population proliferationProtein Wnt-3aHomo sapiens (human)
positive regulation of cell population proliferationProtein Wnt-3aHomo sapiens (human)
COP9 signalosome assemblyProtein Wnt-3aHomo sapiens (human)
positive regulation of gene expressionProtein Wnt-3aHomo sapiens (human)
negative regulation of neuron projection developmentProtein Wnt-3aHomo sapiens (human)
spinal cord association neuron differentiationProtein Wnt-3aHomo sapiens (human)
hippocampus developmentProtein Wnt-3aHomo sapiens (human)
cell proliferation in forebrainProtein Wnt-3aHomo sapiens (human)
Wnt signaling pathway involved in forebrain neuroblast divisionProtein Wnt-3aHomo sapiens (human)
dorsal/ventral neural tube patterningProtein Wnt-3aHomo sapiens (human)
hemopoiesisProtein Wnt-3aHomo sapiens (human)
neuron differentiationProtein Wnt-3aHomo sapiens (human)
extracellular matrix organizationProtein Wnt-3aHomo sapiens (human)
mammary gland developmentProtein Wnt-3aHomo sapiens (human)
positive regulation of B cell proliferationProtein Wnt-3aHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationProtein Wnt-3aHomo sapiens (human)
cell proliferation in midbrainProtein Wnt-3aHomo sapiens (human)
non-canonical Wnt signaling pathwayProtein Wnt-3aHomo sapiens (human)
skeletal muscle cell differentiationProtein Wnt-3aHomo sapiens (human)
post-anal tail morphogenesisProtein Wnt-3aHomo sapiens (human)
synaptic vesicle recyclingProtein Wnt-3aHomo sapiens (human)
B cell proliferationProtein Wnt-3aHomo sapiens (human)
inner ear morphogenesisProtein Wnt-3aHomo sapiens (human)
fat cell differentiationProtein Wnt-3aHomo sapiens (human)
myoblast differentiationProtein Wnt-3aHomo sapiens (human)
negative regulation of fat cell differentiationProtein Wnt-3aHomo sapiens (human)
positive regulation of DNA-templated transcriptionProtein Wnt-3aHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIProtein Wnt-3aHomo sapiens (human)
somatic stem cell divisionProtein Wnt-3aHomo sapiens (human)
positive regulation of mesodermal cell fate specificationProtein Wnt-3aHomo sapiens (human)
paraxial mesodermal cell fate commitmentProtein Wnt-3aHomo sapiens (human)
positive regulation of skeletal muscle tissue developmentProtein Wnt-3aHomo sapiens (human)
positive regulation of collateral sprouting in absence of injuryProtein Wnt-3aHomo sapiens (human)
negative regulation of axon extension involved in axon guidanceProtein Wnt-3aHomo sapiens (human)
negative regulation of neurogenesisProtein Wnt-3aHomo sapiens (human)
modulation of chemical synaptic transmissionProtein Wnt-3aHomo sapiens (human)
regulation of synapse organizationProtein Wnt-3aHomo sapiens (human)
canonical Wnt signaling pathwayProtein Wnt-3aHomo sapiens (human)
cardiac muscle cell fate commitmentProtein Wnt-3aHomo sapiens (human)
positive regulation of dermatome developmentProtein Wnt-3aHomo sapiens (human)
secondary palate developmentProtein Wnt-3aHomo sapiens (human)
regulation of microtubule cytoskeleton organizationProtein Wnt-3aHomo sapiens (human)
platelet aggregationProtein Wnt-3aHomo sapiens (human)
cellular response to retinoic acidProtein Wnt-3aHomo sapiens (human)
axis elongation involved in somitogenesisProtein Wnt-3aHomo sapiens (human)
positive regulation of canonical Wnt signaling pathwayProtein Wnt-3aHomo sapiens (human)
calcium ion transmembrane transport via low voltage-gated calcium channelProtein Wnt-3aHomo sapiens (human)
presynapse assemblyProtein Wnt-3aHomo sapiens (human)
positive regulation of protein localization to plasma membraneProtein Wnt-3aHomo sapiens (human)
negative regulation of dopaminergic neuron differentiationProtein Wnt-3aHomo sapiens (human)
midbrain dopaminergic neuron differentiationProtein Wnt-3aHomo sapiens (human)
regulation of postsynapse to nucleus signaling pathwayProtein Wnt-3aHomo sapiens (human)
regulation of presynapse assemblyProtein Wnt-3aHomo sapiens (human)
positive regulation of cell-cell adhesion mediated by cadherinProtein Wnt-3aHomo sapiens (human)
positive regulation of neural precursor cell proliferationProtein Wnt-3aHomo sapiens (human)
positive regulation of hepatocyte proliferationProtein Wnt-3aHomo sapiens (human)
cell fate commitmentProtein Wnt-3aHomo sapiens (human)
regulation of cell growthProtein kinase C theta typeHomo sapiens (human)
regulation of DNA-templated transcriptionProtein kinase C theta typeHomo sapiens (human)
protein phosphorylationProtein kinase C theta typeHomo sapiens (human)
membrane protein ectodomain proteolysisProtein kinase C theta typeHomo sapiens (human)
inflammatory responseProtein kinase C theta typeHomo sapiens (human)
axon guidanceProtein kinase C theta typeHomo sapiens (human)
positive regulation of telomere maintenance via telomeraseProtein kinase C theta typeHomo sapiens (human)
positive regulation of interleukin-17 productionProtein kinase C theta typeHomo sapiens (human)
