Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 156 hits for monomerid = 11428,11433,24633,27217,105243,105244,50347388,50347389,50139171   

TargetAldo-keto reductase family 1 member C3(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM50139171(Dinaciclib | MK-7965 | SCH-727965 | US11643396, Ex...)
Affinity DataKi:  70nMAssay Description:Inhibition of human AKR1C3 expressed in Escherichia coli incubated for 30 mins in presence of NADPH regeneration system by UHPLC analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-A2/Cyclin-dependent kinase 2(Homo sapiens (Human))
Vernalis (R&D)

LigandPNGBDBM11428(4-({5-[(4-aminocyclohexyl)amino]-3-(propan-2-yl)py...)
Affinity DataIC50:  59nMpH: 7.5 T: 2°CAssay Description:In vitro kinase assay using purified CDK2/Cyclin A was incubated at room temperature with substrate, and test compounds in the presence of 100 uM ATP...More data for this Ligand-Target Pair
TargetCyclin-A2/Cyclin-dependent kinase 2(Homo sapiens (Human))
Vernalis (R&D)

LigandPNGBDBM11433(4-[(5-{[4-(ethylamino)cyclohexyl]amino}-3-(propan-...)
Affinity DataIC50:  61nMpH: 7.5 T: 2°CAssay Description:In vitro kinase assay using purified CDK2/Cyclin A was incubated at room temperature with substrate, and test compounds in the presence of 100 uM ATP...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 beta(Rattus norvegicus (rat))
Martin-Luther-University Halle-Wittenberg

LigandPNGBDBM11428(4-({5-[(4-aminocyclohexyl)amino]-3-(propan-2-yl)py...)
Affinity DataIC50:  4.00E+4nMT: 2°CAssay Description:In vitro kinase assay using purified GSK-3 beta was incubated at room temperature with substrate, and test compounds in the presence of 10 uM ATP/ [g...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 beta(Rattus norvegicus (rat))
Martin-Luther-University Halle-Wittenberg

LigandPNGBDBM11433(4-[(5-{[4-(ethylamino)cyclohexyl]amino}-3-(propan-...)
Affinity DataIC50: >5.00E+4nMT: 2°CAssay Description:In vitro kinase assay using purified GSK-3 beta was incubated at room temperature with substrate, and test compounds in the presence of 10 uM ATP/ [g...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-A2/Cyclin-dependent kinase 2(Homo sapiens (Human))
Vernalis (R&D)

LigandPNGBDBM24633(5-[(4-aminocyclohexyl)amino]-7-(propan-2-ylamino)p...)
Affinity DataIC50:  30nMpH: 7.2 T: 2°CAssay Description:CDK2/cyclin A activity was determined using a radiometric assay to measure the incorporation of gamma-phosphate from [gamma-33P]-ATP into histone H1....More data for this Ligand-Target Pair
TargetCyclin-dependent kinase/G2/mitotic-specific cyclin- 1(Homo sapiens (Human))
Universite De Lyon

LigandPNGBDBM27217((2R)-2-{[4-(benzylamino)-8-(propan-2-yl)pyrazolo[1...)
Affinity DataIC50:  73nMpH: 7.5 T: 2°CAssay Description:In vitro kinase assay using purified enzyme, was incubated at 30 °C with substrate, and test compounds in the presence of 15 uM ATP/ [gamma-33P]...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-A2/Cyclin-dependent kinase 2(Homo sapiens (Human))
Vernalis (R&D)

LigandPNGBDBM27217((2R)-2-{[4-(benzylamino)-8-(propan-2-yl)pyrazolo[1...)
Affinity DataIC50:  40nMpH: 7.5 T: 2°CAssay Description:In vitro kinase assay using purified enzyme, was incubated at 30 °C with substrate, and test compounds in the presence of 15 uM ATP/ [gamma-33P]...More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 5 activator 1 [99-307](Homo sapiens (Human))
Universite De Lyon

LigandPNGBDBM27217((2R)-2-{[4-(benzylamino)-8-(propan-2-yl)pyrazolo[1...)
Affinity DataIC50:  70nMpH: 7.5 T: 2°CAssay Description:In vitro kinase assay using purified enzyme, was incubated at 30 °C with substrate, and test compounds in the presence of 15 uM ATP/ [gamma-33P]...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-H/Cyclin-dependent kinase 7(Homo sapiens (Human))
Universite De Lyon

LigandPNGBDBM27217((2R)-2-{[4-(benzylamino)-8-(propan-2-yl)pyrazolo[1...)
Affinity DataIC50:  500nMpH: 7.5 T: 2°CAssay Description:In vitro kinase assay using purified enzyme, was incubated at 30 °C with substrate, and test compounds in the presence of 15 uM ATP/ [gamma-33P]...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-T1/Cyclin-dependent kinase 9(Homo sapiens (Human))
Universite De Lyon

LigandPNGBDBM27217((2R)-2-{[4-(benzylamino)-8-(propan-2-yl)pyrazolo[1...)
Affinity DataIC50:  43nMpH: 7.5 T: 2°CAssay Description:In vitro kinase assay using purified enzyme, was incubated at 30 °C with substrate, and test compounds in the presence of 15 uM ATP/ [gamma-33P]...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 2(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM105243(US8580782, 17)
Affinity DataIC50:  5.60E+3nMpH: 8.0Assay Description:CDK2 kinase assays (either cyclin A or cyclin E-dependent) were performed in low protein binding 96-well plates (Corning Inc., Corning, N.Y.).More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCyclin-dependent kinase 2(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM105244(US8580782, 18)
Affinity DataIC50:  140nMpH: 8.0Assay Description:CDK2 kinase assays (either cyclin A or cyclin E-dependent) were performed in low protein binding 96-well plates (Corning Inc., Corning, N.Y.).More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCyclin-T1/Cyclin-dependent kinase 9(Homo sapiens (Human))
Universite De Lyon

LigandPNGBDBM50347388(CHEMBL1234833)
Affinity DataIC50:  90nMAssay Description:Inhibition of CDK9/cyclinT assessed as amount of ATP released by luciferase activity based PKLight assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-H/Cyclin-dependent kinase 7(Homo sapiens (Human))
Universite De Lyon

LigandPNGBDBM50347388(CHEMBL1234833)
Affinity DataIC50:  250nMAssay Description:Inhibition of CDK7/cyclinH/MAT1 assessed as amount of ATP released by luciferase activity based PKLight assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Homo sapiens (Human))
Imperial College

Curated by ChEMBL
LigandPNGBDBM50347388(CHEMBL1234833)
Affinity DataIC50:  2.00E+4nMAssay Description:Inhibition of CDK4/cyclinD1 assessed as amount of ATP released by luciferase activity based PKLight assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 6/G1/S-specific cyclin-D1(Homo sapiens (Human))
Imperial College

Curated by ChEMBL
LigandPNGBDBM50347388(CHEMBL1234833)
Affinity DataIC50:  3.55E+4nMAssay Description:Inhibition of CDK6/cyclinD1 assessed as amount of ATP released by luciferase activity based PKLight assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCalcium/calmodulin-dependent protein kinase kinase 2(Homo sapiens (Human))
Imperial College

Curated by ChEMBL
LigandPNGBDBM50347388(CHEMBL1234833)
Affinity DataIC50:  2.45E+3nMAssay Description:Inhibition of CAMKKbetaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 2/G1/S-specific cyclin-E1(Homo sapiens (Human))
Imperial College

Curated by ChEMBL
LigandPNGBDBM50347388(CHEMBL1234833)
Affinity DataIC50:  3nMAssay Description:Inhibition of CDK2/cyclinE assessed as amount of ATP released by luciferase activity based PKLight assayMore data for this Ligand-Target Pair
TargetCyclin-dependent kinase/G2/mitotic-specific cyclin- 1(Homo sapiens (Human))
Universite De Lyon

LigandPNGBDBM50347388(CHEMBL1234833)
Affinity DataIC50:  33nMAssay Description:Inhibition of CDK1/cyclinB1 assessed as amount of ATP released by luciferase activity based PKLight assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-H/Cyclin-dependent kinase 7(Homo sapiens (Human))
Universite De Lyon

