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Found 1136 with Last Name = 'teffera' and Initial = 'y'
LigandPNGBDBM24466(1-(2-hydroxy-2-methylpropyl)-N-{5-[(7-methoxyquino...)
Affinity DataKi:  0.5nM ΔG°:  -52.6kJ/molepH: 7.4 T: 2°CAssay Description:In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHepatocyte growth factor receptor(Homo sapiens (Human))
Amgen

LigandPNGBDBM24459(N-{3-fluoro-4-[(7-methoxyquinolin-4-yl)oxy]phenyl}...)
Affinity DataKi:  1nM ΔG°:  -50.9kJ/molepH: 7.4 T: 2°CAssay Description:In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHepatocyte growth factor receptor(Homo sapiens (Human))
Amgen

LigandPNGBDBM24462(N-{3-fluoro-4-[(7-methoxyquinolin-4-yl)oxy]phenyl}...)
Affinity DataKi:  1nM ΔG°:  -50.9kJ/molepH: 7.4 T: 2°CAssay Description:In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...More data for this Ligand-Target Pair
TargetHepatocyte growth factor receptor(Homo sapiens (Human))
Amgen

LigandPNGBDBM24460(N-{3-fluoro-4-[(7-methoxyquinolin-4-yl)oxy]phenyl}...)
Affinity DataKi:  1.02nM ΔG°:  -50.8kJ/molepH: 7.4 T: 2°CAssay Description:In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHepatocyte growth factor receptor(Homo sapiens (Human))
Amgen

LigandPNGBDBM24463(N-{3-fluoro-4-[(7-methoxyquinolin-4-yl)oxy]phenyl}...)
Affinity DataKi:  1.10nM ΔG°:  -50.6kJ/molepH: 7.4 T: 2°CAssay Description:In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM24466(1-(2-hydroxy-2-methylpropyl)-N-{5-[(7-methoxyquino...)
Affinity DataKi:  1.10nM ΔG°:  -50.6kJ/molepH: 7.4 T: 2°CAssay Description:In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHepatocyte growth factor receptor(Homo sapiens (Human))
Amgen

LigandPNGBDBM24466(1-(2-hydroxy-2-methylpropyl)-N-{5-[(7-methoxyquino...)
Affinity DataKi:  1.20nM ΔG°:  -50.4kJ/molepH: 7.4 T: 2°CAssay Description:In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHepatocyte growth factor receptor(Homo sapiens (Human))
Amgen

LigandPNGBDBM24464(N-{3-fluoro-4-[(7-methoxyquinolin-4-yl)oxy]phenyl}...)
Affinity DataKi:  1.30nM ΔG°:  -50.2kJ/molepH: 7.4 T: 2°CAssay Description:In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHepatocyte growth factor receptor(Mus musculus)
Amgen

LigandPNGBDBM24466(1-(2-hydroxy-2-methylpropyl)-N-{5-[(7-methoxyquino...)
Affinity DataKi:  2nM ΔG°:  -49.2kJ/molepH: 7.4 T: 2°CAssay Description:In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM24464(N-{3-fluoro-4-[(7-methoxyquinolin-4-yl)oxy]phenyl}...)
Affinity DataKi:  2nM ΔG°:  -49.2kJ/molepH: 7.4 T: 2°CAssay Description:In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM24466(1-(2-hydroxy-2-methylpropyl)-N-{5-[(7-methoxyquino...)
Affinity DataKi:  2.20nM ΔG°:  -48.9kJ/molepH: 7.4 T: 2°CAssay Description:In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHepatocyte growth factor receptor(Homo sapiens (Human))
Amgen

LigandPNGBDBM24465(N-{3-fluoro-4-[(7-methoxyquinolin-4-yl)oxy]phenyl}...)
Affinity DataKi:  2.70nM ΔG°:  -48.4kJ/molepH: 7.4 T: 2°CAssay Description:In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...More data for this Ligand-Target Pair
LigandPNGBDBM24466(1-(2-hydroxy-2-methylpropyl)-N-{5-[(7-methoxyquino...)
Affinity DataKi:  4.10nM ΔG°:  -47.4kJ/molepH: 7.4 T: 2°CAssay Description:In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM24466(1-(2-hydroxy-2-methylpropyl)-N-{5-[(7-methoxyquino...)
Affinity DataKi:  4.5nM ΔG°:  -47.2kJ/molepH: 7.4 T: 2°CAssay Description:In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHepatocyte growth factor receptor(Homo sapiens (Human))
Amgen

LigandPNGBDBM24461(N-{3-fluoro-4-[(7-methoxyquinolin-4-yl)oxy]phenyl}...)
Affinity DataKi:  8nM ΔG°:  -45.7kJ/molepH: 7.4 T: 2°CAssay Description:In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM24459(N-{3-fluoro-4-[(7-methoxyquinolin-4-yl)oxy]phenyl}...)
Affinity DataKi:  24nM ΔG°:  -43.1kJ/molepH: 7.4 T: 2°CAssay Description:In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50302904(CHEMBL568138 | N-((6-(3,5-difluorophenyl)-[1,2,4]t...)
Affinity DataKi:  200nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM24463(N-{3-fluoro-4-[(7-methoxyquinolin-4-yl)oxy]phenyl}...)
Affinity DataKi:  386nM ΔG°:  -36.2kJ/molepH: 7.4 T: 2°CAssay Description:In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM24462(N-{3-fluoro-4-[(7-methoxyquinolin-4-yl)oxy]phenyl}...)
Affinity DataKi:  396nM ΔG°:  -36.2kJ/molepH: 7.4 T: 2°CAssay Description:In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50361983(CHEMBL1939697)
Affinity DataKi:  730nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as unbound inhibitor concentration required for half maximal enz...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50361983(CHEMBL1939697)
Affinity DataKi:  740nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using testosterone as substrate assessed as unbound inhibitor concentration required for half maximal ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM24461(N-{3-fluoro-4-[(7-methoxyquinolin-4-yl)oxy]phenyl}...)
Affinity DataKi:  999nM ΔG°:  -33.9kJ/molepH: 7.4 T: 2°CAssay Description:In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM24465(N-{3-fluoro-4-[(7-methoxyquinolin-4-yl)oxy]phenyl}...)
Affinity DataKi:  1.16E+3nM ΔG°:  -33.5kJ/molepH: 7.4 T: 2°CAssay Description:In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50302905(7-methoxy-N-((6-(3-methylisothiazol-5-yl)-[1,2,4]t...)
Affinity DataKi:  1.60E+3nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50361983(CHEMBL1939697)
Affinity DataKi:  1.90E+3nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using testosterone as substrate assessed as residual enzyme activity after 2 to 10 mins by LC-MS/MS an...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50361983(CHEMBL1939697)
Affinity DataKi:  1.90E+3nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as residual enzyme activity after 2 to 10 mins by LC-MS/MS analy...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM24466(1-(2-hydroxy-2-methylpropyl)-N-{5-[(7-methoxyquino...)
Affinity DataKi:  4.10E+3nM ΔG°:  -30.4kJ/molepH: 7.4 T: 2°CAssay Description:In vitro kinase assays were done to establish IC50 values against recombinant enzymes using homogeneous time-resolved fluorescence (HTRF) assay. For ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM50236362(CHEMBL429743 | N-(4-chlorophenyl)-6-(6,7-dimethoxy...)
Affinity DataIC50:  0.0300nMAssay Description:Inhibition of KDR by HTRF assayMore data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM50375681(CHEMBL411630)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of KDR by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM50376042(CHEMBL409512)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of KDR by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM50376025(AMG-0309 | CHEMBL409538)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of KDR by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase mTOR(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50341056(5-(1-(4-amino-6-methyl-1,3,5-triazin-2-yl)-1H-benz...)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of mTOR assessed as inhibition of phosphorylation of 4EBP1 by Lantha-Screen enzyme assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50341056(5-(1-(4-amino-6-methyl-1,3,5-triazin-2-yl)-1H-benz...)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of PI3KbetaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM50376040(CHEMBL272824)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of KDR by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIntegrin alpha-4/beta-1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50109899((R)-3-{[(S)-1-(3,5-Dichloro-benzenesulfonyl)-pyrro...)
Affinity DataIC50:  0.270nMAssay Description:Inhibitory activity against alpha-4 beta-1 receptor (VLA-4) in human RPMI-8866 cells using [125I]-VCAM-Ig ligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM50376030(CHEMBL269916)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of KDR by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM50376026(CHEMBL272691)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of KDR by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM50376019(CHEMBL429585)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of KDR by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM50376036(CHEMBL270092)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of KDR by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIntegrin alpha-4/beta-1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50109908((R)-3-(4-Cyclopropoxy-phenyl)-3-{[(S)-1-(3,5-dichl...)
Affinity DataIC50:  0.310nMAssay Description:Inhibitory activity against alpha-4 beta-1 receptor (VLA-4) in human RPMI-8866 cells using [125I]-VCAM-Ig ligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM50375996(CHEMBL272250)
Affinity DataIC50:  0.370nMAssay Description:Inhibition of KDRMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIntegrin alpha-4/beta-1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50109917((R)-3-{[(S)-1-(3,5-Dichloro-benzenesulfonyl)-azeti...)
Affinity DataIC50:  0.390nMAssay Description:Inhibitory activity against alpha-4 beta-1 receptor (VLA-4) in human RPMI-8866 cells using [125I]-VCAM-Ig ligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIntegrin alpha-4/beta-1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50109917((R)-3-{[(S)-1-(3,5-Dichloro-benzenesulfonyl)-azeti...)
Affinity DataIC50:  0.390nMAssay Description:Inhibitory activity against alpha-4 beta-1 receptor (VLA-4) in human RPMI-8866 cells using [125I]-VCAM-Ig ligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50341056(5-(1-(4-amino-6-methyl-1,3,5-triazin-2-yl)-1H-benz...)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of PI3KdeltaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM50375999(CHEMBL270342)
Affinity DataIC50:  0.450nMAssay Description:Inhibition of KDRMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM50236362(CHEMBL429743 | N-(4-chlorophenyl)-6-(6,7-dimethoxy...)
Affinity DataIC50:  0.480nMAssay Description:Inhibition of KDRMore data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM50375690(CHEMBL270954)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of KDR by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM50375679(CHEMBL270548)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of KDR by HTRF assayMore data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM50236362(CHEMBL429743 | N-(4-chlorophenyl)-6-(6,7-dimethoxy...)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of KDR by HTRF assayMore data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Amgen

LigandPNGBDBM50236362(CHEMBL429743 | N-(4-chlorophenyl)-6-(6,7-dimethoxy...)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of KDR (unknown origin)More data for this Ligand-Target Pair
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