positive regulation of interleukin-2 productionProtein kinase C theta typeHomo sapiens (human)
positive regulation of interleukin-4 productionProtein kinase C theta typeHomo sapiens (human)
intracellular signal transductionProtein kinase C theta typeHomo sapiens (human)
CD4-positive, alpha-beta T cell proliferationProtein kinase C theta typeHomo sapiens (human)
Fc-epsilon receptor signaling pathwayProtein kinase C theta typeHomo sapiens (human)
negative regulation of insulin receptor signaling pathwayProtein kinase C theta typeHomo sapiens (human)
positive regulation of T cell activationProtein kinase C theta typeHomo sapiens (human)
positive regulation of NF-kappaB transcription factor activityProtein kinase C theta typeHomo sapiens (human)
positive regulation of telomerase activityProtein kinase C theta typeHomo sapiens (human)
cell chemotaxisProtein kinase C theta typeHomo sapiens (human)
negative regulation of T cell apoptotic processProtein kinase C theta typeHomo sapiens (human)
regulation of platelet aggregationProtein kinase C theta typeHomo sapiens (human)
positive regulation of telomere cappingProtein kinase C theta typeHomo sapiens (human)
positive regulation of T-helper 17 type immune responseProtein kinase C theta typeHomo sapiens (human)
positive regulation of CD4-positive, alpha-beta T cell proliferationProtein kinase C theta typeHomo sapiens (human)
positive regulation of T-helper 2 cell activationProtein kinase C theta typeHomo sapiens (human)
peptidyl-serine phosphorylationProtein kinase C theta typeHomo sapiens (human)
positive regulation of apoptotic processCyclin-dependent kinase 19Homo sapiens (human)
regulation of cell cycleCyclin-dependent kinase 19Homo sapiens (human)
cellular response to lipopolysaccharideCyclin-dependent kinase 19Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 19Homo sapiens (human)
protein polyubiquitinationPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
Wnt signaling pathwayPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
positive regulation of telomere maintenance via telomerasePoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
protein localization to chromosome, telomeric regionPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
protein poly-ADP-ribosylationPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
protein auto-ADP-ribosylationPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
positive regulation of canonical Wnt signaling pathwayPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
positive regulation of telomere cappingPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
negative regulation of telomere maintenance via telomere lengtheningPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (40)

Processvia Protein(s)Taxonomy
NAD+ ADP-ribosyltransferase activityPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
protein bindingPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
zinc ion bindingPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
nucleotidyltransferase activityPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
histone bindingPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
NAD+-protein ADP-ribosyltransferase activityPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
protein bindingCyclin-CHomo sapiens (human)
identical protein bindingCyclin-CHomo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityCyclin-CHomo sapiens (human)
protein kinase activityCyclin-dependent kinase 8Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 8Homo sapiens (human)
protein bindingCyclin-dependent kinase 8Homo sapiens (human)
ATP bindingCyclin-dependent kinase 8Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityCyclin-dependent kinase 8Homo sapiens (human)
ubiquitin protein ligase activityCyclin-dependent kinase 8Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 8Homo sapiens (human)
protein serine/threonine kinase activityCyclin-dependent kinase 8Homo sapiens (human)
protein serine/threonine kinase activityGlycogen synthase kinase-3 alphaHomo sapiens (human)
signaling receptor bindingGlycogen synthase kinase-3 alphaHomo sapiens (human)
protein bindingGlycogen synthase kinase-3 alphaHomo sapiens (human)
ATP bindingGlycogen synthase kinase-3 alphaHomo sapiens (human)
protein kinase A catalytic subunit bindingGlycogen synthase kinase-3 alphaHomo sapiens (human)
tau protein bindingGlycogen synthase kinase-3 alphaHomo sapiens (human)
tau-protein kinase activityGlycogen synthase kinase-3 alphaHomo sapiens (human)
protein serine kinase activityGlycogen synthase kinase-3 alphaHomo sapiens (human)
protease bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
p53 bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
protein kinase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
protein serine/threonine kinase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
