Page last updated: 2024-11-13

cc214-2

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

CC214-2: an mTOR kinase inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID58298312
CHEMBL ID2348862
SCHEMBL ID135776
MeSH IDM0587414

Synonyms (11)

Synonym
bdbm50431519
CHEMBL2348862 ,
SCHEMBL135776
6-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-4-((tetrahydro-2h-pyran-4-yl)methyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one
UWUPKVZQISLSSA-UHFFFAOYSA-N
MS-26299
HY-145931
cc214-2
1228012-18-7
EX-A6902
CS-0435638

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
"We report here the discovery of a novel series of selective mTOR kinase inhibitors and the identification of CC214-2, a compound with demonstrated anti-tumor activity upon oral dosing in a PC3 prostate cancer xenograft model."( Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
Bisonette, RR; Fultz, KE; Gamez, JC; Harris, R; Hickman, M; Khambatta, G; Lee, BG; Leisten, J; Mortensen, DS; Narla, RK; Parnes, JS; Peng, S; Perrin-Ninkovic, SM; Sankar, S; Sapienza, J; Shevlin, G; Whitefield, B, 2013
)
0.86
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (7)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Macrophage colony-stimulating factor 1 receptorHomo sapiens (human)IC50 (µMol)2.70000.00060.56765.5450AID738006
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)IC50 (µMol)30.00000.00000.734010.0000AID1230505; AID1916702; AID738013
Serine/threonine-protein kinase mTORHomo sapiens (human)IC50 (µMol)0.25640.00000.857510.0000AID1230508; AID1230520; AID1916668; AID1916669; AID1916683; AID738012; AID738014
Rapamycin-insensitive companion of mTORHomo sapiens (human)IC50 (µMol)0.38600.00020.05920.3860AID1916669
Regulatory-associated protein of mTORHomo sapiens (human)IC50 (µMol)0.29400.00000.11390.6600AID1230520; AID1916668; AID738012
Target of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)IC50 (µMol)0.38600.00020.05920.3860AID1916669
Target of rapamycin complex subunit LST8Homo sapiens (human)IC50 (µMol)0.31700.00000.09630.6600AID1230520; AID1916668; AID1916669; AID738012
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (188)

Processvia Protein(s)Taxonomy
positive regulation of macrophage chemotaxisMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
positive regulation of macrophage proliferationMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
positive regulation of protein phosphorylationMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
response to ischemiaMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
inflammatory responseMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
signal transductionMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
axon guidanceMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
cell population proliferationMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
positive regulation of cell population proliferationMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
negative regulation of cell population proliferationMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
regulation of cell shapeMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
peptidyl-tyrosine phosphorylationMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
cytokine-mediated signaling pathwayMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
olfactory bulb developmentMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
forebrain neuron differentiationMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
hemopoiesisMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
monocyte differentiationMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
macrophage differentiationMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
osteoclast differentiationMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
ruffle organizationMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
positive regulation of chemokine productionMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
regulation of actin cytoskeleton organizationMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
cellular response to macrophage colony-stimulating factor stimulusMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
macrophage colony-stimulating factor signaling pathwayMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
negative regulation of apoptotic processMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
positive regulation by host of viral processMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
innate immune responseMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
regulation of bone resorptionMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
cell-cell junction maintenanceMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
protein autophosphorylationMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
mammary gland duct morphogenesisMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
positive regulation of protein tyrosine kinase activityMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
microglial cell proliferationMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
cellular response to cytokine stimulusMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
regulation of macrophage migrationMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
positive regulation of cell motilityMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
positive regulation of cell migrationMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
regulation of MAPK cascadeMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
positive regulation of kinase activityMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
multicellular organism developmentMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
phosphorylationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
angiogenesisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
liver developmentPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
regulation of protein phosphorylationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
vasculature developmentPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
glucose metabolic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phagocytosisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
epidermal growth factor receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
insulin receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of lamellipodium assemblyPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of gene expressionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to muscle inactivityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of macroautophagyPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
actin cytoskeleton organizationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
platelet activationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of actin filament depolymerizationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
T cell costimulationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of TOR signalingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cellular response to insulin stimulusPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to muscle stretchPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
vascular endothelial growth factor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
regulation of multicellular organism growthPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to L-leucinePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
anoikisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
regulation of cellular respirationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of neuron apoptotic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
endothelial cell migrationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol phosphate biosynthetic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
insulin-like growth factor receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of smooth muscle cell proliferationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
T cell receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
relaxation of cardiac musclePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cardiac muscle contractionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
adipose tissue developmentPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cellular response to glucose stimulusPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cellular response to hydrostatic pressurePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to dexamethasonePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cardiac muscle cell contractionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
energy homeostasisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
regulation of actin filament organizationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
autosome genomic imprintingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to butyratePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of protein localization to membranePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of fibroblast apoptotic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of anoikisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol-3-phosphate biosynthetic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol-mediated signalingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cell migrationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
protein destabilizationSerine/threonine-protein kinase mTORHomo sapiens (human)
protein phosphorylationSerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of macroautophagySerine/threonine-protein kinase mTORHomo sapiens (human)
phosphorylationSerine/threonine-protein kinase mTORHomo sapiens (human)
protein autophosphorylationSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of cell growthSerine/threonine-protein kinase mTORHomo sapiens (human)
T-helper 1 cell lineage commitmentSerine/threonine-protein kinase mTORHomo sapiens (human)
heart morphogenesisSerine/threonine-protein kinase mTORHomo sapiens (human)
heart valve morphogenesisSerine/threonine-protein kinase mTORHomo sapiens (human)
energy reserve metabolic processSerine/threonine-protein kinase mTORHomo sapiens (human)
'de novo' pyrimidine nucleobase biosynthetic processSerine/threonine-protein kinase mTORHomo sapiens (human)
