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Found 246 with Last Name = 'bower' and Initial = 'mj'
TargetCyclin-A2/Cyclin-dependent kinase 1(Homo sapiens (Human))
Glaxosmithkline

LigandPNGBDBM2579((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Affinity DataKi:  1nM ΔG°:  -50.9kJ/molepH: 7.4 T: 2°CAssay Description:In vitro CDK enzymatic assay using purified CDK mixed with cyclin A, was incubated with substrate, and test compounds in the presence of 1.4 uM ATP/ ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-A2/Cyclin-dependent kinase 2(Homo sapiens (Human))
Glaxosmithkline

LigandPNGBDBM2579((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Affinity DataKi:  2.90nM ΔG°:  -48.2kJ/molepH: 7.4 T: 2°CAssay Description:In vitro CDK enzymatic assay using purified CDK mixed with cyclin A, was incubated with substrate, and test compounds in the presence of 1.4 uM ATP/ ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Glaxosmithkline

LigandPNGBDBM17054((2S,3R,4R,6R,18R)-18-hydroxy-3-methoxy-2-methyl-4-...)
Affinity DataKi:  5.60nM ΔG°:  -49.0kJ/molepH: 7.4 T: 2°CAssay Description:In vitro Chk1 enzymatic assay using purified enzyme, was incubated with substrate, and test compounds in the presence of 10 uM ATP/ [gamma-32P] ATP. ...More data for this Ligand-Target Pair
TargetCyclin-A2/Cyclin-dependent kinase 2(Homo sapiens (Human))
Glaxosmithkline

LigandPNGBDBM17140((15R,18R)-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1...)
Affinity DataKi:  5.60nM ΔG°:  -46.6kJ/molepH: 7.4 T: 2°CAssay Description:In vitro CDK enzymatic assay using purified CDK mixed with cyclin A, was incubated with substrate, and test compounds in the presence of 1.4 uM ATP/ ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Glaxosmithkline

LigandPNGBDBM2579((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Affinity DataKi:  7.80nM ΔG°:  -48.1kJ/molepH: 7.4 T: 2°CAssay Description:In vitro Chk1 enzymatic assay using purified enzyme, was incubated with substrate, and test compounds in the presence of 10 uM ATP/ [gamma-32P] ATP. ...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Glaxosmithkline

LigandPNGBDBM17140((15R,18R)-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1...)
Affinity DataKi:  15nM ΔG°:  -46.5kJ/molepH: 7.4 T: 2°CAssay Description:In vitro Chk1 enzymatic assay using purified enzyme, was incubated with substrate, and test compounds in the presence of 10 uM ATP/ [gamma-32P] ATP. ...More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Homo sapiens (Human))
Glaxosmithkline

LigandPNGBDBM17140((15R,18R)-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1...)
Affinity DataKi:  16nM ΔG°:  -45.2kJ/molepH: 7.5 T: 2°CAssay Description:CDK4 and cyclin D1 were expressed in a baculovirus expression system and subsequently purified. The catalytic activity of the CDK4 protein was assaye...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-A2/Cyclin-dependent kinase 1(Homo sapiens (Human))
Glaxosmithkline

LigandPNGBDBM17140((15R,18R)-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1...)
Affinity DataKi:  23nM ΔG°:  -43.2kJ/molepH: 7.4 T: 2°CAssay Description:In vitro CDK enzymatic assay using purified CDK mixed with cyclin A, was incubated with substrate, and test compounds in the presence of 1.4 uM ATP/ ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-A2/Cyclin-dependent kinase 2(Homo sapiens (Human))
Glaxosmithkline

LigandPNGBDBM17054((2S,3R,4R,6R,18R)-18-hydroxy-3-methoxy-2-methyl-4-...)
Affinity DataKi:  30nM ΔG°:  -42.5kJ/molepH: 7.4 T: 2°CAssay Description:In vitro CDK enzymatic assay using purified CDK mixed with cyclin A, was incubated with substrate, and test compounds in the presence of 1.4 uM ATP/ ...More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Homo sapiens (Human))
Glaxosmithkline