protein bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
ATP bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
beta-catenin bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
kinase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
protein kinase bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
ubiquitin protein ligase bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
protein kinase A catalytic subunit bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
dynactin bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
tau protein bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
tau-protein kinase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
NF-kappaB bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
protein serine kinase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
transcription coactivator activityProtein Wnt-3aHomo sapiens (human)
signaling receptor bindingProtein Wnt-3aHomo sapiens (human)
protein bindingProtein Wnt-3aHomo sapiens (human)
protein domain specific bindingProtein Wnt-3aHomo sapiens (human)
co-receptor bindingProtein Wnt-3aHomo sapiens (human)
identical protein bindingProtein Wnt-3aHomo sapiens (human)
receptor ligand activityProtein Wnt-3aHomo sapiens (human)
cytokine activityProtein Wnt-3aHomo sapiens (human)
frizzled bindingProtein Wnt-3aHomo sapiens (human)
protein kinase activityProtein kinase C theta typeHomo sapiens (human)
protein serine/threonine kinase activityProtein kinase C theta typeHomo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activityProtein kinase C theta typeHomo sapiens (human)
protein bindingProtein kinase C theta typeHomo sapiens (human)
ATP bindingProtein kinase C theta typeHomo sapiens (human)
metal ion bindingProtein kinase C theta typeHomo sapiens (human)
protein serine kinase activityProtein kinase C theta typeHomo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 19Homo sapiens (human)
ATP bindingCyclin-dependent kinase 19Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 19Homo sapiens (human)
protein serine/threonine kinase activityCyclin-dependent kinase 19Homo sapiens (human)
NAD+ ADP-ribosyltransferase activityPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
protein bindingPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
nucleotidyltransferase activityPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
enzyme bindingPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
metal ion bindingPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
NAD+-protein ADP-ribosyltransferase activityPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (45)

Processvia Protein(s)Taxonomy
Golgi membranePoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
pericentriolar materialPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
chromosome, telomeric regionPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
nucleoplasmPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
Golgi apparatusPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
cytosolPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
nuclear bodyPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
nuclear membranePoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
mitotic spindle polePoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
nuclear porePoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
nucleusPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
cytoplasmPoly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-CHomo sapiens (human)
nucleoplasmCyclin-CHomo sapiens (human)
CKM complexCyclin-CHomo sapiens (human)
nucleusCyclin-CHomo sapiens (human)
mediator complexCyclin-CHomo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-dependent kinase 8Homo sapiens (human)
nucleusCyclin-dependent kinase 8Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 8Homo sapiens (human)
nucleolusCyclin-dependent kinase 8Homo sapiens (human)
CKM complexCyclin-dependent kinase 8Homo sapiens (human)
ubiquitin ligase complexCyclin-dependent kinase 8Homo sapiens (human)
mediator complexCyclin-dependent kinase 8Homo sapiens (human)
protein-containing complexCyclin-dependent kinase 8Homo sapiens (human)
nucleusCyclin-dependent kinase 8Homo sapiens (human)
mitochondrionGlycogen synthase kinase-3 alphaHomo sapiens (human)
cytosolGlycogen synthase kinase-3 alphaHomo sapiens (human)
beta-catenin destruction complexGlycogen synthase kinase-3 alphaHomo sapiens (human)
neuronal cell bodyGlycogen synthase kinase-3 alphaHomo sapiens (human)
apical dendriteGlycogen synthase kinase-3 alphaHomo sapiens (human)
postsynapseGlycogen synthase kinase-3 alphaHomo sapiens (human)
proximal dendriteGlycogen synthase kinase-3 alphaHomo sapiens (human)
cytoplasmGlycogen synthase kinase-3 alphaHomo sapiens (human)
nucleusGlycogen synthase kinase-3 alphaHomo sapiens (human)
axonGlycogen synthase kinase-3 alphaHomo sapiens (human)