protein phosphorylationSerine/threonine-protein kinase mTORHomo sapiens (human)
inflammatory responseSerine/threonine-protein kinase mTORHomo sapiens (human)
DNA damage responseSerine/threonine-protein kinase mTORHomo sapiens (human)
cytoskeleton organizationSerine/threonine-protein kinase mTORHomo sapiens (human)
lysosome organizationSerine/threonine-protein kinase mTORHomo sapiens (human)
germ cell developmentSerine/threonine-protein kinase mTORHomo sapiens (human)
response to nutrientSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of cell sizeSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to starvationSerine/threonine-protein kinase mTORHomo sapiens (human)
response to heatSerine/threonine-protein kinase mTORHomo sapiens (human)
post-embryonic developmentSerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of autophagySerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of lamellipodium assemblySerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of gene expressionSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of epithelial to mesenchymal transitionSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of myotube differentiationSerine/threonine-protein kinase mTORHomo sapiens (human)
macroautophagySerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of macroautophagySerine/threonine-protein kinase mTORHomo sapiens (human)
phosphorylationSerine/threonine-protein kinase mTORHomo sapiens (human)
peptidyl-serine phosphorylationSerine/threonine-protein kinase mTORHomo sapiens (human)
neuronal action potentialSerine/threonine-protein kinase mTORHomo sapiens (human)
protein catabolic processSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of cell growthSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of actin filament polymerizationSerine/threonine-protein kinase mTORHomo sapiens (human)
T cell costimulationSerine/threonine-protein kinase mTORHomo sapiens (human)
ruffle organizationSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of myelinationSerine/threonine-protein kinase mTORHomo sapiens (human)
response to nutrient levelsSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to nutrient levelsSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to nutrientSerine/threonine-protein kinase mTORHomo sapiens (human)
TOR signalingSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of phosphoprotein phosphatase activitySerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to insulin stimulusSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of actin cytoskeleton organizationSerine/threonine-protein kinase mTORHomo sapiens (human)
calcineurin-NFAT signaling cascadeSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to amino acid starvationSerine/threonine-protein kinase mTORHomo sapiens (human)
multicellular organism growthSerine/threonine-protein kinase mTORHomo sapiens (human)
TORC1 signalingSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of circadian rhythmSerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of apoptotic processSerine/threonine-protein kinase mTORHomo sapiens (human)
response to amino acidSerine/threonine-protein kinase mTORHomo sapiens (human)
anoikisSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of osteoclast differentiationSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of translationSerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of cell sizeSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of glycolytic processSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIISerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of translational initiationSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of lipid biosynthetic processSerine/threonine-protein kinase mTORHomo sapiens (human)
behavioral response to painSerine/threonine-protein kinase mTORHomo sapiens (human)
rhythmic processSerine/threonine-protein kinase mTORHomo sapiens (human)
oligodendrocyte differentiationSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of oligodendrocyte differentiationSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationSerine/threonine-protein kinase mTORHomo sapiens (human)
voluntary musculoskeletal movementSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of stress fiber assemblySerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of keratinocyte migrationSerine/threonine-protein kinase mTORHomo sapiens (human)
nucleus localizationSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionSerine/threonine-protein kinase mTORHomo sapiens (human)
cardiac muscle cell developmentSerine/threonine-protein kinase mTORHomo sapiens (human)
cardiac muscle contractionSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to methionineSerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of calcineurin-NFAT signaling cascadeSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to amino acid stimulusSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to L-leucineSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to hypoxiaSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to osmotic stressSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of membrane permeabilitySerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of cellular response to heatSerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of protein localization to nucleusSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of signal transduction by p53 class mediatorSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of transcription of nucleolar large rRNA by RNA polymerase ISerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of wound healing, spreading of epidermal cellsSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of locomotor rhythmSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of cytoplasmic translational initiationSerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of lysosome organizationSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of pentose-phosphate shuntSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to leucine starvationSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of autophagosome assemblySerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of macroautophagySerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of endothelial cell proliferationRapamycin-insensitive companion of mTORHomo sapiens (human)
cytoskeleton organizationRapamycin-insensitive companion of mTORHomo sapiens (human)
embryo development ending in birth or egg hatchingRapamycin-insensitive companion of mTORHomo sapiens (human)
regulation of gene expressionRapamycin-insensitive companion of mTORHomo sapiens (human)
peptidyl-serine phosphorylationRapamycin-insensitive companion of mTORHomo sapiens (human)
actin cytoskeleton organizationRapamycin-insensitive companion of mTORHomo sapiens (human)
positive regulation of cell growthRapamycin-insensitive companion of mTORHomo sapiens (human)
positive regulation of actin filament polymerizationRapamycin-insensitive companion of mTORHomo sapiens (human)
cellular response to nutrient levelsRapamycin-insensitive companion of mTORHomo sapiens (human)
positive regulation of TOR signalingRapamycin-insensitive companion of mTORHomo sapiens (human)
regulation of actin cytoskeleton organizationRapamycin-insensitive companion of mTORHomo sapiens (human)
regulation of peptidyl-serine phosphorylationRapamycin-insensitive companion of mTORHomo sapiens (human)
TORC2 signalingRapamycin-insensitive companion of mTORHomo sapiens (human)
negative regulation of apoptotic processRapamycin-insensitive companion of mTORHomo sapiens (human)
regulation of inflammatory responseRapamycin-insensitive companion of mTORHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationRapamycin-insensitive companion of mTORHomo sapiens (human)
regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionRapamycin-insensitive companion of mTORHomo sapiens (human)
regulation of establishment of cell polarityRapamycin-insensitive companion of mTORHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionRapamycin-insensitive companion of mTORHomo sapiens (human)
regulation of cell growthRegulatory-associated protein of mTORHomo sapiens (human)
positive regulation of endothelial cell proliferationRegulatory-associated protein of mTORHomo sapiens (human)
DNA damage responseRegulatory-associated protein of mTORHomo sapiens (human)
regulation of cell sizeRegulatory-associated protein of mTORHomo sapiens (human)
response to xenobiotic stimulusRegulatory-associated protein of mTORHomo sapiens (human)
negative regulation of autophagyRegulatory-associated protein of mTORHomo sapiens (human)
positive regulation of peptidyl-threonine phosphorylationRegulatory-associated protein of mTORHomo sapiens (human)
positive regulation of cell growthRegulatory-associated protein of mTORHomo sapiens (human)
cellular response to nutrient levelsRegulatory-associated protein of mTORHomo sapiens (human)
TOR signalingRegulatory-associated protein of mTORHomo sapiens (human)
positive regulation of TOR signalingRegulatory-associated protein of mTORHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationRegulatory-associated protein of mTORHomo sapiens (human)
social behaviorRegulatory-associated protein of mTORHomo sapiens (human)
TORC1 signalingRegulatory-associated protein of mTORHomo sapiens (human)
positive regulation of osteoclast differentiationRegulatory-associated protein of mTORHomo sapiens (human)
positive regulation of glycolytic processRegulatory-associated protein of mTORHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIIRegulatory-associated protein of mTORHomo sapiens (human)
positive regulation of lipid biosynthetic processRegulatory-associated protein of mTORHomo sapiens (human)
cellular response to amino acid stimulusRegulatory-associated protein of mTORHomo sapiens (human)
cellular response to L-leucineRegulatory-associated protein of mTORHomo sapiens (human)
cellular response to glucose stimulusRegulatory-associated protein of mTORHomo sapiens (human)
cellular response to hypoxiaRegulatory-associated protein of mTORHomo sapiens (human)
cellular response to osmotic stressRegulatory-associated protein of mTORHomo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleRegulatory-associated protein of mTORHomo sapiens (human)
