Page last updated: 2024-11-13

ly2940680

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

Cross-References

ID SourceID
PubMed CID49848070
CHEMBL ID2142592
SCHEMBL ID2128615
MeSH IDM0585243

Synonyms (48)

Synonym
taladegib ,
HY-13242
CHEMBL2142592
SCHEMBL2128615
LY2940680 ,
ly-2940680
ly 2940680
1ks ,
4-fluoro-n-methyl-n-{1-[4-(1-methyl-1h-pyrazol-5-yl)phthalazin-1-yl]piperidin-4-yl}-2-(trifluoromethyl)benzamide
qy8bwx1lj5 ,
taladegib [usan:inn]
benzamide, 4-fluoro-n-methyl-n-(1-(4-(1-methyl-1h-pyrazol-5-yl)-1-phthalazinyl)-4-piperidinyl)-2-(trifluoromethyl)-
unii-qy8bwx1lj5
BCP9000881
1258861-20-9
NCGC00263170-01
CS-0459
taladegib [who-dd]
taladegib [usan]
taladegib [inn]
4-fluoro-n-methyl-n-(1-(4-(1-methyl-1h-pyrazol-5-yl)phthalazin-1-yl)piperidin-4-yl)-2-(trifluoromethyl)benzamide
4-fluoro-n-methyl-n-(1-(4-(1-methyl-1h-pyrazol-5-yl)-1-phthalazinyl)-4-piperidinyl)-2-(trifluoromethyl)benzamide
smr004702857
MLS006011066
D10671
taladegib (usan/inn)
AC-33096
taladegib (ly2940680)
DTXSID50154986
AKOS026674116
J-515412
EX-A156
benzamide, 4-fluoro-n-methyl-n-[1-[4-(1-methyl-1h-pyrazol-5-yl)-1-phthalazinyl]-4-piperidinyl]-2-(trifluoromethyl)-
AS-75020
mfcd21609264
4-fluoro-n-methyl-n-{1-[4-(1-methyl-1h-pyrazol-5-yl)-1-phthalazinyl]-4-piperidinyl}-2-(trifluoromethyl)benzamide
NCGC00263170-06
ly-2940680(taladegib)
DB12550
BCP02512
SB16504
4-fluoro-n-methyl-n-[1-[4-(2-methylpyrazol-3-yl)phthalazin-1-yl]piperidin-4-yl]-2-(trifluoromethyl)benzamide
gtpl10333
CCG-269788
Q27287564
nsc-767896
nsc767896
bdbm50545020

Research Excerpts

Compound-Compound Interactions

ExcerptReferenceRelevance
" The primary objective was to determine the recommended Phase 2 dose of crenigacestat in combination with other anticancer agents (taladegib, LY3023414 [dual inhibitor of phosphoinositide 3-kinase; mechanistic target of rapamycin], or abemaciclib)."( A phase 1b study of the Notch inhibitor crenigacestat (LY3039478) in combination with other anticancer target agents (taladegib, LY3023414, or abemaciclib) in patients with advanced or metastatic solid tumors.
Anderson, B; Azaro, A; Benhadji, KA; Cassier, PA; Italiano, A; Massard, C; Merchan, J; Oakley, G; Pant, S; Tap, WD; Yu, D; Yuen, E, 2021
)
0.62