cytosolGlycogen synthase kinase-3 alphaHomo sapiens (human)
glutamatergic synapseGlycogen synthase kinase-3 betaHomo sapiens (human)
nucleusGlycogen synthase kinase-3 betaHomo sapiens (human)
nucleoplasmGlycogen synthase kinase-3 betaHomo sapiens (human)
cytoplasmGlycogen synthase kinase-3 betaHomo sapiens (human)
mitochondrionGlycogen synthase kinase-3 betaHomo sapiens (human)
centrosomeGlycogen synthase kinase-3 betaHomo sapiens (human)
cytosolGlycogen synthase kinase-3 betaHomo sapiens (human)
plasma membraneGlycogen synthase kinase-3 betaHomo sapiens (human)
axonGlycogen synthase kinase-3 betaHomo sapiens (human)
dendriteGlycogen synthase kinase-3 betaHomo sapiens (human)
beta-catenin destruction complexGlycogen synthase kinase-3 betaHomo sapiens (human)
presynapseGlycogen synthase kinase-3 betaHomo sapiens (human)
postsynapseGlycogen synthase kinase-3 betaHomo sapiens (human)
Wnt signalosomeGlycogen synthase kinase-3 betaHomo sapiens (human)
cytosolGlycogen synthase kinase-3 betaHomo sapiens (human)
axonGlycogen synthase kinase-3 betaHomo sapiens (human)
nucleusGlycogen synthase kinase-3 betaHomo sapiens (human)
cytoplasmGlycogen synthase kinase-3 betaHomo sapiens (human)
glutamatergic synapseProtein Wnt-3aHomo sapiens (human)
extracellular regionProtein Wnt-3aHomo sapiens (human)
extracellular spaceProtein Wnt-3aHomo sapiens (human)
endoplasmic reticulum lumenProtein Wnt-3aHomo sapiens (human)
Golgi lumenProtein Wnt-3aHomo sapiens (human)
plasma membraneProtein Wnt-3aHomo sapiens (human)
cell surfaceProtein Wnt-3aHomo sapiens (human)
endocytic vesicle membraneProtein Wnt-3aHomo sapiens (human)
early endosome membraneProtein Wnt-3aHomo sapiens (human)
extracellular exosomeProtein Wnt-3aHomo sapiens (human)
presynapseProtein Wnt-3aHomo sapiens (human)
Wnt-Frizzled-LRP5/6 complexProtein Wnt-3aHomo sapiens (human)
extracellular spaceProtein Wnt-3aHomo sapiens (human)
immunological synapseProtein kinase C theta typeHomo sapiens (human)
cytosolProtein kinase C theta typeHomo sapiens (human)
plasma membraneProtein kinase C theta typeHomo sapiens (human)
aggresomeProtein kinase C theta typeHomo sapiens (human)
centriolar satelliteProtein kinase C theta typeHomo sapiens (human)
nucleoplasmCyclin-dependent kinase 8Mus musculus (house mouse)
nucleoplasmCyclin-dependent kinase 19Homo sapiens (human)
cytosolCyclin-dependent kinase 19Homo sapiens (human)
perinuclear region of cytoplasmCyclin-dependent kinase 19Homo sapiens (human)
CKM complexCyclin-dependent kinase 19Homo sapiens (human)
nucleusCyclin-dependent kinase 19Homo sapiens (human)
cytosolCyclin-dependent kinase 19Homo sapiens (human)
Golgi membranePoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
pericentriolar materialPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
chromosome, telomeric regionPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
nucleusPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
nuclear envelopePoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
cytoplasmPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
cytosolPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
perinuclear region of cytoplasmPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
cytoplasmPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
nucleusPoly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (140)

Assay IDTitleYearJournalArticle
AID1731804Growth inhibition human KG-1a cells after 72 hrs by resazurin or MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1295778Inhibition of WNT pathway activation in human COLO205 cells expressing APC mutant2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1731798Inhibition of human GSKalpha S449A mutant (2 to 3nd residues) using YRRAAVPPSPSLSRHSSPHQS(p) EDEEE as substrate incubated for 40 mins in presence of [gamma-33P]-ATP by scintillation counting method2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1198348Antitumor activity against human COLO205-F1756 clone 4 cells harboring APC mutant xenografted in CrTac:NCr-Foxn1nu mouse assessed as reduction in flux normalized to tumor weight at 70 mg/kg, po bid for 9 days relative to control2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1198311Tmax in NMRI mouse at 0.2 mg/kg, iv2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1731820Growth inhibition human WI38 cells after 72 hrs by resazurin or MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1731868Toxicity in BALB/c mouse assessed as monocytes at 70 mg/kg, po administered once daily for 7 days and measured on day 15 by flow cytometric analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1295752Clearance in NMRI mouse at 0.2 mg/kg, iv and 0.5 mg/kg po by LC-MS/MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1852094Antiproliferative activity against human HT-29 cells assessed as cell viability incubated for 48 hrs by MTT assay
