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Found 992 with Last Name = 'hegen' and Initial = 'm'
TargetTyrosine-protein kinase ITK/TSK(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  0.0269nMpH: 7.5Assay Description:Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase TXK(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  0.131nMpH: 7.5Assay Description:Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytoplasmic tyrosine-protein kinase BMX(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  0.545nMpH: 7.5Assay Description:Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Tec(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  0.679nMpH: 7.5Assay Description:Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  6.31nMpH: 7.5Assay Description:Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466897(CHEMBL4287715)
Affinity DataKi:  20nMAssay Description:Displacement of [3H]-25-hydroxycholesterol from human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cell...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466891(CHEMBL4281109)
Affinity DataKi:  20nMAssay Description:Displacement of [3H]-25-hydroxycholesterol from human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cell...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetTyrosine-protein kinase ITK/TSK(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  27nMAssay Description:Inhibition of full length recombinant human GST-tagged cytoplasmic ITK expressed in baculovirus expression system by KT236 probe based TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Blk(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  32.4nMpH: 7.5Assay Description:Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466893(CHEMBL4291727)
Affinity DataKi:  50nMAssay Description:Displacement of [3H]-25-hydroxycholesterol from human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cell...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  62.3nMpH: 7.5Assay Description:Assay buffer was 20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.01% BSA, 1 mM DTT, 0.0005% Tween 20, and 2% DMSO. Inactivation kinetic reactions were performed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase TXK(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  131nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged TXK using GEPLYWSFPAKKK as substrate measured every 60 secs for 1 hr by PK/LDH coupled spectrop...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytoplasmic tyrosine-protein kinase BMX(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  545nMAssay Description:Inhibition of full length recombinant human His-tagged cytoplasmic BMX expressed in baculovirus expression system by KT236 probe based TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Tec(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  679nMAssay Description:Inhibition of full length human His-tagged TEC by KT178 probe based TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466892(CHEMBL4283871)
Affinity DataKi:  1.20E+3nMAssay Description:Displacement of [3H]-25-hydroxycholesterol from human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cell...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  6.31E+3nMAssay Description:Inhibition of recombinant human GST-tagged cytoplasmic JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system by KT2...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNuclear receptor ROR-gamma(Homo sapiens (Human))
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466913(CHEMBL4289304)
Affinity DataKi:  1.90E+4nMAssay Description:Displacement of [3H]-25-hydroxycholesterol from human N-terminal 6His-tagged-RORC2 LBD (259 to 483 residues) expressed in Escherichia coli (DE3) cell...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Blk(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  3.24E+4nMAssay Description:Inhibition of full length recombinant human His-tagged cytoplasmic BLK expressed in baculovirus expression system by KT236 probe based TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataKi:  6.23E+4nMAssay Description:Inhibition of full length recombinant human His-tagged cytoplasmic BTK expressed in baculovirus expression system by KT236 probe based TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInterleukin-1 receptor-associated kinase 4(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50239500(CHEMBL4066705 | US10329302, Example 337 | US107935...)
Affinity DataIC50:  0.100nMAssay Description:Inhibition of N-terminal His6-tagged human full length IRAK4 preincubated for 20 mins followed by biotinylated-AGAGRDKYKTLRQIR substrate addition in ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInterleukin-1 receptor-associated kinase 4(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50239499(CHEMBL4081711 | US10329302, Example 344 | US107935...)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of N-terminal His6-tagged human full length IRAK4 preincubated for 20 mins followed by biotinylated-AGAGRDKYKTLRQIR substrate addition in ...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of recombinant human GST-tagged cytoplasmic JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system using ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50501537(CHEMBL4085582)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of recombinant human GST-tagged cytoplasmic JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system using ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetInterleukin-1 receptor-associated kinase 4(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50239498(CHEMBL4093120 | US10329302, Example 189 | US107935...)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of N-terminal His6-tagged human full length IRAK4 preincubated for 20 mins followed by biotinylated-AGAGRDKYKTLRQIR substrate addition in ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

LigandPNGBDBM209866(PF-06651600 | US11111242, Example 5 | US2023034848...)
Affinity DataIC50:  0.346nMpH: 7.4 T: 2°CAssay Description:Test compounds were solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. Compounds were diluted in DMSO to create an 11-point ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50501536(CHEMBL4064018)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of recombinant human GST-tagged cytoplasmic JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system using ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetInterleukin-1 receptor-associated kinase 4(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50239507(CHEMBL4091434 | US10329302, Example 246 | US107935...)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of N-terminal His6-tagged human full length IRAK4 preincubated for 20 mins followed by biotinylated-AGAGRDKYKTLRQIR substrate addition in ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50357312(IBRUTINIB | PCI-32765 | US10124003, Ref. Ex. Compo...)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of human full-length BTK expressed in Sf9 cells using FAM-Srctide peptide as substrate after 60 mins by TR-FRET AssayMore data for this Ligand-Target Pair
TargetInterleukin-1 receptor-associated kinase 4(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50239508(CHEMBL4085199 | US10329302, Example 309 | US107935...)