positive regulation of odontoblast differentiationRegulatory-associated protein of mTORHomo sapiens (human)
positive regulation of pentose-phosphate shuntRegulatory-associated protein of mTORHomo sapiens (human)
regulation of autophagyRegulatory-associated protein of mTORHomo sapiens (human)
cellular response to starvationRegulatory-associated protein of mTORHomo sapiens (human)
cytoskeleton organizationTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
substantia nigra developmentTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
positive regulation of cell growthTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
cellular response to nutrient levelsTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
negative regulation of apoptotic processTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
negative regulation of Ras protein signal transductionTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
regulation of cellular response to oxidative stressTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
TORC2 signalingTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
DNA damage responseTarget of rapamycin complex subunit LST8Homo sapiens (human)
cytoskeleton organizationTarget of rapamycin complex subunit LST8Homo sapiens (human)
negative regulation of autophagyTarget of rapamycin complex subunit LST8Homo sapiens (human)
positive regulation of cell growthTarget of rapamycin complex subunit LST8Homo sapiens (human)
positive regulation of actin filament polymerizationTarget of rapamycin complex subunit LST8Homo sapiens (human)
cellular response to nutrient levelsTarget of rapamycin complex subunit LST8Homo sapiens (human)
positive regulation of TOR signalingTarget of rapamycin complex subunit LST8Homo sapiens (human)
regulation of actin cytoskeleton organizationTarget of rapamycin complex subunit LST8Homo sapiens (human)
TORC1 signalingTarget of rapamycin complex subunit LST8Homo sapiens (human)
negative regulation of apoptotic processTarget of rapamycin complex subunit LST8Homo sapiens (human)
positive regulation of glycolytic processTarget of rapamycin complex subunit LST8Homo sapiens (human)
positive regulation of lipid biosynthetic processTarget of rapamycin complex subunit LST8Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationTarget of rapamycin complex subunit LST8Homo sapiens (human)
cellular response to hypoxiaTarget of rapamycin complex subunit LST8Homo sapiens (human)
cellular response to osmotic stressTarget of rapamycin complex subunit LST8Homo sapiens (human)
positive regulation of pentose-phosphate shuntTarget of rapamycin complex subunit LST8Homo sapiens (human)
TOR signalingTarget of rapamycin complex subunit LST8Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (38)

Processvia Protein(s)Taxonomy
protein tyrosine kinase activityMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
macrophage colony-stimulating factor receptor activityMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
protein bindingMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
ATP bindingMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
protein phosphatase bindingMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
cytokine bindingMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
protein homodimerization activityMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
growth factor bindingMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
protein serine/threonine kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
protein bindingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
ATP bindingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
1-phosphatidylinositol-3-kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
protein kinase activator activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
insulin receptor substrate bindingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
1-phosphatidylinositol-4,5-bisphosphate 3-kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
protein serine kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
1-phosphatidylinositol-4-phosphate 3-kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
RNA polymerase III type 1 promoter sequence-specific DNA bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
RNA polymerase III type 2 promoter sequence-specific DNA bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
RNA polymerase III type 3 promoter sequence-specific DNA bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
TFIIIC-class transcription factor complex bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
protein kinase activitySerine/threonine-protein kinase mTORHomo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase mTORHomo sapiens (human)
protein bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
ATP bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
kinase activitySerine/threonine-protein kinase mTORHomo sapiens (human)
identical protein bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
ribosome bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
phosphoprotein bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase mTORHomo sapiens (human)
protein bindingRapamycin-insensitive companion of mTORHomo sapiens (human)
protein kinase bindingRapamycin-insensitive companion of mTORHomo sapiens (human)
ribosome bindingRapamycin-insensitive companion of mTORHomo sapiens (human)
protein serine/threonine kinase activator activityRapamycin-insensitive companion of mTORHomo sapiens (human)
molecular adaptor activityRapamycin-insensitive companion of mTORHomo sapiens (human)
protein bindingRegulatory-associated protein of mTORHomo sapiens (human)
protein kinase bindingRegulatory-associated protein of mTORHomo sapiens (human)
protein serine/threonine kinase inhibitor activityRegulatory-associated protein of mTORHomo sapiens (human)
protein kinase activator activityRegulatory-associated protein of mTORHomo sapiens (human)
protein-macromolecule adaptor activityRegulatory-associated protein of mTORHomo sapiens (human)
small GTPase bindingRegulatory-associated protein of mTORHomo sapiens (human)
protein-containing complex bindingRegulatory-associated protein of mTORHomo sapiens (human)
14-3-3 protein bindingRegulatory-associated protein of mTORHomo sapiens (human)
enzyme-substrate adaptor activityRegulatory-associated protein of mTORHomo sapiens (human)
protein bindingTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
phosphatidylinositol-4,5-bisphosphate bindingTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
phosphatidylinositol-3,4,5-trisphosphate bindingTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
protein kinase bindingTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
small GTPase bindingTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
phosphatidylinositol-3,4-bisphosphate bindingTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
molecular adaptor activityTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
phosphatidic acid bindingTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
phosphatidylinositol-3,5-bisphosphate bindingTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
protein bindingTarget of rapamycin complex subunit LST8Homo sapiens (human)
protein serine/threonine kinase activator activityTarget of rapamycin complex subunit LST8Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (32)

Processvia Protein(s)Taxonomy
nucleoplasmMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
plasma membraneMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
cell surfaceMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
intracellular membrane-bounded organelleMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
CSF1-CSF1R complexMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
receptor complexMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
plasma membraneMacrophage colony-stimulating factor 1 receptorHomo sapiens (human)
cytosolPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol 3-kinase complex, class IAPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
intercalated discPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
lamellipodiumPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
perinuclear region of cytoplasmPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol 3-kinase complexPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol 3-kinase complex, class IBPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
plasma membranePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cytoplasmPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
PML bodySerine/threonine-protein kinase mTORHomo sapiens (human)
lysosomal membraneSerine/threonine-protein kinase mTORHomo sapiens (human)
cytosolSerine/threonine-protein kinase mTORHomo sapiens (human)
Golgi membraneSerine/threonine-protein kinase mTORHomo sapiens (human)
nucleoplasmSerine/threonine-protein kinase mTORHomo sapiens (human)
cytoplasmSerine/threonine-protein kinase mTORHomo sapiens (human)
mitochondrial outer membraneSerine/threonine-protein kinase mTORHomo sapiens (human)
lysosomeSerine/threonine-protein kinase mTORHomo sapiens (human)
lysosomal membraneSerine/threonine-protein kinase mTORHomo sapiens (human)
endoplasmic reticulum membraneSerine/threonine-protein kinase mTORHomo sapiens (human)
cytosolSerine/threonine-protein kinase mTORHomo sapiens (human)
endomembrane systemSerine/threonine-protein kinase mTORHomo sapiens (human)
membraneSerine/threonine-protein kinase mTORHomo sapiens (human)
dendriteSerine/threonine-protein kinase mTORHomo sapiens (human)
TORC1 complexSerine/threonine-protein kinase mTORHomo sapiens (human)
TORC2 complexSerine/threonine-protein kinase mTORHomo sapiens (human)
phagocytic vesicleSerine/threonine-protein kinase mTORHomo sapiens (human)
nuclear envelopeSerine/threonine-protein kinase mTORHomo sapiens (human)
nucleusSerine/threonine-protein kinase mTORHomo sapiens (human)
cytoplasmSerine/threonine-protein kinase mTORHomo sapiens (human)
Golgi apparatusRapamycin-insensitive companion of mTORHomo sapiens (human)
cytosolRapamycin-insensitive companion of mTORHomo sapiens (human)
TORC2 complexRapamycin-insensitive companion of mTORHomo sapiens (human)
lysosomal membraneRegulatory-associated protein of mTORHomo sapiens (human)