AID1198329Inhibition of CYP2C9 (unknown origin)2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1198328Thermodynamic aqueous solubility of the compound in phosphate buffer at pH 7.42015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1731866Toxicity in BALB/c mouse assessed as dendritic cells at 70 mg/kg, po administered once daily for 7 days and measured on day 15 by flow cytometric analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1198314Tmax in NMRI mouse at 0.5 mg/kg, po2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1198347Antitumor activity against human COLO205-F1756 clone 4 cells harboring APC mutant xenografted in CrTac:NCr-Foxn1nu mouse assessed as reduction in tumor weight at 70 mg/kg, po bid for 9 days relative to control2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1731805Growth inhibition human MOLM-13 cells after 72 hrs by resazurin or MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1295775Inhibition of WNT pathway activation in human LS174T cells expressing beta-catenin mutant2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1852096Antiproliferative activity against human CT26 cells assessed as cell viability incubated for 48 hrs by MTT assay
AID1731812Growth inhibition human COLO 205 cells after 72 hrs by resazurin or MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1198308Intrinsic clearance in human liver microsome at 1 uM preincubated for 5 mins by LC-MS analysis2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1295754Volume of distribution in NMRI mouse assessed as liver blood flow at 0.2 mg/kg, iv and 0.5 mg/kg, po by LC-MS/MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1852095Antiproliferative activity against human SW480 cells assessed as cell viability incubated for 48 hrs by MTT assay
AID1852092Inhibition of CDK8 (unknown origin) assessed as inhibition rate
AID1198349Drug uptake in tumor of human COLO205-F1756 clone 4 cells harboring APC mutant xenografted CrTac:NCr-Foxn1nu mouse at 70 mg/kg, po bid for 9 days measured after 2 to 6 hrs2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1295761Clearance in Beagle dog at 0.2 mg/kg, iv and 0.5 mg/kg, po by LC-MS/MS analysis relative to liver blood flow2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1198342Inhibition of ligand-induced WNT3A signaling in human PA-1 cells harboring TCF preincubated for 6 hrs before ligand addition measured after 24 hrs by luciferase reporter assay2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1731815Growth inhibition human PANC-1 cells after 72 hrs by resazurin or MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1198338Inhibition of WNT signaling in human 7dF3 cells assessed as inhibition of endogenous cMYC transcription up to 9.1 uM after 2 hrs by RT-PCR analysis relative to control2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1731865Toxicity in BALB/c mouse assessed as B cells at 70 mg/kg, po administered once daily for 7 days and measured on day 15 by flow cytometric analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1198331Inhibition of CYP2C8 (unknown origin)2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1198345Effect on TCF1 level in human COLO205-F1756 clone 4 cells harboring APC mutant and TCF/LEF responsive element at 350 nM by immunoblotting2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1295770Thermodynamic solubility of compound2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1198317Clearance in Wistar rat at 0.2 mg/kg, iv2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1295781Half life in NMRI mouse at 0.2 mg/kg, iv and 0.5 mg/kg, po by LC-MS/MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1295764Binding affinity to His-tagged CDK8 (unknown origin) after 60 mins by FRET based lanthascreen binding assay2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1198306Intrinsic clearance in mouse liver microsome at 1 uM preincubated for 5 mins by LC-MS analysis2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1295766Intrinsic clearance in rat microsomes preincubated for 5 mins followed by addition of 1.5 mM of NADPH measured after 5 to 30 mins by LC-MS/MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1198336Inhibition of GSK3alpha (unknown origin)2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1198321Half life in Wistar rat at 0.2 mg/kg, iv2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1198335Efflux ratio for apparent permeability in human Caco2 cells after 2 hrs by LC-MS/MS analysis2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1731802Growth inhibition human Kasumi-1 cells after 72 hrs by resazurin or MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1731803Growth inhibition human KG-1 cells after 72 hrs by resazurin or MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1731859Toxicity in BALB/c mouse assessed as vasculitis in blood vessels at 70 mg/kg, po administered