LigandPNGBDBM50347389(CHEMBL1801932)
Affinity DataIC50:  21nMAssay Description:Inhibition of CDK7/cyclinH/MAT1 assessed as amount of ATP released by luciferase activity based PKLight assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase/G2/mitotic-specific cyclin- 1(Homo sapiens (Human))
Universite De Lyon

LigandPNGBDBM50139171(Dinaciclib | MK-7965 | SCH-727965 | US11643396, Ex...)
Affinity DataIC50:  72nMAssay Description:Inhibition of CDK2/Cyclin E (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-3...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 5 activator 1(Homo sapiens (Human))
University Of Tours

Curated by ChEMBL
LigandPNGBDBM50347389(CHEMBL1801932)
Affinity DataIC50:  3.70E+3nMAssay Description:Inhibition of CDK5/p35NCK (unknown origin) using histone H1 as substrate in presence of [gamma-33P]ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 5 activator 1(Homo sapiens (Human))
University Of Tours

Curated by ChEMBL
LigandPNGBDBM50139171(Dinaciclib | MK-7965 | SCH-727965 | US11643396, Ex...)
Affinity DataIC50:  45nMAssay Description:Inhibition of CDK5/p35NCK (unknown origin) using histone H1 as substrate in presence of [gamma-33P]ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Homo sapiens (Human))
Imperial College

Curated by ChEMBL
LigandPNGBDBM50347389(CHEMBL1801932)
Affinity DataIC50:  4.47E+4nMAssay Description:Inhibition of CDK4/Cyclin D1 (unknown origin) using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase/G2/mitotic-specific cyclin- 1(Homo sapiens (Human))
Universite De Lyon

LigandPNGBDBM50347389(CHEMBL1801932)
Affinity DataIC50:  1.40E+4nMAssay Description:Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-3...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Homo sapiens (Human))
Imperial College

Curated by ChEMBL
LigandPNGBDBM50139171(Dinaciclib | MK-7965 | SCH-727965 | US11643396, Ex...)
Affinity DataIC50:  127nMAssay Description:Inhibition of CDK4/Cyclin D1 (unknown origin) using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 5(Homo sapiens (Human))
Palack£

Curated by ChEMBL
LigandPNGBDBM50347389(CHEMBL1801932)
Affinity DataIC50:  3.70E+3nMAssay Description:Inhibition of CDK5 (unknown origin) using histone H1 as substrate in presence of [gamma33P]-ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 5(Homo sapiens (Human))
Palack£

Curated by ChEMBL
LigandPNGBDBM50139171(Dinaciclib | MK-7965 | SCH-727965 | US11643396, Ex...)
Affinity DataIC50:  45nMAssay Description:Inhibition of CDK5 (unknown origin) using histone H1 as substrate in presence of [gamma33P]-ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 2/G1/S-specific cyclin-E1(Homo sapiens (Human))
Imperial College

Curated by ChEMBL
LigandPNGBDBM50347389(CHEMBL1801932)
Affinity DataIC50:  1.80E+3nMAssay Description:Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 2/G1/S-specific cyclin-E1(Homo sapiens (Human))
Imperial College

Curated by ChEMBL
LigandPNGBDBM50139171(Dinaciclib | MK-7965 | SCH-727965 | US11643396, Ex...)
Affinity DataIC50:  2nMAssay Description:Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 9(Homo sapiens (Human))
Palack£

Curated by ChEMBL
LigandPNGBDBM50347389(CHEMBL1801932)
Affinity DataIC50:  2.18E+3nMAssay Description:Inhibition of CDK9 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 9(Homo sapiens (Human))
Palack£

Curated by ChEMBL
LigandPNGBDBM50139171(Dinaciclib | MK-7965 | SCH-727965 | US11643396, Ex...)
Affinity DataIC50:  178nMAssay Description:Inhibition of CDK9 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 7(Homo sapiens (Human))
Palack£

Curated by ChEMBL
LigandPNGBDBM50347389(CHEMBL1801932)
Affinity DataIC50:  134nMAssay Description:Inhibition of CDK7 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 4(Homo sapiens (Human))
Palack£

Curated by ChEMBL
LigandPNGBDBM50347389(CHEMBL1801932)
Affinity DataIC50:  4.47E+4nMAssay Description:Inhibition of CDK4 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 4(Homo sapiens (Human))
Palack£