Affinity DataIC50:  0.600nMAssay Description:Inhibition of N-terminal His6-tagged human full length IRAK4 preincubated for 20 mins followed by biotinylated-AGAGRDKYKTLRQIR substrate addition in ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

LigandPNGBDBM316524(US11111242, Example 12 | US9617258, Example 12)
Affinity DataIC50:  0.700nMAssay Description:Inhibition of recombinant human GST-tagged cytoplasmic JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system using ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50357333(CHEMBL1916891)
Affinity DataIC50:  0.700nMAssay Description:Inhibition of human full-length BTK expressed in Sf9 cells using FAM-Srctide peptide as substrate preincubated for 60 mins measured after 60 mins by ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50357314(CHEMBL1916713)
Affinity DataIC50:  0.847nMAssay Description:Inhibition of human full-length BTK expressed in Sf9 cells using FAM-Srctide peptide as substrate after 60 mins by TR-FRET AssayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50357313(CHEMBL1916712)
Affinity DataIC50:  0.847nMAssay Description:Inhibition of human full-length BTK expressed in Sf9 cells using FAM-Srctide peptide as substrate after 60 mins by TR-FRET AssayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50357316(CHEMBL1916715)
Affinity DataIC50:  0.884nMAssay Description:Inhibition of human full-length BTK expressed in Sf9 cells using FAM-Srctide peptide as substrate after 60 mins by TR-FRET AssayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  0.960nMpH: 7.4 T: 2°CAssay Description:Test compounds were solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. Compounds were diluted in DMSO to create an 11-point ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM159756(PF-02384554 | US10966980, Example 8 | US9035074, 8)
Affinity DataIC50:  1nMpH: 7.4 T: 2°CAssay Description:Test compounds were solubilized in dimethyl sulfoxide (DMSO) to a stock concentration of 30 mM. Compounds were diluted in DMSO to create an 11-point ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetInterleukin-1 receptor-associated kinase 4(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50239491(CHEMBL4083655 | US10329302, Example 173 | US107935...)
Affinity DataIC50:  1.30nMAssay Description:Inhibition of N-terminal His6-tagged human full length IRAK4 preincubated for 20 mins followed by biotinylated-AGAGRDKYKTLRQIR substrate addition in ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInterleukin-1 receptor-associated kinase 4(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50239493(CHEMBL4103497 | US10329302, Example 312 | US107935...)
Affinity DataIC50:  1.30nMAssay Description:Inhibition of N-terminal His6-tagged human full length IRAK4 preincubated for 20 mins followed by biotinylated-AGAGRDKYKTLRQIR substrate addition in ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50357333(CHEMBL1916891)
Affinity DataIC50:  1.40nMAssay Description:Inhibition of EGFR preincubated for 60 mins measured after 60 mins by TR-FRET AssayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytoplasmic tyrosine-protein kinase BMX(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50357333(CHEMBL1916891)
Affinity DataIC50:  1.53nMAssay Description:Inhibition of BMX relative to controlMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Lyn(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50357321(CHEMBL1916879)
Affinity DataIC50:  1.55nMAssay Description:Inhibition of LYN-A expressed in Sf9 cells after 60 mins by TR-FRET AssayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50357330(CHEMBL1916888)
Affinity DataIC50:  1.55nMAssay Description:Inhibition of human full-length BTK expressed in Sf9 cells using FAM-Srctide peptide as substrate after 60 mins by TR-FRET AssayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50357334(CHEMBL1916892)
Affinity DataIC50:  1.82nMAssay Description:Inhibition of human full-length BTK expressed in Sf9 cells using FAM-Srctide peptide as substrate after 60 mins by TR-FRET AssayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50357324(CHEMBL1916882)
Affinity DataIC50:  1.89nMAssay Description:Inhibition of human full-length BTK expressed in Sf9 cells using FAM-Srctide peptide as substrate after 60 mins by TR-FRET AssayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInterleukin-1 receptor-associated kinase 4(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50239506(CHEMBL4071526 | US10329302, Example 188 | US107935...)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of N-terminal His6-tagged human full length IRAK4 preincubated for 20 mins followed by biotinylated-AGAGRDKYKTLRQIR substrate addition in ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50357333(CHEMBL1916891)
Affinity DataIC50:  1.93nMAssay Description:Inhibition of human full-length BTK expressed in Sf9 cells using FAM-Srctide peptide as substrate after 60 mins by TR-FRET AssayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInterleukin-1 receptor-associated kinase 4(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50239499(CHEMBL4081711 | US10329302, Example 344 | US107935...)
Affinity DataIC50:  2nMAssay Description:Inhibition of IRAK4 in human PBMC assessed as reduction in R848-stimulated TNF alpha production by measuring plasma protein binding corrected IC50 af...More data for this Ligand-Target Pair
TargetInterleukin-1 receptor-associated kinase 4(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50239499(CHEMBL4081711 | US10329302, Example 344 | US107935...)
Affinity DataIC50:  2nMAssay Description:Inhibition of IRAK4 in human whole blood assessed as reduction R848-induced IL-6 secretion by measuring plasma protein binding corrected IC50 preincu...More data for this Ligand-Target Pair
TargetInterleukin-1 receptor-associated kinase 4(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50239499(CHEMBL4081711 | US10329302, Example 344 | US107935...)
Affinity DataIC50:  2nMAssay Description:Inhibition of IRAK4 in human PBMC assessed as reduction in R848-stimulated TNF alpha production after 3 hrsMore data for this Ligand-Target Pair
TargetInterleukin-1 receptor-associated kinase 4(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50239497(CHEMBL4084228 | US10329302, Example 271 | US107935...)
Affinity DataIC50:  2.40nMAssay Description:Inhibition of N-terminal His6-tagged human full length IRAK4 preincubated for 20 mins followed by biotinylated-AGAGRDKYKTLRQIR substrate addition in ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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