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" This study demonstrated that crenigacestat combined with different anticancer agents (taladegib, LY3023414, or abemaciclib) was poorly tolerated, leading to lowered dosing and disappointing clinical activity in patients with advanced or metastatic solid tumors."( A phase 1b study of the Notch inhibitor crenigacestat (LY3039478) in combination with other anticancer target agents (taladegib, LY3023414, or abemaciclib) in patients with advanced or metastatic solid tumors.
Anderson, B; Azaro, A; Benhadji, KA; Cassier, PA; Italiano, A; Massard, C; Merchan, J; Oakley, G; Pant, S; Tap, WD; Yu, D; Yuen, E, 2021
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency2.13170.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency25.00350.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
GVesicular stomatitis virusPotency8.48660.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency8.48660.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency8.48660.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency8.48660.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency8.48660.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Smoothened homologMus musculus (house mouse)IC50 (µMol)0.00180.00120.37681.9000AID1416097; AID1848242
Smoothened homologHomo sapiens (human)IC50 (µMol)0.20210.00040.16401.5000AID1667114; AID1845992
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (112)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IISmoothened homologHomo sapiens (human)
negative regulation of transcription by RNA polymerase IISmoothened homologHomo sapiens (human)
vasculogenesisSmoothened homologHomo sapiens (human)
osteoblast differentiationSmoothened homologHomo sapiens (human)
in utero embryonic developmentSmoothened homologHomo sapiens (human)
cell fate specificationSmoothened homologHomo sapiens (human)
neural crest cell migrationSmoothened homologHomo sapiens (human)
negative regulation of protein phosphorylationSmoothened homologHomo sapiens (human)
heart loopingSmoothened homologHomo sapiens (human)
positive regulation of neuroblast proliferationSmoothened homologHomo sapiens (human)
positive regulation of mesenchymal cell proliferationSmoothened homologHomo sapiens (human)
determination of left/right asymmetry in lateral mesodermSmoothened homologHomo sapiens (human)
type B pancreatic cell developmentSmoothened homologHomo sapiens (human)
protein import into nucleusSmoothened homologHomo sapiens (human)
apoptotic processSmoothened homologHomo sapiens (human)
G protein-coupled receptor signaling pathwaySmoothened homologHomo sapiens (human)
smoothened signaling pathwaySmoothened homologHomo sapiens (human)
ventral midline determinationSmoothened homologHomo sapiens (human)
neuroblast proliferationSmoothened homologHomo sapiens (human)
midgut developmentSmoothened homologHomo sapiens (human)
anterior/posterior pattern specificationSmoothened homologHomo sapiens (human)
gene expressionSmoothened homologHomo sapiens (human)
positive regulation of gene expressionSmoothened homologHomo sapiens (human)
negative regulation of gene expressionSmoothened homologHomo sapiens (human)
spinal cord dorsal/ventral patterningSmoothened homologHomo sapiens (human)
dentate gyrus developmentSmoothened homologHomo sapiens (human)
cerebellar cortex morphogenesisSmoothened homologHomo sapiens (human)
thalamus developmentSmoothened homologHomo sapiens (human)
dorsal/ventral neural tube patterningSmoothened homologHomo sapiens (human)
central nervous system neuron differentiationSmoothened homologHomo sapiens (human)
cerebral cortex developmentSmoothened homologHomo sapiens (human)
positive regulation of cell migrationSmoothened homologHomo sapiens (human)
negative regulation of epithelial cell differentiationSmoothened homologHomo sapiens (human)
hair follicle morphogenesisSmoothened homologHomo sapiens (human)
multicellular organism growthSmoothened homologHomo sapiens (human)
positive regulation of multicellular organism growthSmoothened homologHomo sapiens (human)
positive regulation of protein import into nucleusSmoothened homologHomo sapiens (human)
odontogenesis of dentin-containing toothSmoothened homologHomo sapiens (human)
negative regulation of apoptotic processSmoothened homologHomo sapiens (human)
negative regulation of DNA bindingSmoothened homologHomo sapiens (human)
positive regulation of smoothened signaling pathwaySmoothened homologHomo sapiens (human)
positive regulation of organ growthSmoothened homologHomo sapiens (human)
astrocyte activationSmoothened homologHomo sapiens (human)
skeletal muscle fiber developmentSmoothened homologHomo sapiens (human)
smooth muscle tissue developmentSmoothened homologHomo sapiens (human)
forebrain morphogenesisSmoothened homologHomo sapiens (human)
homeostasis of number of cells within a tissueSmoothened homologHomo sapiens (human)
epithelial cell proliferationSmoothened homologHomo sapiens (human)
positive regulation of epithelial cell proliferationSmoothened homologHomo sapiens (human)
protein stabilizationSmoothened homologHomo sapiens (human)
myoblast migrationSmoothened homologHomo sapiens (human)
negative regulation of hair follicle developmentSmoothened homologHomo sapiens (human)
contact inhibitionSmoothened homologHomo sapiens (human)
atrial septum morphogenesisSmoothened homologHomo sapiens (human)
mammary gland epithelial cell differentiationSmoothened homologHomo sapiens (human)
epithelial-mesenchymal cell signalingSmoothened homologHomo sapiens (human)
somite developmentSmoothened homologHomo sapiens (human)
pancreas morphogenesisSmoothened homologHomo sapiens (human)
left/right axis specificationSmoothened homologHomo sapiens (human)
cellular response to cholesterolSmoothened homologHomo sapiens (human)
dopaminergic neuron differentiationSmoothened homologHomo sapiens (human)
mesenchymal to epithelial transition involved in metanephric renal vesicle formationSmoothened homologHomo sapiens (human)
positive regulation of branching involved in ureteric bud morphogenesisSmoothened homologHomo sapiens (human)
regulation of somatic stem cell population maintenanceSmoothened homologHomo sapiens (human)
regulation of heart morphogenesisSmoothened homologHomo sapiens (human)
pattern specification processSmoothened homologHomo sapiens (human)
central nervous system developmentSmoothened homologHomo sapiens (human)
commissural neuron axon guidanceSmoothened homologHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (24)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
cAMP-dependent protein kinase inhibitor activitySmoothened homologHomo sapiens (human)
G protein-coupled receptor activitySmoothened homologHomo sapiens (human)
patched bindingSmoothened homologHomo sapiens (human)
protein bindingSmoothened homologHomo sapiens (human)
oxysterol bindingSmoothened homologHomo sapiens (human)
protein kinase A catalytic subunit bindingSmoothened homologHomo sapiens (human)
protein sequestering activitySmoothened homologHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (33)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endocytic vesicle membraneSmoothened homologMus musculus (house mouse)
ciliary membraneSmoothened homologMus musculus (house mouse)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
Golgi apparatusSmoothened homologHomo sapiens (human)
caveolaSmoothened homologHomo sapiens (human)
late endosomeSmoothened homologHomo sapiens (human)
endoplasmic reticulumSmoothened homologHomo sapiens (human)
endoplasmic reticulum-Golgi intermediate compartmentSmoothened homologHomo sapiens (human)
centrioleSmoothened homologHomo sapiens (human)
plasma membraneSmoothened homologHomo sapiens (human)
ciliumSmoothened homologHomo sapiens (human)
endocytic vesicle membraneSmoothened homologHomo sapiens (human)
intracellular membrane-bounded organelleSmoothened homologHomo sapiens (human)
ciliary membraneSmoothened homologHomo sapiens (human)
extracellular exosomeSmoothened homologHomo sapiens (human)
ciliary tipSmoothened homologHomo sapiens (human)
9+0 non-motile ciliumSmoothened homologHomo sapiens (human)
ciliumSmoothened homologHomo sapiens (human)
dendriteSmoothened homologHomo sapiens (human)
plasma membraneSmoothened homologHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (48)