LigandPNGBDBM2579((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Affinity DataKi:  41nM ΔG°:  -42.9kJ/molepH: 7.5 T: 2°CAssay Description:CDK4 and cyclin D1 were expressed in a baculovirus expression system and subsequently purified. The catalytic activity of the CDK4 protein was assaye...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-A2/Cyclin-dependent kinase 1(Homo sapiens (Human))
Glaxosmithkline

LigandPNGBDBM17054((2S,3R,4R,6R,18R)-18-hydroxy-3-methoxy-2-methyl-4-...)
Affinity DataKi:  95nM ΔG°:  -39.7kJ/molepH: 7.4 T: 2°CAssay Description:In vitro CDK enzymatic assay using purified CDK mixed with cyclin A, was incubated with substrate, and test compounds in the presence of 1.4 uM ATP/ ...More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Homo sapiens (Human))
Glaxosmithkline

LigandPNGBDBM17054((2S,3R,4R,6R,18R)-18-hydroxy-3-methoxy-2-methyl-4-...)
Affinity DataKi:  3.60E+3nM ΔG°:  -31.6kJ/molepH: 7.5 T: 2°CAssay Description:CDK4 and cyclin D1 were expressed in a baculovirus expression system and subsequently purified. The catalytic activity of the CDK4 protein was assaye...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125902(US8765727, 5)
Affinity DataIC50:  1.90nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125902(US8765727, 5)
Affinity DataIC50:  2.40nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125902(US8765727, 5)
Affinity DataIC50:  4.20nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125913(US8765727, 16)
Affinity DataIC50:  5nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50099348(2-(2,4-Dimethyl-phenoxy)-4-[5-(4-fluoro-phenyl)-3-...)
Affinity DataIC50:  6nMAssay Description:Inhibitory concentration against mitogen-activated protein kinase p38 alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125904(US8765727, 7)
Affinity DataIC50:  6.40nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50099358(2-{4-[5-(4-Fluoro-phenyl)-3-piperidin-4-yl-3H-imid...)
Affinity DataIC50:  6.60nMAssay Description:Inhibitory concentration against mitogen-activated protein kinase p38 alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50099373(2-(4-Ethyl-phenoxy)-4-[5-(4-fluoro-phenyl)-3-piper...)
Affinity DataIC50:  7.40nMAssay Description:Inhibitory concentration against mitogen-activated protein kinase p38 alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125904(US8765727, 7)
Affinity DataIC50:  8.30nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125899(US8765727, 2)
Affinity DataIC50:  9.20nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125899(US8765727, 2)
Affinity DataIC50:  10nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50099345(2-(2,5-Dimethyl-phenoxy)-4-[5-(4-fluoro-phenyl)-3-...)
Affinity DataIC50:  11nMAssay Description:Inhibitory concentration against mitogen-activated protein kinase p38 alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125899(US8765727, 2)
Affinity DataIC50:  13nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50099343(2-(2-Fluoro-phenoxy)-4-[5-(4-fluoro-phenyl)-3-pipe...)
Affinity DataIC50:  13nMAssay Description:Inhibitory concentration against mitogen-activated protein kinase p38 alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50099367(4-{4-[5-(4-Fluoro-phenyl)-3-piperidin-4-yl-3H-imid...)
Affinity DataIC50:  14nMAssay Description:Inhibitory concentration against mitogen-activated protein kinase p38 alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125913(US8765727, 16)
Affinity DataIC50:  15nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125913(US8765727, 16)
Affinity DataIC50:  15nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50099342(4-[5-(4-Fluoro-phenyl)-3-piperidin-4-yl-3H-imidazo...)
Affinity DataIC50:  15nMAssay Description:Inhibitory concentration against mitogen-activated protein kinase p38 alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50099349(2-(2,3-Dimethyl-phenoxy)-4-[5-(4-fluoro-phenyl)-3-...)
Affinity DataIC50:  15nMAssay Description:Inhibitory concentration against mitogen-activated protein kinase p38 alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50099355(4-[5-(4-Fluoro-phenyl)-3-piperidin-4-yl-3H-imidazo...)
Affinity DataIC50:  16nMAssay Description:Inhibitory concentration against mitogen-activated protein kinase p38 alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50125604(1-[9-Benzyl-2-(2-fluoro-phenyl)-9H-purin-6-yl]-1-(...)
Affinity DataIC50:  16nMAssay Description:Inhibition of human MAP p38-alpha kinase in vitro.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125904(US8765727, 7)
Affinity DataIC50:  16nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125898(US8765727, 1)
Affinity DataIC50:  17nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50099352(4-[5-(4-Fluoro-phenyl)-3-piperidin-4-yl-3H-imidazo...)
Affinity DataIC50:  19nMAssay Description:Inhibitory concentration against mitogen-activated protein kinase p38 alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50099374(4-[5-(4-Fluoro-phenyl)-3-piperidin-4-yl-3H-imidazo...)
Affinity DataIC50:  19nMAssay Description:Inhibitory concentration against mitogen-activated protein kinase p38 alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50099341(4-[5-(4-Fluoro-phenyl)-3-piperidin-4-yl-3H-imidazo...)
Affinity DataIC50:  19nMAssay Description:Inhibitory concentration against mitogen-activated protein kinase p38 alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM15239(4-[4-(4-fluorophenyl)-1-(piperidin-4-yl)-1H-imidaz...)
Affinity DataIC50:  20nMAssay Description:Inhibitory concentration against mitogen-activated protein kinase p38 alphaMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50099344(3-{4-[5-(4-Fluoro-phenyl)-3-piperidin-4-yl-3H-imid...)
Affinity DataIC50:  20nMAssay Description:Inhibitory concentration against mitogen-activated protein kinase p38 alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125901(US8765727, 4)
Affinity DataIC50:  21nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetTyrosine-protein phosphatase non-receptor type 1(Homo sapiens (Human))
Incyte

