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TargetCyclin-dependent kinase 8(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50189412(CHEMBL3827983)
Affinity DataIC50: 0.200nMAssay Description:Binding affinity to CDK8 (unknown origin) expressed in human 7dF3 cells preincubated for 2 hrs followed by beta-oestradiol addition measured after 24...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2017
Entry Details Article
PubMed
LigandPNGBDBM25041(N'-[(1E)-{6-cyanoimidazo[1,2-a]pyridin-3-yl}methyl...)
Affinity DataIC50: 0.260nMpH: 7.4 T: 2°CAssay Description:The test compounds and enzyme were mixed in buffer, and the substrate and [gamma-33P] ATP/ATP were added to the mixture to initiate the reaction. Aft...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/26/2008
Entry Details Article
PubMed
LigandPNGBDBM25036(CHEMBL393525 | N'-[(1E)-{6-bromoimidazo[1,2-a]pyri...)
Affinity DataIC50: 0.300nMpH: 7.4 T: 2°CAssay Description:The test compounds and enzyme were mixed in buffer, and the substrate and [gamma-33P] ATP/ATP were added to the mixture to initiate the reaction. Aft...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/26/2008
Entry Details Article
PubMed
LigandPNGBDBM15131(5-{5-[(2S)-2-amino-3-(1H-indol-3-yl)propoxy]pyridi...)
Affinity DataIC50: 0.5nMpH: 7.2 T: 2°CAssay Description:The purified PKB beta enzyme was assayed with a peptide substrate and test compound in the presence of 30 uM ATP/ [gamma-33P]ATP in 96-well plates. I...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/30/2007
Entry Details Article
PubMed
TargetCyclin-dependent kinase 8(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50189417(CHEMBL3828116)
Affinity DataIC50: 0.5nMAssay Description:Binding affinity to CDK8 (unknown origin) expressed in human 7dF3 cells preincubated for 2 hrs followed by beta-oestradiol addition measured after 24...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2017
Entry Details Article
PubMed
TargetCyclin-dependent kinase 8(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50189435(CHEMBL3828003)
Affinity DataIC50: 0.600nMAssay Description:Binding affinity to CDK8 (unknown origin) expressed in human 7dF3 cells preincubated for 2 hrs followed by beta-oestradiol addition measured after 24...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2017
Entry Details Article
PubMed
TargetCyclin-C(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50189434(CHEMBL3828221)
Affinity DataIC50: 0.710nMAssay Description:Competitive binding affinity to full length His-tagged human recombinant CDK8/cyclin C expressed in baculovirus after 20 mins in presence of Alexa647...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2017
Entry Details Article
PubMed
LigandPNGBDBM25037(N'-[(1E)-{6-chloroimidazo[1,2-a]pyridin-3-yl}methy...)
