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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)

Found 7 hits in this display   

TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
University Of Manchester

Curated by ChEMBL
LigandPNGBDBM4627(5-[(6,7-dimethoxyquinazolin-4-yl)amino]-4-fluoro-2...)
Affinity DataIC50:  0.75nMAssay Description:Inhibition of human RET cytoplasmic domain (658 to 1114 residues) expressed in baculovirus system preincubated for 15 mins followed by substrate addi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
University Of Manchester

Curated by ChEMBL
LigandPNGBDBM4627(5-[(6,7-dimethoxyquinazolin-4-yl)amino]-4-fluoro-2...)
Affinity DataIC50:  2.30nMAssay Description:Inhibition of recombinant His-tagged human KDR expressed in insect Sf21 cells preincubated for 15 mins followed by substrate addition measured after ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
University Of Manchester

Curated by ChEMBL
LigandPNGBDBM4627(5-[(6,7-dimethoxyquinazolin-4-yl)amino]-4-fluoro-2...)
Affinity DataIC50:  3nMT: 2°CAssay Description:An ELISA assay was used to determine the ability of inhibitor to inhibit VEGF-R RTK activity. The compounds were incubated with enzyme 20 min at room...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
University Of Manchester

Curated by ChEMBL
LigandPNGBDBM4627(5-[(6,7-dimethoxyquinazolin-4-yl)amino]-4-fluoro-2...)
Affinity DataIC50:  9.5nMAssay Description:Inhibition of KDR (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based lumine...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 1(Homo sapiens (Human))
Astrazeneca

LigandPNGBDBM4627(5-[(6,7-dimethoxyquinazolin-4-yl)amino]-4-fluoro-2...)
Affinity DataIC50:  30nMpH: 7.4 T: 2°CAssay Description:An ELISA assay was used to determine the ability of inhibitor to inhibit VEGF-R RTK activity. The compounds were incubated with enzyme 20 min at room...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKinesin-1 heavy chain/Proto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
University Of Manchester

Curated by ChEMBL
LigandPNGBDBM4627(5-[(6,7-dimethoxyquinazolin-4-yl)amino]-4-fluoro-2...)
Affinity DataIC50:  41nMAssay Description:Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFibroblast growth factor receptor 1(Homo sapiens (Human))
Astrazeneca

LigandPNGBDBM4627(5-[(6,7-dimethoxyquinazolin-4-yl)amino]-4-fluoro-2...)
Affinity DataIC50:  2.50E+3nMT: 2°CAssay Description:An ELISA assay was used to determine the ability of inhibitor to inhibit FGFR-1 TK activity. The compounds were incubated with enzyme 20 min at room ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed