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Found 2582 with Last Name = 'stevens' and Initial = 'kl'
TargetInsulin receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50256480(CHEMBL466397 | N-(2,6-difluorophenyl)-5-(3-(2-(5-e...)
Affinity DataKi:  1.30nMAssay Description:Binding affinity to insulin receptor by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50256480(CHEMBL466397 | N-(2,6-difluorophenyl)-5-(3-(2-(5-e...)
Affinity DataKi:  1.60nMAssay Description:Binding affinity to IGF1R by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50256478(CHEMBL507714 | N-(2,6-difluorophenyl)-3-(3-(2-(2-m...)
Affinity DataKi:  2.20nMAssay Description:Binding affinity to insulin receptor by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50256478(CHEMBL507714 | N-(2,6-difluorophenyl)-3-(3-(2-(2-m...)
Affinity DataKi:  5.20nMAssay Description:Binding affinity to IGF1R by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50168293(CHEMBL3805430)
Affinity DataIC50:  0.100nMAssay Description:Inhibition human full length PI3Kdelta catalytic subunit/p85alpha assessed as formation of PIP3 after 30 mins by europium labeled GRP-based TR-FRET a...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM50168297(CHEMBL3805760 | US9765060, Compound 96)
Affinity DataIC50:  0.100nMAssay Description:TR-FRET monitored the formation of 3,4,5-inositol triphosphate molecule that competed with fluorescently labeled PIP3 for binding to the GRP-1 plecks...More data for this Ligand-Target Pair
In DepthDetails US Patent
LigandPNGBDBM50168290(CHEMBL3805572)
Affinity DataIC50:  0.100nMAssay Description:Inhibition human full length PI3Kdelta catalytic subunit/p85alpha assessed as formation of PIP3 after 30 mins by europium labeled GRP-based TR-FRET a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50168297(CHEMBL3805760 | US9765060, Compound 96)
Affinity DataIC50:  0.130nMAssay Description:Inhibition human full length PI3Kdelta catalytic subunit/p85alpha assessed as formation of PIP3 after 30 mins by europium labeled GRP-based TR-FRET a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50168299(CHEMBL3805664)
Affinity DataIC50:  0.150nMAssay Description:Inhibition human full length PI3Kdelta catalytic subunit/p85alpha assessed as formation of PIP3 after 30 mins by europium labeled GRP-based TR-FRET a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50265871(3-(2-(1-(2-(dimethylamino)acetyl)-6-methoxy-4,4-di...)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of IGF1RMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM208824(US9266878, 49a)
Affinity DataIC50:  0.300nMAssay Description:Inhibition human full length PI3Kdelta catalytic subunit/p85alpha assessed as formation of PIP3 after 30 mins by europium labeled GRP-based TR-FRET a...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
LigandPNGBDBM208826(US9266878, 51a)
Affinity DataIC50:  0.300nMAssay Description:Inhibition human full length PI3Kdelta catalytic subunit/p85alpha assessed as formation of PIP3 after 30 mins by europium labeled GRP-based TR-FRET a...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM27826(4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine, 9 | 4...)
Affinity DataIC50:  0.300nMpH: 7.5 T: 2°CAssay Description:Assays are performed in 384-well microtiter plates in reaction buffer containing biotinylated substrate, ATP, and purified activated GST-IGF-1R in th...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50265869(3-(2-(1-(2-(dimethylamino)acetyl)-5-methoxyindolin...)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of IGF1RMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 2(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50293153(CHEMBL526110 | N-(3-nitrophenyl)-4-(pyrazolo[1,5-b...)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of human CDK2 by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 4(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50293153(CHEMBL526110 | N-(3-nitrophenyl)-4-(pyrazolo[1,5-b...)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of CDK4 by radioactive glutathione plate-binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM341173((S)-2,4-diamino-6-(((5-chloro-4-oxo-3-phenyl-3,4-d...)
Affinity DataIC50:  0.300nMAssay Description:TR-FRET monitored the formation of 3,4,5-inositol triphosphate molecule that competed with fluorescently labeled PIP3 for binding to the GRP-1 plecks...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50265847(3-(2-(1-(2-(dimethylamino)acetyl)-6-methoxy-1,2,3,...)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of IGF1RMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM500197(US11021467, Compound 54)
Affinity DataIC50:  0.400nMAssay Description:Class I PI3K isoforms were expressed and purified as heterodimeric recombinant proteins. All assay reagents and buffers for the TR-FRET assay were pu...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM500199(US11021467, Compound 56)
Affinity DataIC50:  0.400nMAssay Description:Class I PI3K isoforms were expressed and purified as heterodimeric recombinant proteins. All assay reagents and buffers for the TR-FRET assay were pu...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM341280(N-((3R,5S)-5-(5-chloro-4-oxo-3-phenyl-3,4-dihydroq...)
Affinity DataIC50:  0.400nMAssay Description:TR-FRET monitored the formation of 3,4,5-inositol triphosphate molecule that competed with fluorescently labeled PIP3 for binding to the GRP-1 plecks...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM50168484(CHEMBL3805137 | US9765060, Compound Y)
Affinity DataIC50:  0.400nMAssay Description:TR-FRET monitored the formation of 3,4,5-inositol triphosphate molecule that competed with fluorescently labeled PIP3 for binding to the GRP-1 plecks...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM341219((S)-2,4-diamino-6-((1-(4-oxo-3-phenyl-5-(3-(piperi...)
Affinity DataIC50:  0.400nMAssay Description:TR-FRET monitored the formation of 3,4,5-inositol triphosphate molecule that competed with fluorescently labeled PIP3 for binding to the GRP-1 plecks...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM341228((S)-2,4-diamino-6-((1-(5-(3-(3,3-difluoropyrrolidi...)
Affinity DataIC50:  0.400nMAssay Description:TR-FRET monitored the formation of 3,4,5-inositol triphosphate molecule that competed with fluorescently labeled PIP3 for binding to the GRP-1 plecks...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM50168484(CHEMBL3805137 | US9765060, Compound Y)
Affinity DataIC50:  0.400nMAssay Description:Inhibition human full length PI3Kdelta catalytic subunit/p85alpha assessed as formation of PIP3 after 30 mins by europium labeled GRP-based TR-FRET a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50265869(3-(2-(1-(2-(dimethylamino)acetyl)-5-methoxyindolin...)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of IRMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50265869(3-(2-(1-(2-(dimethylamino)acetyl)-5-methoxyindolin...)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of ALKMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM208793(US9266878, 16a)
Affinity DataIC50:  0.400nMAssay Description:Inhibition human full length PI3Kdelta catalytic subunit/p85alpha assessed as formation of PIP3 after 30 mins by europium labeled GRP-based TR-FRET a...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM27825(4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine, 8 | 4...)
Affinity DataIC50:  0.400nMpH: 7.5 T: 2°CAssay Description:Assays are performed in 384-well microtiter plates in reaction buffer containing biotinylated substrate, ATP, and purified activated GST-IGF-1R in th...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50168300(CHEMBL3804870)
Affinity DataIC50:  0.450nMAssay Description:Inhibition human full length PI3Kdelta catalytic subunit/p85alpha assessed as formation of PIP3 after 30 mins by europium labeled GRP-based TR-FRET a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50168431(CHEMBL3805913)
Affinity DataIC50:  0.470nMAssay Description:Inhibition human full length PI3Kdelta catalytic subunit/p85alpha assessed as formation of PIP3 after 30 mins by europium labeled GRP-based TR-FRET a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM500198(US11021467, Compound 55)
Affinity DataIC50:  0.5nMAssay Description:Class I PI3K isoforms were expressed and purified as heterodimeric recombinant proteins. All assay reagents and buffers for the TR-FRET assay were pu...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM27842(4,5-difluoro-2-{[2-({2-methoxy-4-[4-(propan-2-yl)p...)
Affinity DataIC50:  0.5nMpH: 7.5 T: 2°CAssay Description:Assays are performed in 384-well microtiter plates in reaction buffer containing biotinylated substrate, ATP, and purified activated GST-IGF-1R in th...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50265872(3-(2-(1-(2-(dimethylamino)acetyl)-6-methoxy-1,2,3,...)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of IGF1RMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM27793(2-{[2-({5-[2-(dimethylamino)acetamido]-2-methoxy-4...)
Affinity DataIC50:  0.5nMpH: 7.5 T: 2°CAssay Description:Assays are performed in 384-well microtiter plates in reaction buffer containing biotinylated substrate, ATP, and purified activated GST-IGF-1R in th...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM341210((S)-3-(2-(1-((2,6-diamino-5-cyanopyrimidin-4-yl)am...)
Affinity DataIC50:  0.5nMAssay Description:TR-FRET monitored the formation of 3,4,5-inositol triphosphate molecule that competed with fluorescently labeled PIP3 for binding to the GRP-1 plecks...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM208819(US9266878, 44a)
Affinity DataIC50:  0.5nMAssay Description:Inhibition human full length PI3Kdelta catalytic subunit/p85alpha assessed as formation of PIP3 after 30 mins by europium labeled GRP-based TR-FRET a...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50265849(2-(dimethylamino)-1-(7-(4-(indolin-1-yl)-7H-pyrrol...)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of IGF1RMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM341227((S)-2,4-diamino-6-((1-(4-oxo-3-phenyl-5-(3-(2,2,6,...)
Affinity DataIC50:  0.5nMAssay Description:TR-FRET monitored the formation of 3,4,5-inositol triphosphate molecule that competed with fluorescently labeled PIP3 for binding to the GRP-1 plecks...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM341221((S)-2,4-diamino-6-((1-(5-(3-(4,4-difluoropiperidin...)
Affinity DataIC50:  0.5nMAssay Description:TR-FRET monitored the formation of 3,4,5-inositol triphosphate molecule that competed with fluorescently labeled PIP3 for binding to the GRP-1 plecks...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM341211((S)-3-(2-(1-((2,6-diamino-5-cyanopyrimidin-4-yl)am...)
Affinity DataIC50:  0.5nMAssay Description:TR-FRET monitored the formation of 3,4,5-inositol triphosphate molecule that competed with fluorescently labeled PIP3 for binding to the GRP-1 plecks...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM50168427(CHEMBL3805887)
Affinity DataIC50:  0.540nMAssay Description:Inhibition human full length PI3Kdelta catalytic subunit/p85alpha assessed as formation of PIP3 after 30 mins by europium labeled GRP-based TR-FRET a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM341270((S)-2-(1-((2-amino-5-iodo-6-methylpyrimidin-4-yl)a...)
Affinity DataIC50:  0.600nMAssay Description:TR-FRET monitored the formation of 3,4,5-inositol triphosphate molecule that competed with fluorescently labeled PIP3 for binding to the GRP-1 plecks...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM27822(2-[(2-{[2-methoxy-4-(1-propyl-1,2,5,6-tetrahydropy...)
Affinity DataIC50:  0.600nMpH: 7.5 T: 2°CAssay Description:Assays are performed in 384-well microtiter plates in reaction buffer containing biotinylated substrate, ATP, and purified activated GST-IGF-1R in th...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM341234((S)-2,4-diamino-6-((1-(5-(3-morpholinopropyl)-4-ox...)
Affinity DataIC50:  0.600nMAssay Description:TR-FRET monitored the formation of 3,4,5-inositol triphosphate molecule that competed with fluorescently labeled PIP3 for binding to the GRP-1 plecks...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM500263(US11021467, Compound 122)
Affinity DataIC50:  0.700nMAssay Description:Class I PI3K isoforms were expressed and purified as heterodimeric recombinant proteins. All assay reagents and buffers for the TR-FRET assay were pu...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM341218((S)-2,4-diamino-6-((1-(4-oxo-3-phenyl-5-(2-(pyrrol...)
Affinity DataIC50:  0.700nMAssay Description:TR-FRET monitored the formation of 3,4,5-inositol triphosphate molecule that competed with fluorescently labeled PIP3 for binding to the GRP-1 plecks...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50265850(3-(2-(1-(2-(dimethylamino)acetyl)-5-methoxyindolin...)
Affinity DataIC50:  0.700nMAssay Description:Inhibition of IGF1RMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
Gilead Sciences

US Patent
LigandPNGBDBM341282(N-((3R,5S)-5-(5-chloro-3-(3,5-difluorophenyl)-4-ox...)
Affinity DataIC50:  0.700nMAssay Description:TR-FRET monitored the formation of 3,4,5-inositol triphosphate molecule that competed with fluorescently labeled PIP3 for binding to the GRP-1 plecks...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM27828(4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine, 11 | ...)
Affinity DataIC50:  0.700nMAssay Description:Inhibition of IGF1RMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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