Curated by ChEMBL
LigandPNGBDBM50139171(Dinaciclib | MK-7965 | SCH-727965 | US11643396, Ex...)
Affinity DataIC50:  127nMAssay Description:Inhibition of CDK4 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 1(Homo sapiens (Human))
Palack£

Curated by ChEMBL
LigandPNGBDBM50347389(CHEMBL1801932)
Affinity DataIC50:  1.40E+4nMAssay Description:Inhibition of CDK1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 1(Homo sapiens (Human))
Palack£

Curated by ChEMBL
LigandPNGBDBM50139171(Dinaciclib | MK-7965 | SCH-727965 | US11643396, Ex...)
Affinity DataIC50:  72nMAssay Description:Inhibition of CDK1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 15(Homo sapiens (Human))
Imperial College

Curated by ChEMBL
LigandPNGBDBM50347388(CHEMBL1234833)
Affinity DataIC50:  330nMAssay Description:Inhibition of ERK8More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin receptor-related protein(Homo sapiens (Human))
Imperial College

Curated by ChEMBL
LigandPNGBDBM50347388(CHEMBL1234833)
Affinity DataIC50:  1.80E+3nMAssay Description:Inhibition of IRRMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Homo sapiens (Human))
Imperial College

Curated by ChEMBL
LigandPNGBDBM50347388(CHEMBL1234833)
Affinity DataIC50:  2.10E+3nMAssay Description:Inhibition of DYRK1AMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 1(Homo sapiens (Human))
Imperial College

Curated by ChEMBL
LigandPNGBDBM50347388(CHEMBL1234833)
Affinity DataIC50:  3.11E+3nMAssay Description:Inhibition of ERK2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 3(Homo sapiens (Human))
Imperial College

Curated by ChEMBL
LigandPNGBDBM50347388(CHEMBL1234833)
Affinity DataIC50:  3.73E+3nMAssay Description:Inhibition of ERK1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCasein kinase I isoform alpha(Homo sapiens (Human))
Imperial College

Curated by ChEMBL
LigandPNGBDBM50347388(CHEMBL1234833)
Affinity DataIC50:  1.04E+3nMAssay Description:Inhibition of CK1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase/G2/mitotic-specific cyclin- 1(Homo sapiens (Human))
Universite De Lyon

LigandPNGBDBM50139171(Dinaciclib | MK-7965 | SCH-727965 | US11643396, Ex...)
Affinity DataIC50:  3nMAssay Description:Inhibition of recombinant CDK1/cyclin B (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated histone H1 as substrat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 5(Homo sapiens (Human))
Palack£

Curated by ChEMBL
LigandPNGBDBM50139171(Dinaciclib | MK-7965 | SCH-727965 | US11643396, Ex...)
Affinity DataIC50:  1nMAssay Description:Inhibition of recombinant CDK5 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated Histone H1 as substrate after 1...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 2(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM50139171(Dinaciclib | MK-7965 | SCH-727965 | US11643396, Ex...)
Affinity DataIC50:  1nMAssay Description:Inhibition of recombinant CDK2 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated Histone H1 as substrate after 1...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 1(Homo sapiens (Human))
Palack£

Curated by ChEMBL
LigandPNGBDBM50139171(Dinaciclib | MK-7965 | SCH-727965 | US11643396, Ex...)
Affinity DataIC50:  3nMAssay Description:Inhibition of recombinant CDK1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated Histone H1 as substrate after 1...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 5 activator 1(Homo sapiens (Human))
University Of Tours

Curated by ChEMBL
LigandPNGBDBM50139171(Dinaciclib | MK-7965 | SCH-727965 | US11643396, Ex...)
Affinity DataIC50:  1nMAssay Description:Inhibition of recombinant CDK5/p25 (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated histone H1 as substrate aft...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-T1/Cyclin-dependent kinase 9(Homo sapiens (Human))
Universite De Lyon

LigandPNGBDBM50139171(Dinaciclib | MK-7965 | SCH-727965 | US11643396, Ex...)
Affinity DataIC50:  4nMAssay Description:Inhibition of recombinant CDK9/cyclin T (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated histone H1 as substrat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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