once daily for 7 days and measured on day 152021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1295777Inhibition of WNT pathway activation in human SW480 cells expressing APC mutant2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1731814Growth inhibition human HT-29 cells after 72 hrs by resazurin or MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1198323AUC in Wistar rat at 0.5 mg/kg, po2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1731838Cmax in Sprague-Dawley rat at 20 mg/kg, po measured up to 24 hrs by LC-MS/MS analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1198312AUC in NMRI mouse at 0.2 mg/kg, iv2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1295769Kinetic solubility of compound2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1731811Growth inhibition human U-937 cells after 72 hrs by resazurin or MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1852097Cytotoxicity against human GES1 cells assessed as cell viability incubated for 48 hrs by MTT assay
AID1198340Inhibition of basal WNT signaling in human LS174T cells harboring beta-catenin mutant and TCF/LEF responsive element after 24 hrs by firefly luciferase reporter assay2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1198341Inhibition of basal WNT signaling in human SW480 cells harboring APC mutant2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1198316Oral bioavailability in NMRI mouse at 0.5 mg/kg2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1198350Drug uptake in plasma of human COLO205-F1756 clone 4 cells harboring APC mutant xenografted CrTac:NCr-Foxn1nu mouse at 70 mg/kg, po bid for 9 days measured after 2 to 6 hrs2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1198320AUC in Wistar rat at 0.2 mg/kg, iv2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1731864Toxicity in BALB/c mouse assessed as increase in dead splenocytes at 70 mg/kg, po administered once daily for 7 days and measured on day 15 by flow cytometric analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1295749Binding affinity to CDK8/CDK19 in human 7dF3 cells preincubated for 2 hrs followed by addition 10 uM of beta-oestradiol measured after 24 hrs by luciferase reporter gene assay2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1731819Growth inhibition human MDA-MB-453 cells after 72 hrs by resazurin or MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1198343Inhibition of WNT signaling in human RKO-F1522 cells after 24 hrs by EF1alpha promoter-driven luciferase reporter assay2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1198324Oral bioavailability in Wistar rat at 0.5 mg/kg2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1731834Half life in Sprague-Dawley rat at 5 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1295771Plasma clearance in wild type mouse2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1731818Growth inhibition human MDA-MB-231 cells after 72 hrs by resazurin or MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1731809Growth inhibition human PL-21 cells after 72 hrs by resazurin or MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1731840Half life in Sprague-Dawley rat at 20 mg/kg, po measured up to 24 hrs by LC-MS/MS analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1295759Clearance in Wistar rat at 0.2 mg/kg, iv and 0.5 mg/kg po by LC-MS/MS analysis relative to liver blood flow2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1731862Toxicity in BALB/c mouse assessed as pathological alterations in left femora at 70 mg/kg, po administered once daily for 7 days and measured on day 152021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1295750Efflux ratio in human Caco2 cells after 2 hrs by LC-MS/MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1295756Clearance in Beagle dog at 0.2 mg/kg, iv and 0.5 mg/kg, po by LC-MS/MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1295782Half life in Wistar rat at 0.2 mg/kg, iv and 0.5 mg/kg po by LC-MS/MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1295760Volume of distribution in Wistar rat assessed as liver blood flow at 0.2 mg/kg, iv and 0.5 mg/kg po by LC-MS/MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1731799Inhibition of human GSKbeta H350L mutant (2 to 3nd residues) using YRRAAVPPSPSLSRHSSPHQS(p) EDEEE as substrate incubated for 40 mins in presence of [gamma-33P]-ATP by scintillation counting method2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1731867Toxicity in BALB/c mouse assessed as granulocytes at 70 mg/kg, po administered once daily for 7 days and measured on day 15 by flow cytometric analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1198307Intrinsic clearance in rat liver microsome at 1 uM preincubated for 5 mins by LC-MS analysis2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1731832Cmax in Sprague-Dawley rat at 5 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1731872Growth inhibition human T47D cells after 72 hrs by resazurin or MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1731817Growth inhibition human MCF7 cells after 72 hrs by resazurin or MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1731777Growth inhibition of human MV4-11 cells after 72 hrs by resazurin staining based assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1295765Binding affinity to human CDK19 (1 to 502 amino acid residues)/Cyclin C (1 to 283 amino acid residues) by reporter displacement assay2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1198346Effect on TCF4 level in human COLO205-F1756 clone 4 cells harboring APC mutant and TCF/LEF responsive element at 350 nM by immunoblotting2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1295757Oral bioavailability NMRI mouse assessed as liver blood flow at 0.5 mg/kg by LC-MS/MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1731863Toxicity in BALB/c mouse assessed as pathological alterations in lung at 70 mg/kg, po administered once daily for 7 days and measured on day 152021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1295776Inhibition of WNT ligand dependent WNT pathway activation in human PA1 cells2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1198313Half life in NMRI mouse at 0.2 mg/kg, iv2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1295768Intrinsic clearance in human microsomes preincubated for 5 mins followed by addition of 1.5 mM of NADPH measured after 5 to 30 mins by LC-MS/MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1731860Toxicity in BALB/c mouse assessed as infiltration of inflammatory cells at 70 mg/kg, po administered once daily for 7 days and measured on day 152021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1731871Toxicity in BALB/c mouse assessed as increase in CD3-T cells at 70 mg/kg, po administered once daily for 7 days and measured on day 15 by flow cytometric analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1198309Clearance in NMRI mouse at 0.2 mg/kg, iv2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1731813Growth inhibition human HCT-116 cells after 72 hrs by resazurin or MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1295755Oral bioavailability in Wistar rat at 0.5 mg/kg by LC-MS/MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1295772Drug excretion in wild type mouse feces assessed as parent compound remaining level2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1295762Volume of distribution in Beagle dog at 0.2 mg/kg, iv and 0.5 mg/kg, po by LC-MS/MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1198332Inhibition of CYP3A4 (unknown origin)2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1731837Clearance in Sprague-Dawley rat at 5 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1198327Kinetic solubility of the compound in phosphate buffer at pH 7.42015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1731870Toxicity in BALB/c mouse assessed as neutrophils at 70 mg/kg, po administered once daily for 7 days and measured on day 15 by flow cytometric analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1731816Growth inhibition human A2780 cells after 72 hrs by resazurin or MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1731869Toxicity in BALB/c mouse assessed as macrophages at 70 mg/kg, po administered once daily for 7 days and measured on day 15 by flow cytometric analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1731833Tmax in Sprague-Dawley rat at 5 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1198318Volume of distribution at steady state in Wistar rat at 0.2 mg/kg, iv2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1198325Inhibition of GST-tagged TNKS1 (1023 to 1327 aa) (unknown origin) after 90 mins by HTRF assay2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1731857Toxicity in BALB/c mouse assessed as interstitial pneumonitis in lung at 70 mg/kg, po administered once daily for 7 days and measured on day 152021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1731836Volume of distribution at steady state in Sprague-Dawley rat at 5 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1198344Inhibition of basal WNT signaling in human COLO205-F1756 clone 4 cells harboring APC mutant and TCF/LEF responsive element after 24 hrs by firefly luciferase reporter assay2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1731835AUC in Sprague-Dawley rat at 5 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1295767Intrinsic clearance in mouse microsomes preincubated for 5 mins followed by addition of 1.5 mM of NADPH measured after 5 to 30 mins by LC-MS/MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1731841AUC in Sprague-Dawley rat at 20 mg/kg, po measured up to 24 hrs by LC-MS/MS analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1731858Toxicity in BALB/c mouse assessed as increase in number of alveolar macrophages at 70 mg/kg, po administered once daily for 7 days and measured on day 152021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1295784Lipophilicity, logD of the compound2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1295783Half life in Beagle dog at 0.2 mg/kg, iv and 0.5 mg/kg, po by LC-MS/MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1852091Inhibition of CDK8 (unknown origin) assessed as inhibition rate at 200 nM relative to control
