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Found 158 with Last Name = 'geoghegan' and Initial = 'kf'
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
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
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
TargetCytochrome P450 3A4(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50088503(CHEMBL3527048)
Affinity DataKi:  120nMAssay Description:Inhibition of midazolam 1'-hydroxylase activity of human recombinant CYP3A4 harboring human P450 oxidoreductase and b5 assessed as decrease in enzyme...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50088503(CHEMBL3527048)
Affinity DataKi:  170nMAssay Description:Inhibition of testosterone 6beta-hydroxylase activity of human recombinant CYP3A4 in presence of human P450 oxidoreductase and b5 assessed as decreas...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A5(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50088503(CHEMBL3527048)
Affinity DataKi:  1.20E+3nMAssay Description:Inhibition of testosterone 6beta-hydroxylase activity of human recombinant CYP3A5 in presence of human P450 oxidoreductase and b5 assessed as decreas...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A5(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50088503(CHEMBL3527048)
Affinity DataKi:  2.00E+3nMAssay Description:Inhibition of midazolam 1'-hydroxylase activity of human recombinant CYP3A5 harboring human P450 oxidoreductase and b5 assessed as decrease in enzyme...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

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
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
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
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM159756(PF-02384554 | US10966980, Example 8 | US9035074, 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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
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
LigandPNGBDBM50113040((2R,4R)-1-[4-(4-Fluoro-benzyloxy)-benzenesulfonyl]...)
Affinity DataIC50:  5nMAssay Description:Inhibitory concentration against recombinant tumor necrosis factor alpha converting enzyme More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50113041((2R,5R)-5-Hydroxy-1-[4-(2-trifluoromethyl-benzylox...)
Affinity DataIC50:  5nMAssay Description:Inhibitory concentration against recombinant tumor necrosis factor alpha converting enzyme More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLiver carboxylesterase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM195575((R)-(3-(4-(2-morpholinopyrimidin-5-yl)phenyl)-1H-1...)
Affinity DataIC50:  5nMpH: 7.5Assay Description:For determination of IC50 values for CES1 inhibitors, the reactions were carried out in 1.5 mL microcentrifuge tubes in a total reaction volume of 25...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLiver carboxylesterase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM195574((R)-(2-phenylpiperidin-1-yl)(3-(4-(pyridin-3-yl)ph...)
Affinity DataIC50:  5nMpH: 7.5Assay Description:For determination of IC50 values for CES1 inhibitors, the reactions were carried out in 1.5 mL microcentrifuge tubes in a total reaction volume of 25...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLiver carboxylesterase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM195572((R)-N,N-dimethyl-4'-(2-(2-phenylpiperidine-1-c...)
Affinity DataIC50: <5nMpH: 7.5Assay Description:For determination of IC50 values for CES1 inhibitors, the reactions were carried out in 1.5 mL microcentrifuge tubes in a total reaction volume of 25...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLiver carboxylesterase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM195571((R)-4'-(2-(2-phenylpiperidine-1-carbonyl)-2H-1...)
Affinity DataIC50: <5nMpH: 7.5Assay Description:For determination of IC50 values for CES1 inhibitors, the reactions were carried out in 1.5 mL microcentrifuge tubes in a total reaction volume of 25...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLiver carboxylesterase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM195570((S)-4'-(2-(2-phenylpiperidine-1-carbonyl)-2H-1...)
Affinity DataIC50: <5nMpH: 7.5Assay Description:For determination of IC50 values for CES1 inhibitors, the reactions were carried out in 1.5 mL microcentrifuge tubes in a total reaction volume of 25...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLysophospholipase-like protein 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM195581((2R,3R)-2-(3-ethynylphenyl)-1-(3-(4-(2-morpholinop...)
Affinity DataIC50:  5nMpH: 7.5Assay Description:For determination of IC50 values for LYPLAL1 inhibitors, the reactions were carried out in 1.5 mL microcentrifuge tubes in a total reaction volume of...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50113028((2R,4S)-4-Hydroxy-1-[4-(2-methyl-benzyloxy)-benzen...)
Affinity DataIC50:  6nMAssay Description:Inhibitory concentration against recombinant tumor necrosis factor alpha converting enzyme More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysophospholipase-like protein 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM195580((2R,3R)-1-(3-(4-(2-morpholinopyrimidin-5-yl)phenyl...)
Affinity DataIC50:  6nMpH: 7.5Assay Description:For determination of IC50 values for LYPLAL1 inhibitors, the reactions were carried out in 1.5 mL microcentrifuge tubes in a total reaction volume of...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50113035((2R,4S)-1-[4-(4-Chloro-benzyloxy)-benzenesulfonyl]...)
Affinity DataIC50:  7nMAssay Description:Inhibitory concentration against recombinant tumor necrosis factor alpha converting enzyme More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLiver carboxylesterase 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM195573((R)-4'-(1-(2-phenylpiperidine-1-carbonyl)-1H-1...)
Affinity DataIC50:  7nMpH: 7.5Assay Description:For determination of IC50 values for CES1 inhibitors, the reactions were carried out in 1.5 mL microcentrifuge tubes in a total reaction volume of 25...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50113046((2R,5R)-5-Hydroxy-1-[4-(2-iodo-benzyloxy)-benzenes...)