Curated by ChEMBL
LigandPNGBDBM50228014(2-[4-((R)-2-{1-(3-fluoro-benzenesulfonylamino)-2-[...)
Affinity DataIC50:  22nMAssay Description:Inhibition of PTP1B by pNPP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50099347(2-(3,4-Dimethyl-phenoxy)-4-[5-(4-fluoro-phenyl)-3-...)
Affinity DataIC50:  22nMAssay Description:Inhibitory concentration against mitogen-activated protein kinase p38 alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein phosphatase non-receptor type 1(Homo sapiens (Human))
Incyte

Curated by ChEMBL
LigandPNGBDBM50228013(3-fluoro-N-{1-{(R)-5-[2-(3-methanesulfonyl-phenoxy...)
Affinity DataIC50:  23nMAssay Description:Inhibition of PTP1B by pNPP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125906(US8765727, 9)
Affinity DataIC50:  23nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50099338(2-(Benzo[1,3]dioxol-5-yloxy)-4-[5-(4-fluoro-phenyl...)
Affinity DataIC50:  23nMAssay Description:Inhibitory concentration against mitogen-activated protein kinase p38 alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein phosphatase non-receptor type 2(Homo sapiens (Human))
Incyte

Curated by ChEMBL
LigandPNGBDBM50228024(3-fluoro-N-{1-[5-(3-phenyl-propyl)-1H-imidazol-2-y...)
Affinity DataIC50:  24nMAssay Description:Inhibition of TCPTP by pNPP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein phosphatase non-receptor type 2(Homo sapiens (Human))
Incyte

Curated by ChEMBL
LigandPNGBDBM50228013(3-fluoro-N-{1-{(R)-5-[2-(3-methanesulfonyl-phenoxy...)
Affinity DataIC50:  25nMAssay Description:Inhibition of TCPTP by pNPP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125910(US8765727, 13)
Affinity DataIC50:  25nMpH: 7.8 T: 2°CAssay Description:One or more compounds herein were tested for inhibitory activity of JAK targets according to the following in vitro assay described in Park et al., A...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Incyte

US Patent
LigandPNGBDBM125902(US8765727, 5)
Affinity DataIC50:  25nMAssay Description:TYK2 assays described by James E. Thompson et. al, Photochemical preparation of a pyridone containing tetracycle: A JAK protein kinase inhibitor, Bio...More data for this Ligand-Target Pair
In DepthDetails US Patent
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