nucleoplasmRegulatory-associated protein of mTORHomo sapiens (human)
cytoplasmRegulatory-associated protein of mTORHomo sapiens (human)
lysosomeRegulatory-associated protein of mTORHomo sapiens (human)
lysosomal membraneRegulatory-associated protein of mTORHomo sapiens (human)
cytosolRegulatory-associated protein of mTORHomo sapiens (human)
cytoplasmic stress granuleRegulatory-associated protein of mTORHomo sapiens (human)
dendriteRegulatory-associated protein of mTORHomo sapiens (human)
TORC1 complexRegulatory-associated protein of mTORHomo sapiens (human)
neuronal cell bodyRegulatory-associated protein of mTORHomo sapiens (human)
cytoplasmRegulatory-associated protein of mTORHomo sapiens (human)
nucleoplasmTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
Golgi apparatusTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
cytosolTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
plasma membraneTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
cytoplasmic vesicleTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
TORC2 complexTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
cytoplasmTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
plasma membraneTarget of rapamycin complex 2 subunit MAPKAP1Homo sapiens (human)
nucleoplasmTarget of rapamycin complex subunit LST8Homo sapiens (human)
cytoplasmTarget of rapamycin complex subunit LST8Homo sapiens (human)
lysosomal membraneTarget of rapamycin complex subunit LST8Homo sapiens (human)
cytosolTarget of rapamycin complex subunit LST8Homo sapiens (human)
TORC1 complexTarget of rapamycin complex subunit LST8Homo sapiens (human)
TORC2 complexTarget of rapamycin complex subunit LST8Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (583)

Assay IDTitleYearJournalArticle
AID737517Inhibition of EGFR L858R mutant (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737205Inhibition of PKA (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737476Inhibition of HIPK1(unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737252Inhibition of MAPKAPK2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737214Inhibition of PASK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741247Inhibition of EGFR L861Q mutant (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740730Inhibition of PRKG1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740767Inhibition of NEK6 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740783Inhibition of MRCKbeta (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741515Inhibition of TAO1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737474Inhibition of HCK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740772Inhibition of MET (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740764Inhibition of PAK2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741537Inhibition of PRKX (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740458Inhibition of p38alpha (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740498Inhibition of ROCK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741056Inhibition of EPHB1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1916669Inhibition of mTORC2 (unknown origin)2022European journal of medicinal chemistry, Aug-05, Volume: 238Contemporary mTOR inhibitor scaffolds to diseases breakdown: A patent review (2015-2021).
AID741031Inhibition of GRK6 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741255Inhibition of DCAMKL2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737469Inhibition of IKK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741561Inhibition of PKCbeta2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741287Inhibition of BRK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740464Inhibition of cKit (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737993In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of S6 phosphorylation at 30 mg/kg, po qd measured at 24 hrs relative to vehicle-treated control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741496Inhibition of p38alpha (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741292Inhibition of Aurora B (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737472Inhibition of IGF-1R (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737471Inhibition of IKKbeta (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737263Inhibition of JNK3 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741010Inhibition of JAK3 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741556Inhibition of PKCiota (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737467Inhibition of IRAK4 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740479Inhibition of STK25 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740485Inhibition of SGK2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741521Inhibition of SNF1LK2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737494Inhibition of FER (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741525Inhibition of RSK4 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740991Inhibition of MARK4 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737261Inhibition of KHS1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741251Inhibition of DYRK4 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230522Ratio of drug uptake in human PC3 cells xenografted in mouse at 100 mg/kg, po measured after 2 hrs to IC50 for mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID1230521In vivo inhibition of mTORC1 in human PC3 cells xenografted in mouse assessed as inhibition of S6 phosphorylation at 100 mg/kg, po measured after 2 hrs relative to control2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID737530Inhibition of CAMK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737268Inhibition of JAK2-JH1-JH2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740724Inhibition of PIM2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740780Inhibition of MST1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741043Inhibition of FES (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230531Ratio of drug uptake in human PC3 cells xenografted in mouse at 100 mg/kg, po measured after 24 hrs to IC50 for mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID741044Inhibition of FER (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740488Inhibition of RSK3 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740484Inhibition of SGK3 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741303Inhibition of p38gamma (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737752Inhibition of ABL T315I mutant (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740466Inhibition of ZIPK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741547Inhibition of PRKG2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740774Inhibition of MER (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741284Inhibition of BMX (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740744Inhibition of PKCbeta2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741266Inhibition of CLK2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741280Inhibition of CDK5/p35 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737527Inhibition of CAMK2beta (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741551Inhibition of PKD3 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741502Inhibition of cKit (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737250Inhibition of MARK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1916702Inhibition of PI3Kalpha (unknown origin)2022European journal of medicinal chemistry, Aug-05, Volume: 238Contemporary mTOR inhibitor scaffolds to diseases breakdown: A patent review (2015-2021).
AID740752Inhibition of PI3Kalpha (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740769Inhibition of NEK2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740474Inhibition of TSSK2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737728Inhibition of CK1delta (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741557Inhibition of PKCgamma (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737217Inhibition of PAK4 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737751Inhibition of ABL Y253F mutant (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737999Antitumor activity against human PC3 cells xenografted in po dosed CB17 SCID mouse assessed as tumor growth inhibition administered on day 11 post tumor implantation measured after 32 days relative to vehicle-treated control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737727Inhibition of CK1gamma2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740996Inhibition of MAPKAPK3 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID738005Antitumor activity against human PC3 cells xenografted in CB17 SCID mouse assessed as tumor growth inhibition at 20 mg/kg, po bid administered on day 11 post tumor implantation measured after 32 days2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741501Inhibition of cKit T670I mutant (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737241Inhibition of MKK6 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741055Inhibition of EPHB2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737480Inhibition of GRK7 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741002Inhibition of LYNB (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741257Inhibition of CAMK4 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740473Inhibition of TIE2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741512Inhibition of TSSK2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740756Inhibition of PDGFRalpha T674I mutant (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737493Inhibition of FES (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737525Inhibition of DAPK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737262Inhibition of KDR (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741507Inhibition of TYK2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737731Inhibition of CK1alpha1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1916668Inhibition of mTORC1 (unknown origin)2022European journal of medicinal chemistry, Aug-05, Volume: 238Contemporary mTOR inhibitor scaffolds to diseases breakdown: A patent review (2015-2021).
