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Found 3223 with Last Name = 'vajdos' and Initial = 'f'
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
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
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
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
LigandPNGBDBM50406141(CHEMBL5286547)
Affinity DataKi:  1.80E+3nMAssay Description:Antagonistic activity against M2 muscarinic receptor in guinea pig left atrium derived by plotting log(DR - 1) vs log[antagonist]More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM50406139(CHEMBL5281816)
Affinity DataKi:  3.60E+3nMAssay Description:Antagonistic activity against M2 muscarinic receptor in guinea pig left atrium derived by plotting log(DR - 1) vs log[antagonist]More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM50406140(CHEMBL5284779)
Affinity DataKi:  4.00E+3nMAssay Description:Antagonistic activity against M2 muscarinic receptor in guinea pig left atrium derived by plotting log(DR - 1) vs log[antagonist]More data for this Ligand-Target Pair
In DepthDetails PubMed
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
LigandPNGBDBM50406144(CHEMBL5283506)
Affinity DataKi:  1.10E+4nMAssay Description:Antagonistic activity against M2 muscarinic receptor in guinea pig left atrium derived by plotting log(DR - 1) vs log[antagonist]More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM50406145(CHEMBL5287800)
Affinity DataKi:  1.70E+4nMAssay Description:Antagonistic activity against M2 muscarinic receptor in guinea pig left atrium derived by plotting log(DR - 1) vs log[antagonist]More data for this Ligand-Target Pair
In DepthDetails PubMed
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
LigandPNGBDBM50406143(CHEMBL5287916)
Affinity DataKi:  1.90E+4nMAssay Description:Antagonistic activity against M2 muscarinic receptor in guinea pig left atrium derived by plotting log(DR - 1) vs log[antagonist]More data for this Ligand-Target Pair
In DepthDetails PubMed
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
LigandPNGBDBM50406142(CHEMBL5280788)
Affinity DataKi:  3.70E+4nMAssay Description:Antagonistic activity against M2 muscarinic receptor in guinea pig left atrium derived by plotting log(DR - 1) vs log[antagonist]More data for this Ligand-Target Pair
In DepthDetails PubMed
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
TargetBeta-secretase 1(Homo sapiens (Human))
The Scripps Research Institute

Curated by ChEMBL
LigandPNGBDBM160666(US9045498, 8)
Affinity DataIC50:  0.00600nMAssay Description:Inhibition of BACE1 (unknown origin) using biotin-GLTNIKTEEISEISYEVEFR-C[oregon green]KK-OH as substrate after 3 hrs by fluorescence polarization ass...More data for this Ligand-Target Pair
TargetBeta-secretase 1(Homo sapiens (Human))
The Scripps Research Institute