Affinity DataIC50: 0.770nMpH: 7.4 T: 2°CAssay Description:The test compounds and enzyme were mixed in buffer, and the substrate and [gamma-33P] ATP/ATP were added to the mixture to initiate the reaction. Aft...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/26/2008
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase PLK1(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50: 0.830nMAssay Description:Inhibition of PLK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMed
TargetCyclin-C(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50189415(CHEMBL3828637)
Affinity DataIC50: 0.900nMAssay Description:Competitive binding affinity to full length His-tagged human recombinant CDK8/cyclin C expressed in baculovirus after 20 mins in presence of Alexa647...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2017
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase B-raf(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50430022(CHEMBL2144069)
Affinity DataIC50: 1nMAssay Description:Inhibition of recombinant human GST-tagged BRAF V600E mutant expressed in baculovirus expression systemMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCyclin-C(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50189428(CHEMBL3828458)
Affinity DataIC50: 1nMAssay Description:Competitive binding affinity to full length His-tagged human recombinant CDK8/cyclin C expressed in baculovirus after 20 mins in presence of Alexa647...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2017
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase B-raf(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50428286(GSK2118436A | DABRAFENIB)
Affinity DataIC50: 1nMAssay Description:Inhibition of recombinant human GST-tagged BRAF V600E mutant expressed in baculovirus expression systemMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetSerine/threonine-protein kinase B-raf(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50029085(CHEBI:83405 | GDC-0879 | CHEMBL525191)
Affinity DataIC50: 1nMAssay Description:Inhibition of recombinant human GST-tagged BRAF V600E mutant expressed in baculovirus expression systemMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMed
TargetCyclin-dependent kinase 8(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50189436(CHEMBL3827327)
Affinity DataIC50: 1.10nMAssay Description:Binding affinity to CDK8 (unknown origin) expressed in human 7dF3 cells preincubated for 2 hrs followed by beta-oestradiol addition measured after 24...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2017
Entry Details Article
PubMed
TargetCyclin-C(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50189447(CHEMBL3828553)
Affinity DataIC50: 1.10nMAssay Description:Competitive binding affinity to full length His-tagged human recombinant CDK8/cyclin C expressed in baculovirus after 20 mins in presence of Alexa647...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2017
Entry Details Article
PubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50335609(3-((4-(6-bromo-2-(4-(4-methylpiperazin-1-yl)phenyl...)
Affinity DataKd:  1.20nMAssay Description:Binding affinity to FLT3More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetCyclin-C(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50189417(CHEMBL3828116)
Affinity DataIC50: 1.5nMAssay Description:Competitive binding affinity to full length His-tagged human recombinant CDK8/cyclin C expressed in baculovirus after 20 mins in presence of Alexa647...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2017
Entry Details Article
PubMed
TargetCyclin-dependent kinase 8(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50163767(CHEMBL3798944)
Affinity DataIC50: 1.60nMAssay Description:Binding affinity to His-tagged CDK8 (unknown origin) after 60 mins by FRET based lanthascreen binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/10/2017
Entry Details Article
PubMed
TargetCyclin-dependent kinase 8(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50189415(CHEMBL3828637)
Affinity DataIC50: 1.70nMAssay Description:Binding affinity to CDK8 (unknown origin) expressed in human 7dF3 cells preincubated for 2 hrs followed by beta-oestradiol addition measured after 24...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2017
Entry Details Article
PubMed
TargetCyclin-dependent kinase 8(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50163774(CHEMBL3797855)
Affinity DataIC50: 1.70nMAssay Description:Binding affinity to His-tagged CDK8 (unknown origin) after 60 mins by FRET based lanthascreen binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/10/2017
Entry Details Article
PubMed
TargetCyclin-C(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50189426(CHEMBL3827944)
Affinity DataIC50: 1.80nMAssay Description:Competitive binding affinity to full length His-tagged human recombinant CDK8/cyclin C expressed in baculovirus after 20 mins in presence of Alexa647...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2017
Entry Details Article
PubMed
LigandPNGBDBM25052(3-{6-bromoimidazo[1,2-a]pyridin-3-yl}-1-[(2-methyl...)
Affinity DataIC50: 1.80nMpH: 7.4 T: 2°CAssay Description:The test compounds and enzyme were mixed in buffer, and the substrate and [gamma-33P] ATP/ATP were added to the mixture to initiate the reaction. Aft...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/27/2008
Entry Details Article
PubMed
TargetCyclin-dependent kinase 8(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50163857(CHEMBL3798853)
Affinity DataIC50: 1.90nMAssay Description:Binding affinity to His-tagged CDK8 (unknown origin) after 60 mins by FRET based lanthascreen binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/10/2017
Entry Details Article
PubMed
TargetAurora kinase B(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50443493(CHEMBL3087777)
Affinity DataIC50: 2nMAssay Description:Inhibition of full-length aurora-B (unknown origin) using 5FAMLRRASLG-CONH2 as substrate after 60 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/25/2014
Entry Details Article
PubMed
LigandPNGBDBM31767(3-(4-morpholinopyrido[2,3]furo[2,4-b]pyrimidin-2-y...)