AID740759Inhibition of PASK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741299Inhibition of ABL (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737249Inhibition of MARK2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740454Inhibition of p70S6K (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737224Inhibition of NEK2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741511Inhibition of TIE2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741528Inhibition of RSK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737269Inhibition of JAK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737780Plasma concentration in CB17 SCID mouse xenografted with human PC3 cells at 30 mg/kg, po qd at 24 hrs2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737491Inhibition of FLT1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740490Inhibition of RSK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737220Inhibition of NEK9 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740777Inhibition of MST3 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740998Inhibition of MAPK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737270Inhibition of JAK2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740993Inhibition of MARK2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230518AUC (0 to infinity) in rat at 5 mg/kg, po2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID740776Inhibition of MST4 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741035Inhibition of GRK2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740988Inhibition of MEK2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737501Inhibition of ERBB4 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737235Inhibition of MSSK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737998Toxicity in CB17 SCID mouse xenografted with human PC3 cells at 10 to 50 mg/kg, po qd administered on day 11 post tumor implantation measured after 32 days2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737222Inhibition of NEK6 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737208Inhibition of PDK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737730Inhibition of CHK2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740482Inhibition of SRMS (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737772Drug uptake in tumor of CB17 SCID mouse xenografted with human PC3 cells at 30 mg/kg, po qd at 24 hrs2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741009Inhibition of JNK1alpha1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737783Plasma concentration in CB17 SCID mouse xenografted with human PC3 cells at 30 mg/kg, po qd at 2 hrs2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737486Inhibition of GRK2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737210Inhibition of PDGFRalpha V561D mutant (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741514Inhibition of TBK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737502Inhibition of ERBB2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741046Inhibition of FGFR3 K650E mutant (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740733Inhibition of PRAK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737473Inhibition of HGK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741264Inhibition of CLK3 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID738010Cytotoxicity against human PC3 cells assessed as growth inhibition after 3 days by WST1 assay2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737992In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of AKTS473 phosphorylation at 30 mg/kg, po qd after 2 to 8 hrs relative to vehicle-treated control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740487Inhibition of RSK4 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741304Inhibition of p38beta (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740725Inhibition of PIM1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740770Inhibition of NEK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737238Inhibition of MRCKbeta (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737735Inhibition of CDK7/cyclin H/MAT1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737203Inhibition of PKBbeta (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737749Inhibition of ARG (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID738015Inhibition of ALK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741253Inhibition of DYRK1B (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737511Inhibition of EPHA2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741297Inhibition of ABL G250E mutant (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741281Inhibition of CDK2/cyclin A (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741012Inhibition of JAK2-JH1-JH2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740771Inhibition of MUSK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741240Inhibition of EPHA5 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741047Inhibition of FGFR3 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737529Inhibition of CAMK2alpha (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741500Inhibition of cSRC (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741562Inhibition of PKCbeta1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741273Inhibition of CK1epsilon (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID738002Antitumor activity against human PC3 cells xenografted in CB17 SCID mouse assessed as tumor growth inhibition at 10 mg/kg, po qd administered on day 11 post tumor implantation measured after 32 days relative to vehicle-treated control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741242Inhibition of EPHA3 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230505Inhibition of PI3K-alpha (unknown origin) by mobility shift assay2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID741271Inhibition of CK1gamma1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741529Inhibition of RSE (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741029Inhibition of GSK3alpha (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737477Inhibition of GCK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741022Inhibition of IGF-1R (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740456Inhibition of p38delta (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741520Inhibition of SRMS (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737771Ratio of drug level in CB17 SCID mouse plasma xenografted with human PC3 cells at 30 mg/kg, po qd at 2 hrs to IC50 for mTORC2 in human PC3 cells2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737246Inhibition of MEK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737470Inhibition of IKKepsilon (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740999Inhibition of MAP3K8 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID738001Antitumor activity against human PC3 cells xenografted in CB17 SCID mouse assessed as tumor growth inhibition at 25 mg/kg, po qd administered on day 11 post tumor implantation measured after 32 days relative to vehicle-treated control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741249Inhibition of EGFR L858R mutant (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737757Inhibition of ALK4 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741555Inhibition of PKCmu (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737248Inhibition of MARK3 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737738Inhibition of CDK1/cyclin B (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741259Inhibition of CAMK2delta (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230528In vivo inhibition of mTORC1 in human PC3 cells xenografted in mouse assessed as inhibition of S6 phosphorylation at 100 mg/kg, po measured after 24 hrs relative to control2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID1230508Inhibition of mTOR (unknown origin) by HTR-FRET substrate phosphorylation assay2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID740782Inhibition of MSK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741564Inhibition of PKBgamma (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737761Ratio of drug level in tumor of CB17 SCID mouse xenografted with human PC3 cells at 30 mg/kg, po qd at 8 hrs to IC50 for mTORC2 in human PC3 cells2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737737Inhibition of CDK2/cyclin A (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741254Inhibition of DYR1A (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737481Inhibition of GRK6 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741245Inhibition of EGFR T790M/L858R double mutant (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737266Inhibition of JAK3 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740784Inhibition of MRCKalpha (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737509Inhibition of EPHA4 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740457Inhibition of p38beta (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737740Inhibition of BLK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737764Ratio of free drug level in CB17 SCID mouse plasma xenografted with human PC3 cells at 30 mg/kg, po qd at 24 hrs to IC50 for mTORC2 in human PC3 cells2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740748Inhibition of PKBgamma (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741300Inhibition of AMPK A2/B1/G1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741051Inhibition of ERBB4 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741298Inhibition of ABL E255K mutant (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737519Inhibition of DYRK4 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741006Inhibition of KDR (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737734Inhibition of CDK5/p35 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741523Inhibition of SGK2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740781Inhibition of MSK2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737504Inhibition of EPHB3 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741543Inhibition of PHKgamma2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737488Inhibition of FLT4 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737724Inhibition of CK1gamma3 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737484Inhibition of GRK3 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737503Inhibition of EPHB4 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737512Inhibition of EPHA1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID738003Antitumor activity against human PC3 cells xenografted in CB17 SCID mouse assessed as tumor growth inhibition at 100 mg/kg, po administered on day 11 for every two days post tumor implantation measured after 32 days2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737997In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of S6 phosphorylation at 100 mg/kg, po qd after 24 hrs2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737487Inhibition of FMS (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741544Inhibition of PHKgamma1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741294Inhibition of ARG (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737743Inhibition of BRK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740477Inhibition of TAO1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741527Inhibition of RSK2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737498Inhibition of FGFR2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741539Inhibition of PLK2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230537Ratio of drug uptake in human PC3 