Curated by ChEMBL
LigandPNGBDBM50259962(CHEMBL4088234)
Affinity DataIC50:  0.0240nMAssay Description:Inhibition of BACE1 in human H4 cells expressing wild type APP695 assessed as reduction in soluble APPbeta level after 18 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPantetheinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50585537(CHEMBL5084938)
Affinity DataIC50:  0.0400nMAssay Description:Inhibition of recombinant N-terminal FLAG/His6-tagged human vanin-1 expressed in CHO cells using Pantetheine-7-amino-4-trifluoromethykournarin as sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetPantetheinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM480924(US10906888, Example 138)
Affinity DataIC50:  0.0400nMAssay Description:Inhibition of recombinant N-terminal FLAG/His6-tagged human vanin-1 expressed in CHO cells using Pantetheine-7-amino-4-trifluoromethykournarin as sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetPantetheinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM480965(8-oxa-2-azaspiro[4.5]dec-2-yl(2-{[2-(pyrazin-2-yl)...)
Affinity DataIC50:  0.0600nMAssay Description:Inhibition of recombinant N-terminal FLAG/His6-tagged human vanin-1 expressed in CHO cells using Pantetheine-7-amino-4-trifluoromethykournarin as sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetPantetheinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM480929(8-oxa-2-azaspiro[4.5]dec-2-yl(2-{[2-(pyrimidin-5-y...)
Affinity DataIC50:  0.0800nMAssay Description:Inhibition of recombinant N-terminal FLAG/His6-tagged human vanin-1 expressed in CHO cells using Pantetheine-7-amino-4-trifluoromethykournarin as sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetPantetheinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM480917(7-oxa-2-azaspiro[3.5]non-2-yl(2-{[2-(pyrazin-2-yl)...)
Affinity DataIC50:  0.110nMAssay Description:Inhibition of recombinant N-terminal FLAG/His6-tagged human vanin-1 expressed in CHO cells using Pantetheine-7-amino-4-trifluoromethykournarin as sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetPantetheinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM480956(US10906888, Example 173)
Affinity DataIC50:  0.120nMAssay Description:Inhibition of recombinant N-terminal FLAG/His6-tagged human vanin-1 expressed in CHO cells using Pantetheine-7-amino-4-trifluoromethykournarin as sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetAcetyl-CoA carboxylase 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50314930(1-(2-(1-methyl-1H-pyrazol-3-yl)-1H-benzo[d]imidazo...)
Affinity DataIC50:  0.210nMAssay Description:Inhibition of human recombinant ACC2 expressed in CHO cells after 1 hr by fluorescence readerMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPantetheinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM480931(8-oxa-2-azaspiro[4.5]dec-2-yl(2-{[(1S)-1-(pyrazin-...)
Affinity DataIC50:  0.240nMAssay Description:Inhibition of recombinant N-terminal FLAG/His6-tagged human vanin-1 expressed in CHO cells using Pantetheine-7-amino-4-trifluoromethykournarin as sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetPantetheinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM480971(8-oxa-2-azaspiro[4.5]dec-2-yl(2-{[1-(pyrimidin-5-y...)
Affinity DataIC50:  0.280nMAssay Description:Inhibition of recombinant N-terminal FLAG/His6-tagged human vanin-1 expressed in CHO cells using Pantetheine-7-amino-4-trifluoromethykournarin as sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetAcetyl-CoA carboxylase 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50314931(1-(7-methyl-1H-indazole-5-carbonyl)-6'-(1-methyl-1...)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of human recombinant ACC2 expressed in CHO cells after 1 hr by fluorescence readerMore 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:  0.300nMAssay Description:Inhibition of recombinant human GST-tagged JAK3 JH1 domain using KAIETDKEYYTVKD-NH2 as substrate in presence of ATP at Km concentration by coupled PK...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:  0.300nMAssay 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
TargetAcetyl-CoA carboxylase 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50314932(6'-methoxy-1-(7-methyl-1H-indazole-5-carbonyl)spir...)
Affinity DataIC50:  0.310nMAssay Description:Inhibition of human recombinant ACC2 expressed in CHO cells after 1 hr by fluorescence readerMore 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
TargetPantetheinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM480918(US10906888, Example 132)
Affinity DataIC50:  0.350nMAssay Description:Inhibition of recombinant N-terminal FLAG/His6-tagged human vanin-1 expressed in CHO cells using Pantetheine-7-amino-4-trifluoromethykournarin as sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
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
TargetPantetheinase(Mus musculus)
Pfizer

Curated by ChEMBL
LigandPNGBDBM480917(7-oxa-2-azaspiro[3.5]non-2-yl(2-{[2-(pyrazin-2-yl)...)
Affinity DataIC50:  0.410nMAssay Description:Inhibition of mouse vanin-1More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetPantetheinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM480919(US10906888, Example 133)
Affinity DataIC50:  0.430nMAssay Description:Inhibition of recombinant N-terminal FLAG/His6-tagged human vanin-1 expressed in CHO cells using Pantetheine-7-amino-4-trifluoromethykournarin as sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50466664(CHEMBL4292341)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of recombinant human GST-tagged JAK3 JH1 domain using KAIETDKEYYTVKD-NH2 as substrate in presence of ATP at Km concentration by coupled PK...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50466668(CHEMBL4280180)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of recombinant human GST-tagged JAK3 JH1 domain using KAIETDKEYYTVKD-NH2 as substrate in presence of ATP at Km concentration by coupled PK...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50466679(CHEMBL4288086)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of recombinant human GST-tagged JAK3 JH1 domain using KAIETDKEYYTVKD-NH2 as substrate in presence of ATP at Km concentration by coupled PK...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
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