Affinity DataIC50: 2nMAssay Description:Inhibition of GST-tagged Ptdlns3p P110alpha (unknown origin) expressed in baculovirus infected insect cells incubated for 15 mins in presence of ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetCyclin-dependent kinase 8(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50189420(CHEMBL3827799)
Affinity DataIC50: 2nMAssay Description:Binding affinity to CDK8 (unknown origin) expressed in human 7dF3 cells preincubated for 2 hrs followed by beta-oestradiol addition measured after 24...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2017
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase B-raf(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM99471(US8497274, 32)
Affinity DataIC50: 2nMAssay Description:Inhibition of recombinant human GST-tagged BRAF V600E mutant expressed in baculovirus expression systemMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetAurora kinase A(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50318595(6-Bromo-7-[4-(5-methyl-isoxazol-3-ylmethyl)-pipera...)
Affinity DataIC50: 2nMAssay Description:Inhibition of human recombinant Aurora A expressed in baculovirus systemMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/31/2012
Entry Details Article
PubMed
LigandPNGBDBM31767(3-(4-morpholinopyrido[2,3]furo[2,4-b]pyrimidin-2-y...)
Affinity DataIC50: 2nMAssay Description:Inhibition of human recombinant PI3Kalpha in the presence of ATP by scintillation proximity radiometric assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetCyclin-C(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50189436(CHEMBL3827327)
Affinity DataIC50: 2.10nMAssay Description:Competitive binding affinity to full length His-tagged human recombinant CDK8/cyclin C expressed in baculovirus after 20 mins in presence of Alexa647...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2017
Entry Details Article
PubMed
TargetCyclin-dependent kinase 8(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50163854(CHEMBL3799581)
Affinity DataIC50: 2.10nMAssay Description:Binding affinity to His-tagged CDK8 (unknown origin) after 60 mins by FRET based lanthascreen binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/10/2017
Entry Details Article
PubMed
TargetCyclin-dependent kinase 8(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50163795(CHEMBL3798382)
Affinity DataIC50: 2.30nMAssay Description:Binding affinity to His-tagged CDK8 (unknown origin) after 60 mins by FRET based lanthascreen binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/10/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCyclin-dependent kinase 8(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50163777(CHEMBL3799307)
Affinity DataIC50: 2.30nMAssay Description:Binding affinity to His-tagged CDK8 (unknown origin) after 60 mins by FRET based lanthascreen binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/10/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCyclin-dependent kinase 8(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50163855(CHEMBL3799212)
Affinity DataIC50: 2.30nMAssay Description:Binding affinity to His-tagged CDK8 (unknown origin) after 60 mins by FRET based lanthascreen binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/10/2017
Entry Details Article
PubMed
TargetCyclin-C(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50189427(CHEMBL3827470)
Affinity DataIC50: 2.40nMAssay Description:Competitive binding affinity to full length His-tagged human recombinant CDK8/cyclin C expressed in baculovirus after 20 mins in presence of Alexa647...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2017
Entry Details Article
PubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50401441(CHEMBL2207518)
Affinity DataKd:  2.40nMAssay Description:Binding affinity to FLT3More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetCyclin-dependent kinase 8(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50163781(CHEMBL3798987)
Affinity DataIC50: 2.40nMAssay Description:Binding affinity to His-tagged CDK8 (unknown origin) after 60 mins by FRET based lanthascreen binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/10/2017
Entry Details Article
PubMed
TargetCyclin-dependent kinase 8(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50163771(CHEMBL3800311)
Affinity DataIC50: 2.40nMAssay Description:Binding affinity to His-tagged CDK8 (unknown origin) after 60 mins by FRET based lanthascreen binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/10/2017
Entry Details Article
PubMed
TargetCyclin-dependent kinase 8(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50163772(CHEMBL3797571)
Affinity DataIC50: 2.40nMAssay Description:Binding affinity to His-tagged CDK8 (unknown origin) after 60 mins by FRET based lanthascreen binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/10/2017
Entry Details Article
PubMed
LigandPNGBDBM25018(thienopyrimidine derivative, 1 | CHEMBL541643 | 3-...)