cells xenografted in mouse at 100 mg/kg, po measured after 24 hrs to IC50 for mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S4732015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID737744Inhibition of BRAF V599E mutant (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737227Inhibition of MET M1250T mutant (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740723Inhibition of PLK2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID738011Inhibition of mTORC2 in human PC3 cells assessed as inhibition of AKTS473 phosphorylation after 1 hr by sandwich immunoassay2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741559Inhibition of PKCepsilon (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741282Inhibition of CDK1/cyclin B (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740729Inhibition of PTK2B (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737489Inhibition of FLT3 D835Y mutant (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737209Inhibition of PDGFR beta (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741531Inhibition of RON (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737478Inhibition of GSK3beta (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230533In vivo inhibition of mTORC1 in human PC3 cells xenografted in mouse assessed as inhibition of Akt phosphorylation at S473 at 100 mg/kg, po measured after 8 hrs relative to control2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID737768Ratio of drug level in CB17 SCID mouse plasma xenografted with human PC3 cells at 30 mg/kg, po qd at 8 hrs to IC50 for mTORC2 in human PC3 cells2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737221Inhibition of NEK7 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740788Inhibition of MELK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230535Ratio of drug uptake in human PC3 cells xenografted in mouse at 100 mg/kg, po measured after 2 hrs to IC50 for mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S4732015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID737506Inhibition of EPHB1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737748Inhibition of Aurora B (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737532Inhibition of CLK2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741020Inhibition of IKKepsilon (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737242Inhibition of MINK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741295Inhibition of ABL Y253F mutant (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737750Inhibition of Aurora A (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737786Cmax in rat at 5 mg/kg, po2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740731Inhibition of PRKG2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741283Inhibition of BRSK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740459Inhibition of mTOR (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737996In vivo inhibition of mTORC2 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of AKTS473 phosphorylation at 100 mg/kg, po qd after 24 hrs2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737784Tmax in rat at 5 mg/kg, po2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737490Inhibition of FLT3 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737739Inhibition of BRSK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741549Inhibition of PRK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737213Inhibition of PDGFRalpha (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737787Mean residence time in rat at 2 mg/kg, iv2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737260Inhibition of LRRK2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741252Inhibition of DYRK3 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740787Inhibition of MINK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741279Inhibition of CDK5/p25 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737778Free plasma concentration in CB17 SCID mouse xenografted with human PC3 cells at 30 mg/kg, po qd at 4 hrs2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737775Drug uptake in tumor of CB17 SCID mouse xenografted with human PC3 cells at 30 mg/kg, po qd at 4 hrs2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740753Inhibition of PDK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740722Inhibition of PLK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737495Inhibition of FGFR4 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740470Inhibition of TRKC (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737745Inhibition of AXL (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741546Inhibition of PTK2B (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741007Inhibition of JNK3 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737776Free plasma concentration in CB17 SCID mouse xenografted with human PC3 cells at 30 mg/kg, po qd at 8 hrs2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737497Inhibition of FGFR3 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740735Inhibition of PKD2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737505Inhibition of EPHB2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737253Inhibition of MAPK3 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740491Inhibition of RSE (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230527In vivo inhibition of mTORC1 in human PC3 cells xenografted in mouse assessed as inhibition of S6 phosphorylation at 100 mg/kg, po measured after 8 hrs relative to control2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID741011Inhibition of JAK2 JH1 JH2 V617F mutant (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737721Inhibition of CLK3 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740779Inhibition of MSSK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741258Inhibition of CAMK2beta (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737520Inhibition of DYRK3 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737468Inhibition of IR (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741042Inhibition of FGR (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740471Inhibition of TRKB (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737226Inhibition of MUSK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740472Inhibition of TRKA (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741288Inhibition of BRAF V599E mutant (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741005Inhibition of KHS1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737513Inhibition of EGFR T790M/L858R double mutant (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741526Inhibition of RSK3 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737215Inhibition of PAK7 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740739Inhibition of PKCmu (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737524Inhibition of CAMK4 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741021Inhibition of IKKbeta (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741030Inhibition of GRK7 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737245Inhibition of MATK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741036Inhibition of FYN (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740741Inhibition of PKCepsilon (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741517Inhibition of STK25 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737747Inhibition of Aurora C (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737758Inhibition of AMPK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740997Inhibition of MAPK3 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740467Inhibition of ZAP70 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737789Volume of distribution at steady state in rat at 2 mg/kg, iv2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740728Inhibition of PTK5 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741260Inhibition of CAMK1-delta (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID738008Clearance in rat at 2 mg/kg, iv2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230509Metabolic stability in rat S9 fraction assessed as compound remaining measured at 60 mins2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID737763Ratio of drug level in tumor of CB17 SCID mouse xenografted with human PC3 cells at 30 mg/kg, po qd at 2 hrs to IC50 for mTORC2 in human PC3 cells2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740762Inhibition of PAK4 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741017Inhibition of IRR (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741014Inhibition of ITK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230541Antitumor activity against human PC3 cells xenografted in mouse assessed as tumor growth inhibition at 50 mg/kg, po qd2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID741497Inhibition of mTOR (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737759Inhibition of ALK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737725Inhibition of CK2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737254Inhibition of MAPK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741265Inhibition of CLK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740740Inhibition of PKCgamma (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740745Inhibition of PKCbeta1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737785AUC (0 to infinity) in rat at 5 mg/kg, po2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741028Inhibition of GSK3beta (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740738Inhibition of PKCiota (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737256Inhibition of LTK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737781Plasma concentration in CB17 SCID mouse xenografted with human PC3 cells at 30 mg/kg, po qd at 4 hrs2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741285Inhibition of BLK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740757Inhibition of PDGFRalpha D842V mutant (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740742Inhibition of PKCeta (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740994Inhibition of MARK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230534In vivo inhibition of mTORC1 in human PC3 cells xenografted in mouse assessed as inhibition of Akt phosphorylation at S473 at 100 mg/kg, po measured after 24 hrs relative to control2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID737211Inhibition of PDGFRalpha T674I mutant (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741016Inhibition of IRAK4 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741026Inhibition of HIPK1(unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740495Inhibition of RET (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741262Inhibition of CSK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737483Inhibition of GRK4 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740758Inhibition of PDGFRalpha (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741004Inhibition of LRRK2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740755Inhibition of PDGFRalpha V561D mutant (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741550Inhibition of PRAK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737206Inhibition of PI3Kgamma (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737492Inhibition of FGR (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737994In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of S6 phosphorylation at 30 mg/kg, po qd after 2 to 8 hrs relative to vehicle-treated control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741290Inhibition of AXL (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740468Inhibition