Compile Data Set for Download or QSAR
Report error Found 176 Enz. Inhib. hit(s) with Target = 'Bromodomain-containing protein 4' and Ligand = 'BDBM50365262'
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  13nMAssay Description:Binding affinity to biotinylated BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometr...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  6.70nMAssay Description:Binding affinity to biotinylated BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferomet...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  34nMAssay Description:Binding affinity to human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells by isothermal titration...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  49nMAssay Description:Binding affinity to BRD4-BD1 by isothermal titration calorimetryMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  60nMAssay Description:Binding affinity to BRD4 by isothermal titration calorimetryMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  49nMAssay Description:Binding affinity to BRD4-BD1 by isothermal titration calorimetryMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  90.1nMAssay Description:Binding affinity to BRD4-BD2 by isothermal titration calorimetryMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  49nMAssay Description:Binding affinity to BRD4 isoform 1More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  3.60E+3nMAssay Description:A BROMOscan binding assay was utilized to test the in vitro binding activity of (S)-Compounds 1, 2, 3, 4, 5 and 7 to the first and second bromodomain...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataEC50:  153nMAssay Description:Inhibition of BRD4 in human H1299 cells assessed as decrease in HPV LCR-E2-EP400-mediated transcriptional repression after 24 hrs by Bright-Glo lucif...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  100nMAssay Description:Binding affinity to human BRD4 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by isothermal titration calorimetry-based assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  92nMAssay Description:Binding affinity to human His6-tagged BRD4 BD1 (N44 to E168 residues) expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorime...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  90nMAssay Description:Inhibition of human 6x-His-tagged BRD4 bromodomain 2 expressed in Escherichia coliMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  49nMAssay Description:Inhibition of human 6x-His-tagged BRD4 bromodomain 1 expressed in Escherichia coliMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  200nMAssay Description:Binding affinity to BRD4 C-terminal bromodomain 2 H437D mutant (unknown origin) expressed in Escherichia coli Bl21(DE3) by fluorescence polarization ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  120nMAssay Description:Binding affinity to BRD4 C-terminal bromodomain 2 (unknown origin) expressed in Escherichia coli Bl21(DE3)More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  62nMAssay Description:Binding affinity to recombinant BRD4 BD2 (unknown origin) incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  92nMAssay Description:Binding affinity to recombinant BRD4 BD1 (unknown origin) incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  49nMAssay Description:Binding affinity to BRD4 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  13nMAssay Description:Binding affinity to human BRD4 BD1 (N44 to E168 aa residues) by bromoKdELECT Discover assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  35nMAssay Description:Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by MST assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  8.20nMAssay Description:Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by qPCR assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  71nMAssay Description:Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by ITC analysisMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  19nMAssay Description:Binding affinity to BRD4 D1 (unknown origin) assessed as dissociation constant by isothermal titration calorimetryMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  130nMAssay Description:Binding affinity to BRD4 D2 (unknown origin) assessed as dissociation constant by isothermal titration calorimetryMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  27nMAssay Description:Binding affinity towards BRD4-BD1 (unknown origin) measured by isothermal titration calorimetry (ITC) methodMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  9nMAssay Description:Binding affinity to BRD4 BD1 (unknown origin) by thermal denaturation assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  14nMAssay Description:Binding affinity to BRD4 BD2 (unknown origin) by thermal denaturation assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  49nMAssay Description:Binding affinity to BRD4 BD1 domain (unknown origin) by isothermal titration calorimetry assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  90nMAssay Description:Binding affinity to BRD4 BD2 domain (unknown origin) by isothermal titration calorimetry assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  51nMAssay Description:Binding affinity to BRD4 BD1 (unknown origin) assessed as dissociation constant by ITC analysisMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataKd:  230nMAssay Description:Binding affinity to BRD4 BD2 (unknown origin) assessed as dissociation constant by ITC analysisMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataIC50: 3.90nMAssay Description:Inhibition of BRD4 BD2 (unknown origin) preincubated for 15 mins followed by peptide addition and measured after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataIC50: 5.20nMAssay Description:Binding affinity to human partial length BRD4 BD2 (K333 to E460 residues) expressed in bacterial expression system using H4K5acIC8acK12acK16ac-biotin...More data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataIC50: 5.30nMAssay Description:Inhibition of C-terminal His6-tagged BRD4 BD2 (unknown origin) using H-YSGRGK(Ac)GGK(Ac)GLGK(Ac)-GGAK(Ac)RHRK-Biotin-OH as substrate incubated for 1 ...More data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataIC50: 8nMAssay Description:Inhibition of BRD4 bromodomain-1 (unknown origin) by europium based LANCE TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataIC50: 9nMAssay Description:Displacement of biotinylated acetylated histone H4 peptide from human recombinant N-terminal GST-tagged BRD4 BD1 (49 to 170 residues) expressed in Es...More data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataIC50: 12nMAssay Description:Inhibition of BRD4 BD1 (unknown origin) preincubated for 15 mins followed by peptide addition and measured after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataIC50: 13nMAssay Description:Inhibition of BRD4 BD2 (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataIC50: 14nMpH: 7.4 T: 2°CAssay Description:BRD4(2): Assays were performed as described previously with minor modifications from the manufacturer's protocol (PerkinElmer, USA). All reagents wer...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataIC50: 14nMAssay Description:Inhibition of C-terminal His6-tagged BRD4 BD1 (unknown origin) using H-YSGRGK(Ac)GGK(Ac)GLGK(Ac)-GGAK(Ac)RHRK-Biotin-OH as substrate incubated for 1 ...More data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataIC50: 18nMpH: 7.4 T: 2°CAssay Description:BRD4(1): Assays were performed as described previously with minor modifications from the manufacturer's protocol (PerkinElmer, USA). All reagents wer...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataIC50: 21nMAssay Description:Inhibition of human BRD4 BD2 (342 to 460 residues) at 30 uM preincubated for 30 mins followed by substrate addition measured after 30 mins by TR-FRET...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataIC50: 22nMAssay Description:Binding affinity to human BRD4 BD1 (44 to 168 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataIC50: 22nMAssay Description:Inhibition of human recombinant His-tagged BRD4 BD1 domain using H-SGRGK(Ac)GGK(Ac)GLGK-(Ac)GGAK(Ac)RHRK(Biotin)-OH as substrate preincubated with en...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataIC50: 22nMAssay Description:Inhibition of BRD4 bromodomain 1 (unknown origin) by Alphascreen based methodMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataIC50: 23nMAssay Description:Inhibition of BRD4 BD1 (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataIC50: 24nMAssay Description:Displacement of biotinylated tetra-acetylated histone H4 from human his-tagged BRD4 bromodomain1 by alphascreen assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataIC50: 24nMAssay Description:Inhibition of His-FLAG-tagged BRD4 binding domain1 (unknown origin) binding to H4-TetraAc-biotin peptide after 20 mins by AlphaLISAMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365262(CHEMBL1957266 | (S)-JQ1 (1) | US9320741, (S)-JQ1 |...)
Affinity DataIC50: 24nMAssay Description:Inhibition of His/FLAG-tagged BRD4 BD1 (unknown origin) using histone H4-TetraAcetylated-biotin peptide as substrate incubated for 20 mins by AlphaLI...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
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