AID1731842Oral bioavailability in Sprague-Dawley rat at 20 mg/kg measured up to 24 hrs by LC-MS/MS analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1198315AUC in NMRI mouse at 0.5 mg/kg, po2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1731800Inhibition of human full length PKCtheta using histone H1 as substrate incubated for 40 mins in presence of [gamma-33P]-ATP by scintillation counting method2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1731808Inhibition of CDK8 in human MV4-11 cells assessed as reduction in STAT1 phosphorylation at s727 residues at 1 to 5 times of GI50 concentration after 2 hrs by Western blot analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1731861Toxicity in BALB/c mouse assessed as destruction of vessel walls at 70 mg/kg, po administered once daily for 7 days and measured on day 152021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1295758Clearance in Wistar rat at 0.2 mg/kg, iv and 0.5 mg/kg po by LC-MS/MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1198326Inhibition of GST-tagged TNKS2 (873 to 1166 aa) (unknown origin) after 90 mins by HTRF assay2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1295773Plasma clearance in P-gp KO mouse2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1198296Inhibition of WNT signaling in human 7dF3 cells preincubated for 2 hrs before beta-estradiol addition measured after 24 hrs by luciferase reporter assay2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1731839Tmax in Sprague-Dawley rat at 20 mg/kg, po measured up to 24 hrs by LC-MS/MS analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1731807Effect on total STAT1 level in human MV4-11 cells at 1 to 5 times of GI50 concentration after 2 hrs by Western blot analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1295774Drug excretion in P-gp knock-out mouse feces assessed as parent compound remaining level2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1198339Inhibition of WNT signaling in human 7dF3 cells assessed as inhibition of endogenous cMYC transcription after 2 hrs by RT-PCR analysis2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1852093Antiproliferative activity against human HCT-116 cells assessed as cell viability incubated for 48 hrs by MTT assay
AID1295763Oral bioavailability in Beagle dog at 0.5 mg/kg by LC-MS/MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1731806Growth inhibition human NB4 cells after 72 hrs by resazurin or MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1198322Tmax in Wistar rat at 0.5 mg/kg, po2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1731810Growth inhibition human THP1 cells after 72 hrs by resazurin or MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1198337Inhibition of GSK3beta (unknown origin)2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1295753Clearance in NMRI mouse at 0.2 mg/kg, iv and 0.5 mg/kg, po by LC-MS/MS analysis relative to liver blood flow2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
AID1198319Tmax in Wistar rat at 0.2 mg/kg, iv2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1198310Volume of distribution at steady state in NMRI mouse at 0.2 mg/kg, iv2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
AID1731776Inhibition of CDK8/cyclin C (unknown origin) using RBER-IRStide as substrate incubated for 60 mins in presence of [gamma33P]ATP by scintillation counting method2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1731801Growth inhibition human HL-60 cells after 72 hrs by resazurin or MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347414qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1345673Human cyclin dependent kinase 19 (CDK8 subfamily)2015Nature chemical biology, Dec, Volume: 11, Issue:12
A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
AID1345661Human cyclin dependent kinase 8 (CDK8 subfamily)2015Nature chemical biology, Dec, Volume: 11, Issue:12
A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's4 (50.00)24.3611
2020's4 (50.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 20.07

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index20.07 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.64 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (20.07)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]