of YES (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741301Inhibition of AMPK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740754Inhibition of PDGFR beta (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737767Ratio of free drug level in CB17 SCID mouse plasma xenografted with human PC3 cells at 30 mg/kg, po qd at 2 hrs to IC50 for mTORC2 in human PC3 cells2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740992Inhibition of MARK3 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740493Inhibition of RON (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741037Inhibition of FMS (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741015Inhibition of JAK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737247Inhibition of MARK4 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741291Inhibition of Aurora C (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737212Inhibition of PDGFRalpha D842V mutant (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737755Inhibition of ABL (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740497Inhibition of ROCK2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740743Inhibition of PKCdelta (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230519Oral bioavailability in rat at 5 mg/kg2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID737479Inhibition of GSK3alpha (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741548Inhibition of PRKG1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737258Inhibition of LYNB (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741504Inhibition of c-RAF (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741532Inhibition of RET Y791F mutant (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740761Inhibition of PAK6 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740463Inhibition of cKit T670I mutant (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID738012Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr by sandwich immunoassay2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737765Ratio of free drug level in CB17 SCID mouse plasma xenografted with human PC3 cells at 30 mg/kg, po qd at 8 hrs to IC50 for mTORC2 in human PC3 cells2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741041Inhibition of FLT1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740494Inhibition of RET Y791F mutant (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741563Inhibition of PKCalpha (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740778Inhibition of MST2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737729Inhibition of CK1epsilon (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741000Inhibition of LCK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741019Inhibition of IKK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737991In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of AKTS473 phosphorylation at 30 mg/kg, po qd measured at 24 hrs relative to vehicle-treated control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740476Inhibition of TBK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740720Inhibition of PRKX (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741505Inhibition of ZAP70 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740492Inhibition of ROS (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741510Inhibition of TRKA (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737723Inhibition of CK2 alpha2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741302Inhibition of p70S6K (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740786Inhibition of MKK6 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737742Inhibition of BTK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737508Inhibition of EPHA5 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741027Inhibition of GCK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID738004Antitumor activity against human PC3 cells xenografted in CB17 SCID mouse assessed as tumor growth inhibition at 50 mg/kg, po qd administered on day 11 post tumor implantation measured after 32 days2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737265Inhibition of JNK1alpha1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737259Inhibition of LYNA (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741269Inhibition of CK1gamma2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740462Inhibition of cSRC (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID738009Selectivity ratio of IC50 for PI3Kalpha (unknown origin) to IC50 for recombinant mTOR (unknown origin)2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741052Inhibition of ERBB2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740750Inhibition of PKA (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737255Inhibition of MAP3K8 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741018Inhibition of IR (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740763Inhibition of PAK3 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741053Inhibition of EPHB4 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741518Inhibition of SRPK2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737244Inhibition of MEK2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741513Inhibition of TSSK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737754Inhibition of ABL E255K mutant (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230536Ratio of drug uptake in human PC3 cells xenografted in mouse at 100 mg/kg, po measured after 8 hrs to IC50 for mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S4732015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID740768Inhibition of NEK4 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741289Inhibition of BRAF (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737228Inhibition of MET (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741516Inhibition of SYK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741025Inhibition of HIPK4 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741533Inhibition of RET V804L mutant (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737485Inhibition of FYN (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741246Inhibition of EGFR T790M mutant (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741534Inhibition of RET (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741261Inhibition of CAMK2alpha (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737515Inhibition of EGFR L861Q mutant (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740746Inhibition of PKCalpha (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737240Inhibition of MLK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740727Inhibition of PHKgamma1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737482Inhibition of GRK5 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737782Plasma concentration in CB17 SCID mouse xenografted with human PC3 cells at 30 mg/kg, po qd at 8 hrs2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737518Inhibition of EEF2K (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741250Inhibition of EEF2K (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740751Inhibition of PI3Kgamma (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741558Inhibition of PKCeta (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741241Inhibition of EPHA4 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741013Inhibition of JAK2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1916683Inhibition of mTOR (unknown origin)2022European journal of medicinal chemistry, Aug-05, Volume: 238Contemporary mTOR inhibitor scaffolds to diseases breakdown: A patent review (2015-2021).
AID1230524In vivo inhibition of mTORC1 in human PC3 cells xenografted in mouse assessed as inhibition of Akt phosphorylation at S473 at 100 mg/kg, po measured after 2 hrs relative to control2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID737753Inhibition of ABL G250E mutant (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID738007Oral bioavailability in rat at 5 mg/kg2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740465Inhibition of c-RAF (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741272Inhibition of CK1delta (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740721Inhibition of PLK3 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737243Inhibition of MELK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741001Inhibition of LTK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740775Inhibition of MYLK2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737733Inhibition of CHK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741270Inhibition of CK1gamma3 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741540Inhibition of PLK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737251Inhibition of MAPKAPK3 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740455Inhibition of p38gamma (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737239Inhibition of MRCKalpha (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737762Ratio of drug level in tumor of CB17 SCID mouse xenografted with human PC3 cells at 30 mg/kg, po qd at 4 hrs to IC50 for mTORC2 in human PC3 cells2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740747Inhibition of PKBbeta (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737496Inhibition of FGFR3 K650E mutant (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741305Inhibition of p38delta (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737756Inhibition of AMPK A2/B1/G1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737465Inhibition of ITK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID738013Inhibition of PI3Kalpha (unknown origin) by mobility shift assay2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737229Inhibition of MER (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737995Plasma protein binding in CB17 SCID mouse xenografted with human PC3 cells at 30 mg/kg, po qd after 24 hrs2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740460Inhibition of cSRC N1 mutant (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230530Ratio of drug uptake in human PC3 cells xenografted in mouse at 100 mg/kg, po measured after 8 hrs to IC50 for mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID1230544Antitumor activity against human PC3 cells xenografted in mouse assessed as tumor volume reduction at 50 mg/kg, po qd for 21 days relative to control2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID737774Drug uptake in tumor of CB17 SCID mouse xenografted with human PC3 cells at 30 mg/kg, po qd at 2 hrs2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741263Inhibition of CAMK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741552Inhibition of PKD2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741506Inhibition of YES (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741050Inhibition of FAK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230539Antitumor activity against human PC3 cells xenografted in po dosed mouse assessed as tumor growth inhibition administered as qd for 21 days2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID1230515Selectivity ratio of IC50 for PI3K-alpha (unknown origin) to IC50 for mTOR (unknown origin)2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID741048Inhibition of FGFR2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741524Inhibition of SGK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737514Inhibition of EGFR T790M mutant (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737218Inhibition of PAK3 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID738016Inhibition of ALK4 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741296Inhibition of ABL