Assay IDTitleYearJournalArticle
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID686947qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Identification of potent Yes1 kinase inhibitors using a library screening approach.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1496028Inhibition of hedgehog signaling pathway in mouse Light2 cells after 48 hrs by Gli-luciferase reporter gene assay2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Synthesis and evaluation of novel dimethylpyridazine derivatives as hedgehog signaling pathway inhibitors.
AID1491493Antitumor activity against Ptch+/- and p53-/- mouse medulloblastoma cells allografted in athymic nude mouse assessed as tumor growth inhibition at 50 mg/kg, po bid administered daily via gavage for 13 days2017European journal of medicinal chemistry, Sep-29, Volume: 138Design, synthesis, and biological evaluation of optimized phthalazine derivatives as hedgehog signaling pathway inhibitors.
AID1667116Antiproliferation activity against human A2058 cells incubated for 72 hrs by MTT assay2020Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6
Design, synthesis and biological evaluation of anthranilamide derivatives as potent SMO inhibitors.
AID1845993Antiproliferative activity against human Daoy cells assessed as inhibition of cell growth2021European journal of medicinal chemistry, Apr-05, Volume: 215Medulloblastoma drugs in development: Current leads, trials and drawbacks.
AID1848242Inhibition of SMO in mouse 3T3/HH FlashII-7 cells incubated for 36 hrs in presence of SHH by Gli-luciferase reporter assay2022Bioorganic & medicinal chemistry, 11-15, Volume: 74Design, synthesis and biological evaluation of novel 4-aminopiperidine derivatives as SMO/ERK dual inhibitors.
AID1848246Antiproliferative activity against human RBE cells overexpressing Hh/ERK pathway assessed as inhibition of cell growth incubated for 96 hrs by CCK8 assay2022Bioorganic & medicinal chemistry, 11-15, Volume: 74Design, synthesis and biological evaluation of novel 4-aminopiperidine derivatives as SMO/ERK dual inhibitors.
AID1416098Stability of the compound in DMEM at 100 uL by RP-HPLC analysis2017MedChemComm, Jun-01, Volume: 8, Issue:6
A structurally guided dissection-then-evolution strategy for ligand optimization of smoothened receptor.
AID1667115Antiproliferative activity against human DaOY cells incubated for 72 hrs by MTT assay2020Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6
Design, synthesis and biological evaluation of anthranilamide derivatives as potent SMO inhibitors.
AID1848243Inhibition of ERK2 (unknown origin) using kinase substrate 8 incubated for 40 mins in presence of ATP by mobility shift assay2022Bioorganic & medicinal chemistry, 11-15, Volume: 74Design, synthesis and biological evaluation of novel 4-aminopiperidine derivatives as SMO/ERK dual inhibitors.
AID1496027Inhibition of hedgehog signaling pathway in mouse Light2 cells at 100 nM after 48 hrs by Gli-luciferase reporter gene assay relative to control2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Synthesis and evaluation of novel dimethylpyridazine derivatives as hedgehog signaling pathway inhibitors.
AID1491490Inhibition of hedgehog signaling pathway in mouse NIH/3T3 Light2 cells by Gli-luciferase reporter gene assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Design, synthesis, and biological evaluation of optimized phthalazine derivatives as hedgehog signaling pathway inhibitors.
AID1416097Antagonist activity at Smo receptor in mouse NIH/3T3 cells harboring GRE-Luc assessed as inhibition of SAG-induced Hh signaling pathway preincubated for 1 to 2 hrs followed by SAG addition and measured after 24 hrs by Bright-Glo luciferase reporter gene a2017MedChemComm, Jun-01, Volume: 8, Issue:6
A structurally guided dissection-then-evolution strategy for ligand optimization of smoothened receptor.
AID1491491Antiproliferative activity against Ptch+/- and p53-/- mouse medulloblastoma cells after 36 hrs by Brdu incorporation assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Design, synthesis, and biological evaluation of optimized phthalazine derivatives as hedgehog signaling pathway inhibitors.
AID1667114Inhibition of SMO D473H mutant receptor (unknown origin) assessed as inhibition of SAG-induced Hh signaling pathway by Gli luciferase reporter cell-based assay2020Bioorganic & medicinal chemistry, 03-15, Volume: 28, Issue:6
Design, synthesis and biological evaluation of anthranilamide derivatives as potent SMO inhibitors.
AID1845992Antagonist activity at resistant Smo D473H mutant (unknown origin) in presence of GDC04492021European journal of medicinal chemistry, Apr-05, Volume: 215Medulloblastoma drugs in development: Current leads, trials and drawbacks.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (22)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's12 (54.55)24.3611
2020's10 (45.45)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 19.04

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

MetricThis Compound (vs All)
Research Demand Index19.04 (24.57)
Research Supply Index3.18 (2.92)
Research Growth Index4.58 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.04)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (4.55%)5.53%
Reviews3 (13.64%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other18 (81.82%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]