Affinity DataIC50: 2.5nMAssay Description:Inhibition of p110alpha by SPA assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/10/2012
Entry Details Article
PubMed
TargetCyclin-dependent kinase 8(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50189421(CHEMBL3827118)
Affinity DataIC50: 2.5nMAssay Description:Binding affinity to CDK8 (unknown origin) expressed in human 7dF3 cells preincubated for 2 hrs followed by beta-oestradiol addition measured after 24...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2017
Entry Details Article
PubMed
LigandPNGBDBM25018(thienopyrimidine derivative, 1 | CHEMBL541643 | 3-...)
Affinity DataIC50: 2.5nMpH: 7.4 T: 2°CAssay Description:The test compounds and enzyme were mixed in buffer, and the substrate and [gamma-33P] ATP/ATP were added to the mixture to initiate the reaction. Aft...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/26/2008
Entry Details Article
PubMed
TargetCyclin-dependent kinase 8(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50163755(CHEMBL3799396)
Affinity DataIC50: 2.70nMAssay Description:Binding affinity to His-tagged CDK8 (unknown origin) after 60 mins by FRET based lanthascreen binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/10/2017
Entry Details Article
PubMed
LigandPNGBDBM25050(3-{6-chloro-2-methylimidazo[1,2-a]pyridin-3-yl}-1-...)
Affinity DataIC50: 2.80nMpH: 7.4 T: 2°CAssay Description:The test compounds and enzyme were mixed in buffer, and the substrate and [gamma-33P] ATP/ATP were added to the mixture to initiate the reaction. Aft...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/27/2008
Entry Details Article
PubMed
TargetHeat shock factor protein 1(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50234074(CHEMBL4070633 | US9701664, Example 39)
Affinity DataIC50: 2.80nMAssay Description:Inhibition of 17-AAG-induced HSF1 pathway in human U20S cells assessed as reduction in HSP72 induction preincubated for 1 hr followed by 17-AAG addit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/9/2019
Entry Details Article
PubMed
TargetCyclin-dependent kinase 8(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50163784(CHEMBL3798804)
Affinity DataIC50: 2.80nMAssay Description:Binding affinity to His-tagged CDK8 (unknown origin) after 60 mins by FRET based lanthascreen binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/10/2017
Entry Details Article
PubMed
LigandPNGBDBM25056(4-{6-chloroimidazo[1,2-a]pyridin-3-yl}-2-[(2-methy...)
Affinity DataIC50: 2.80nMpH: 7.4 T: 2°CAssay Description:The test compounds and enzyme were mixed in buffer, and the substrate and [gamma-33P] ATP/ATP were added to the mixture to initiate the reaction. Aft...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/27/2008
Entry Details Article
PubMed
TargetHeat shock factor protein 1(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50234074(CHEMBL4070633 | US9701664, Example 39)
Affinity DataIC50: 2.80nMAssay Description:Inhibition of 17-AAG-induced HSF1 pathway in human U20S cells assessed as reduction in HSP72 induction preincubated for 1 hr followed by 17-AAG addit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/9/2019
Entry Details Article
PubMed
TargetCyclin-dependent kinase 8(Human)
The Institute of Cancer Research

Curated by ChEMBL
LigandPNGBDBM50163789(CHEMBL3799824)
Affinity DataIC50: 2.80nMAssay Description:Binding affinity to His-tagged CDK8 (unknown origin) after 60 mins by FRET based lanthascreen binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/10/2017
Entry Details Article
PubMed
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