T315I mutant (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741554Inhibition of PKCtheta (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741054Inhibition of EPHB3 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741024Inhibition of HCK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741040Inhibition of FLT3 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741293Inhibition of Aurora A (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740478Inhibition of SYK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230526In vivo inhibition of mTORC1 in human PC3 cells xenografted in mouse assessed as inhibition of S6 phosphorylation at 100 mg/kg, po measured after 4 hrs relative to control2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID737531Inhibition of CSK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741503Inhibition of ZIPK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741538Inhibition of PLK3 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737233Inhibition of MST3 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741542Inhibition of PIM1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737257Inhibition of LCK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741049Inhibition of FGFR1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741243Inhibition of EPHA2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740766Inhibition of NEK7 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741033Inhibition of GRK4 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741509Inhibition of TRKB (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741278Inhibition of CDK7/cyclin H/MAT1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737773Drug uptake in tumor of CB17 SCID mouse xenografted with human PC3 cells at 30 mg/kg, po qd at 8 hrs2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741530Inhibition of ROS (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741286Inhibition of BTK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737788AUC (0 to infinity) in rat at 2 mg/kg, iv2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737769Ratio of drug level in CB17 SCID mouse plasma xenografted with human PC3 cells at 30 mg/kg, po qd at 24 hrs to IC50 for mTORC2 in human PC3 cells2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737741Inhibition of BMX (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737267Inhibition of JAK2 JH1 JH2 V617F mutant (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741560Inhibition of PKCdelta (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737526Inhibition of CAMK2delta (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737232Inhibition of MST2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741256Inhibition of DAPK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741499Inhibition of IRRK2 G2019S mutant (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737225Inhibition of NEK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740726Inhibition of PHKgamma2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737219Inhibition of PAK2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID738006Inhibition of FMS (unknown origin)2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737766Ratio of free drug level in CB17 SCID mouse plasma xenografted with human PC3 cells at 30 mg/kg, po qd at 4 hrs to IC50 for mTORC2 in human PC3 cells2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740995Inhibition of MAPKAPK2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741535Inhibition of ROCK2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740732Inhibition of PRK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740990Inhibition of MATK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741244Inhibition of EPHA1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737507Inhibition of EPHA8 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740489Inhibition of RSK2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737237Inhibition of MSK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737236Inhibition of MSK2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740734Inhibition of PKD3 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741277Inhibition of CHK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737779Free plasma concentration in CB17 SCID mouse xenografted with human PC3 cells at 30 mg/kg, po qd at 2 hrs2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741545Inhibition of PTK5 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737521Inhibition of DYR1A (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737746Inhibition of BRAF (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737516Inhibition of EGFR (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740496Inhibition of RET V804L mutant (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737231Inhibition of MST4 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741034Inhibition of GRK3 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737760Ratio of drug level in tumor of CB17 SCID mouse xenografted with human PC3 cells at 30 mg/kg, po qd at 24 hrs to IC50 for mTORC2 in human PC3 cells2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID738000Antitumor activity against human PC3 cells xenografted in CB17 SCID mouse assessed as tumor growth inhibition at 50 mg/kg, po qd administered on day 11 post tumor implantation measured after 32 days relative to vehicle-treated control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740475Inhibition of TSSK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741039Inhibition of FLT3 D835Y mutant (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741522Inhibition of SGK3 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737207Inhibition of PI3Kalpha (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740737Inhibition of PKCtheta (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737732Inhibition of CDK9/cyclin T1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741023Inhibition of HGK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID738014Inhibition of recombinant mTOR (unknown origin) using GST-p70S6 as substrate after 60 mins by TR-FRET analysis2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230532In vivo inhibition of mTORC1 in human PC3 cells xenografted in mouse assessed as inhibition of Akt phosphorylation at S473 at 100 mg/kg, po measured after 4 hrs relative to control2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID741275Inhibition of CK1alpha1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737223Inhibition of NEK4 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230516Cmax in rat at 5 mg/kg, po2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID737522Inhibition of DYRK1B (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740461Inhibition of IRRK2 G2019S mutant (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741519Inhibition of SRPK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737234Inhibition of MST1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740736Inhibition of PKCzeta (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740480Inhibition of SRPK2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230529Ratio of drug uptake in human PC3 cells xenografted in mouse at 100 mg/kg, po measured after 4 hrs to IC50 for mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID737475Inhibition of HIPK4 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737264Inhibition of JNK2alpha2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737722Inhibition of CLK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741248Inhibition of EGFR (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740773Inhibition of MET M1250T mutant (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741239Inhibition of EPHA8 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741032Inhibition of GRK5 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741267Inhibition of CK2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230523Inhibition of mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S473 after 1 hr2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID737736Inhibition of CDK5/p25 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740785Inhibition of MLK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740765Inhibition of NEK9 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741003Inhibition of LYNA (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741541Inhibition of PIM2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737466Inhibition of IRR (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741274Inhibition of CHK2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737230Inhibition of MYLK2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230520Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID741508Inhibition of TRKC (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737499Inhibition of FGFR1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741498Inhibition of cSRC N1 mutant (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737528Inhibition of CAMK1-delta (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737770Ratio of drug level in CB17 SCID mouse plasma xenografted with human PC3 cells at 30 mg/kg, po qd at 4 hrs to IC50 for mTORC2 in human PC3 cells2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741268Inhibition of CK2 alpha2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740486Inhibition of SGK (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740469Inhibition of TYK2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740749Inhibition of PKBalpha (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741008Inhibition of JNK2alpha2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741045Inhibition of FGFR4 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737510Inhibition of EPHA3 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740989Inhibition of MEK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737204Inhibition of PKBalpha (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737523Inhibition of DCAMKL2 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230514Clearance in rat at 2 mg/kg, iv2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID741276Inhibition of CDK9/cyclin T1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741038Inhibition of FLT4 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737216Inhibition of PAK6 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737500Inhibition of FAK (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740483Inhibition of SNF1LK2 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737726Inhibition of CK1gamma1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID1230525Ratio of drug uptake in human PC3 cells xenografted in mouse at 100 mg/kg, po measured after 4 hrs to IC50 for mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S4732015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
AID740760Inhibition of PAK7 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID737777Free plasma concentration in CB17 SCID mouse xenografted with human PC3 cells at 30 mg/kg, po qd at 24 hrs2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741536Inhibition of ROCK1 (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID741553Inhibition of PKCzeta (unknown origin) assessed as remaining activity at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
AID740481Inhibition of SRPK1 (unknown origin) assessed as remaining activity at 1 uM relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's5 (83.33)24.3611
2020's1 (16.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (16.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (83.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]