Compile Data Set for Download or QSAR
Report error Found 992 with Last Name = 'hegen' and Initial = 'm'
LigandPNGBDBM209866(PF-06651600 | US9617258, Example 5 | US11111242, E...)
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 Depth
Date in BDB:
1/23/2017
Entry Details Article
PubMed
TargetAryl hydrocarbon receptor(Mouse)
Pfizer

Curated by ChEMBL
LigandPNGBDBM23927(Tetrachlorodibenzodioxin | 2,3,7,8-Tetrachlorodibe...)
Affinity DataEC50:  0.0300nMAssay Description:Agonist activity at Ah receptor in genetically engineered mouse cells expressing firefly luciferase gene by CALUX transactivational assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
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 Depth
Date in BDB:
9/22/2019
Entry Details Article
PubMed
TargetTyrosine-protein kinase TXK(Human)
Pfizer

LigandPNGBDBM209866(PF-06651600 | US9617258, Example 5 | US11111242, E...)
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 Depth
Date in BDB:
1/23/2017
Entry Details Article
PubMed
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
In Depth
Date in BDB:
9/22/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
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 Depth
Date in BDB:
9/22/2019
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM209866(PF-06651600 | US9617258, Example 5 | US11111242, E...)
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 Depth
Date in BDB:
9/5/2020
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Pfizer

Curated by ChEMBL
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
In Depth
Date in BDB:
9/5/2020
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM209866(PF-06651600 | US9617258, Example 5 | US11111242, E...)
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 Depth
Date in BDB:
1/23/2017
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Pfizer

Curated by ChEMBL
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
In Depth
Date in BDB:
9/5/2020
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50357312(IBRUTINIB | US9181263, 1 | US9108973, Ref 1 | US92...)
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
In Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
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 Depth
Date in BDB:
9/22/2019
Entry Details Article
PubMed
LigandPNGBDBM209866(PF-06651600 | US9617258, Example 5 | US11111242, E...)
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 Depth
Date in BDB:
1/23/2017
Entry Details Article
PubMed
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 Depth
Date in BDB:
9/22/2019
Entry Details Article
PubMed
TargetTyrosine-protein kinase Tec(Human)
Pfizer

LigandPNGBDBM209866(PF-06651600 | US9617258, Example 5 | US11111242, E...)
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 Depth
Date in BDB:
1/23/2017
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Pfizer

Curated by ChEMBL
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 Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM316524(US9617258, Example 12 | US11111242, Example 12 | U...)
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
In Depth
Date in BDB:
9/5/2020
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Pfizer

Curated by ChEMBL
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 Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Pfizer

Curated by ChEMBL
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 Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Pfizer

Curated by ChEMBL
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 Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
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 Depth
Date in BDB:
1/23/2017
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Pfizer

LigandPNGBDBM159756(PF-02384554 | US9035074, 8 | US10966980, Example 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
In Depth
Date in BDB:
1/23/2017
Entry Details Article
PubMed
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 Depth
Date in BDB:
9/22/2019
Entry Details Article
PubMed
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 Depth
Date in BDB:
9/22/2019
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(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 Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
LigandPNGBDBM50357333(CHEMBL1916891)
Affinity DataIC50: 1.53nMAssay Description:Inhibition of BMX relative to controlMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Pfizer

Curated by ChEMBL
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 Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
TargetTyrosine-protein kinase Lyn(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 Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Pfizer

Curated by ChEMBL
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 Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Pfizer

Curated by ChEMBL
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 Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
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 Depth
Date in BDB:
9/22/2019
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Pfizer

Curated by ChEMBL
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 Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
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
In Depth
Date in BDB:
9/22/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
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
In Depth
Date in BDB:
9/22/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
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
In Depth
Date in BDB:
9/22/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
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 Depth
Date in BDB:
9/22/2019
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50357315(CHEMBL1916714)
Affinity DataIC50: 2.52nMAssay 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 Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50357339(CHEMBL1916897)
Affinity DataIC50: 2.60nMAssay 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 Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Pfizer

LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
Affinity DataIC50: 2.60nMpH: 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 Depth
Date in BDB:
1/23/2017
Entry Details Article
PubMed
LigandPNGBDBM50239492(CHEMBL4070515 | US10329302, Example 211 | US107935...)
Affinity DataIC50: 2.70nMAssay 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 Depth
Date in BDB:
9/22/2019
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Pfizer

LigandPNGBDBM159756(PF-02384554 | US9035074, 8 | US10966980, Example 8)
Affinity DataIC50: 2.70nMpH: 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 Depth
Date in BDB:
1/23/2017
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50357323(CHEMBL1916881)
Affinity DataIC50: 2.96nMAssay 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 Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
TargetCollagenase 3(Human)
Wyeth Research

LigandPNGBDBM23498((3S)-4-{[4-(but-2-yn-1-yloxy)benzene]sulfonyl}-N-h...)
Affinity DataIC50: 3nMpH: 7.4 T: 2°CAssay Description:A continuous assay was used in which the substrate is a synthetic peptide containing a fluorescent group (7-methoxycoumarin), which is quenched by en...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2008
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Pfizer

LigandPNGBDBM50243852(CHEMBL4103698)
Affinity DataIC50: 3nMAssay Description:Inhibition of recombinant human JAK1 using 5'FAM-KKSRGDYMTMQID as substrate in presence of 1 mM ATP by mobility shift assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/19/2019
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Pfizer

LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
Affinity DataIC50: 3.10nMpH: 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 Depth
Date in BDB:
1/23/2017
Entry Details Article
PubMed
TargetNuclear receptor ROR-gamma(Human)
Karo Pharma

Curated by ChEMBL
LigandPNGBDBM50466890(CHEMBL4290728)
Affinity DataIC50: 3.30nMAssay Description:Inverse agonist activity at RORC2 in human Th17 cells assessed as inhibition of IL17A production after 6 days by sandwich ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase BTK(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50357333(CHEMBL1916891)
Affinity DataIC50: 3.31nMAssay Description:Inhibition of BTK relative to controlMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50357322(CHEMBL1916880)
Affinity DataIC50: 3.33nMAssay 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 Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50357339(CHEMBL1916897)
Affinity DataIC50: 3.35nMAssay Description:Inhibition of EGFR preincubated for 60 mins measured after 60 mins by TR-FRET AssayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
LigandPNGBDBM50239505(CHEMBL4061801 | US10329302, Example 248 | US107935...)
Affinity DataIC50: 3.70nMAssay 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 Depth
Date in BDB:
9/22/2019
Entry Details Article
PubMed
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