Affinity DataIC50:  7nMAssay Description:Inhibitory concentration against recombinant tumor necrosis factor alpha converting enzyme More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50113048((2R,5R)-1-(4-Benzyloxy-benzenesulfonyl)-5-hydroxy-...)
Affinity DataIC50:  7nMAssay Description:Inhibitory concentration against recombinant tumor necrosis factor alpha converting enzyme More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysophospholipase-like protein 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM195575((R)-(3-(4-(2-morpholinopyrimidin-5-yl)phenyl)-1H-1...)
Affinity DataIC50:  7nMpH: 7.5Assay Description:For determination of IC50 values for LYPLAL1 inhibitors, the reactions were carried out in 1.5 mL microcentrifuge tubes in a total reaction volume of...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50113044((2R,5R)-5-Hydroxy-1-[4-(2-methyl-benzyloxy)-benzen...)
Affinity DataIC50:  8nMAssay Description:Inhibitory concentration against recombinant tumor necrosis factor alpha converting enzyme More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInterstitial collagenase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50113029((2R,4R)-1-[4-(4-Fluoro-phenoxy)-benzenesulfonyl]-2...)
Affinity DataIC50:  8.5nMAssay Description:Inhibitory concentration of the compound against Matrix metalloproteinase-1 was determinedMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50113038((2R,4S)-1-(4-Benzyloxy-benzenesulfonyl)-4-hydroxy-...)
Affinity DataIC50:  9nMAssay Description:Inhibitory concentration against recombinant tumor necrosis factor alpha converting enzyme More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50113037((2R,5R)-5-Hydroxy-1-[4-(4-trifluoromethyl-benzylox...)
Affinity DataIC50:  10nMAssay Description:Inhibitory concentration against recombinant tumor necrosis factor alpha converting enzyme More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50113034((2R,4S)-1-[4-(3-Chloro-benzyloxy)-benzenesulfonyl]...)
Affinity DataIC50:  10nMAssay Description:Inhibitory concentration against recombinant tumor necrosis factor alpha converting enzyme More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50113045((2R,5R)-1-[4-(2-Ethyl-benzyloxy)-benzenesulfonyl]-...)
Affinity DataIC50:  10nMAssay Description:Inhibitory concentration against recombinant tumor necrosis factor alpha converting enzyme More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysophospholipase-like protein 1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM195578((2R, 4R)-1-(3-(4-(2-morpholinopyrimidin-5-yl)pheny...)
Affinity DataIC50:  11nMpH: 7.5Assay Description:For determination of IC50 values for LYPLAL1 inhibitors, the reactions were carried out in 1.5 mL microcentrifuge tubes in a total reaction volume of...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50113039((2R,5R)-5-Hydroxy-1-[4-(2-isopropyl-benzyloxy)-ben...)
Affinity DataIC50:  11nMAssay Description:Inhibitory concentration against recombinant tumor necrosis factor alpha converting enzyme More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50113047((2R,4S)-4-Hydroxy-1-[4-(2-methoxy-benzyloxy)-benze...)
Affinity DataIC50:  14nMAssay Description:Inhibitory concentration against recombinant tumor necrosis factor alpha converting enzyme More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50113024((2R,4S)-1-[4-(4-Fluoro-benzyloxy)-benzenesulfonyl]...)
Affinity DataIC50:  14nMAssay Description:Inhibitory concentration against recombinant tumor necrosis factor alpha converting enzyme More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Pfizer

LigandPNGBDBM50193995(3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyr...)
Affinity DataIC50:  15nMpH: 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
LigandPNGBDBM50113033((2R,5R)-5-Hydroxy-1-[4-(3-trifluoromethyl-benzylox...)
Affinity DataIC50:  15nMAssay Description:Inhibitory concentration against recombinant tumor necrosis factor alpha converting enzyme More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50113021((2R,4S)-1-[4-(3-Cyano-benzyloxy)-benzenesulfonyl]-...)
Affinity DataIC50:  15nMAssay Description:Inhibitory concentration against recombinant tumor necrosis factor alpha converting enzyme More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50113025((2R,5R)-5-Hydroxy-1-[4-(naphthalen-1-ylmethoxy)-be...)
Affinity DataIC50:  16nMAssay Description:Inhibitory concentration against recombinant tumor necrosis factor alpha converting enzyme More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50113027((2R,4S)-4-Hydroxy-1-[4-(2-trifluoromethyl-benzylox...)
Affinity DataIC50:  16nMAssay Description:Inhibitory concentration against recombinant tumor necrosis factor alpha converting enzyme More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50113023((2R,4S)-4-Hydroxy-1-[4-(3-methyl-benzyloxy)-benzen...)
Affinity DataIC50:  18nMAssay Description:Inhibitory concentration against recombinant tumor necrosis factor alpha converting enzyme More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInterstitial collagenase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50113049((2R,4R)-2-Hydroxycarbamoyl-1-(4-methoxy-benzenesul...)
Affinity DataIC50:  19nMAssay Description:Inhibitory concentration of the compound against Matrix metalloproteinase-1 was determinedMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50113030((2R,4S)-4-Hydroxy-1-[4-(4-methyl-benzyloxy)-benzen...)
Affinity DataIC50:  20nMAssay Description:Inhibitory concentration against recombinant tumor necrosis factor alpha converting enzyme More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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