BindingDB PrimarySearch

Found 24 Enz. Inhib. hit(s) with Target = 'Bromodomain-containing protein 4' and Ligand = 'BDBM25121'

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

Ki: 56nMAssay Description:Binding affinity to BRD4 (unknown origin) expressed in Escherichia coli BL21 after 1 hr by proprietary competition assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

IC50: 1.20nMAssay Description:Inhibition of BRD4 (unknown origin) by alpha-screen assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

IC50: 25nMAssay Description:Inhibition of BRD4 (unknown origin) by alpha screen assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

IC50: 25nMAssay Description:Inhibition of BRD4 (unknown origin)More data for this Ligand-Target Pair

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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

IC50: 25nMAssay Description:Inhibition of BRD4 (unknown origin)More data for this Ligand-Target Pair

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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

IC50: 25nMAssay Description:Inhibition of N-terminal 6His-tagged human BRD4 bromodomain 1 (44 to 168 residues) expressed in Escherichia coli BL21 (DE3) using biotinylated histon...More data for this Ligand-Target Pair

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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

IC50: 25nMAssay Description:Inhibition of recombinant human N-terminal His6-tagged BRD4 expressed in Escherichia coli BL21(DE3) cells using biotinylated histone H4 peptide as su...More data for this Ligand-Target Pair

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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

IC50: 25nMAssay Description:Inhibition of human N-terminal His6-tagged BRD4-BD1 (44 to 168 residues) expressed in Escherichia coli BL21 (DE3) cells using protein thermal shift d...More data for this Ligand-Target Pair

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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

IC50: 59nMAssay Description:Displacement of FITC-JQ1 from His6-tagged BRD4 bromodomain-1 (unknown origin) expressed in Escherichia coli BL21(DE3) after 4 hrs by fluorescence ani...More data for this Ligand-Target Pair

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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

IC50: 150nMAssay Description:Displacement of Bio-JQ1 from recombinant human His6 tagged BRD4 bromodomain 1 by alphascreen assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

IC50: 184nMAssay Description:Displacement of biotin-PEG2- SGRGKacGGKacGLGKacGGAKacRHPvK-COOH from BRD4 (unknown origin) after 1.5 hrs by acetyl-histone binding based Alphascreen ...More data for this Ligand-Target Pair

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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

IC50: 205nMAssay Description:Inhibition of BRD4-BD1 (unknown origin) incubated for 1 hr by AlphaScreen biotin-JQ1 competition assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

IC50: 250nMAssay Description:Inhibition of JQ1-FITC binding to His6-tagged BRD4-BD1 (unknown origin) expressed in Escherichia coli BL21 (DE3)-codon plus-RIL cells incubated in da...More data for this Ligand-Target Pair

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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

IC50: 300nMAssay Description:Inhibition of full-length C-terminal NanoLuc-tagged BRD4 BD1 (unknown origin) expressed in human HEK293 cells after 2 hrs by NanoBRET target engageme...More data for this Ligand-Target Pair

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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

Kd: 24nMAssay 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

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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

Kd: 112nMAssay 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

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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

Kd: 37nMAssay Description:Binding affinity to His6/TEV fused recombinant human BRD4 expressed in bacteria assessed as dissociation constant by isothermal titration calorimetry...More data for this Ligand-Target Pair

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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

Kd: 37nMAssay Description:Binding affinity to BRD4 (unknown origin) by isothermal titration calorimetry assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

Kd: 57nMAssay 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

PDB Reactome pathway KEGG
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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

Kd: 87nMAssay Description:Binding affinity to BRD4 (unknown origin) by isothermal titration calorimetric assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

Kd: 24nMAssay Description:Binding affinity to human partial length BRD4 bromodomain 1 long isoform (N44 to E168 residues) expressed in bacterial expression system by competiti...More data for this Ligand-Target Pair

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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

Kd: 37nMAssay Description:Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat thoracic aorta (Alpha-1D adrenoceptor)More data for this Ligand-Target Pair

PDB Reactome pathway KEGG
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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

Kd: 37nMAssay Description:Binding affinity to recombinant human His6-TEV protease-tagged BRD4 bromodomain 1 expressed in bacteria by isothermal titration calorimetric methodMore data for this Ligand-Target Pair

PDB Reactome pathway KEGG
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3D Structure (crystal)

Bromodomain-containing protein 4(Homo sapiens (Human))
University Of Maryland

Curated by ChEMBL

BDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)

Kd: 37nMAssay Description:Binding affinity to BRD4 (unknown origin) by isothermal calorimetryMore data for this Ligand-Target Pair

PDB Reactome pathway KEGG
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3D Structure (crystal)

Filter my 24 hits

Targets 1▿
- Bromodomain-containing protein 4 24
Publications 13▿
- J Med Chem 64: 15772-15786 (2021) 3
- ACS Med Chem Lett 6: 764-9 (2015) 3
- Eur J Med Chem 137: 176-195 (2017) 2
- ACS Med Chem Lett 10: 1443-1449 (2019) 2
- J Med Chem 62: 2618-2637 (2019) 2
- ACS Med Chem Lett 7: 131-131 (2016) 2
- Nat Rev Drug Discov 16: 424-440 (2017) 2
- Eur J Med Chem 191: (2020) 1
- Eur J Med Chem 150: 156-175 (2018) 1
- J Med Chem 65: 10133-10160 (2022) 1
- J Med Chem 61: 7785-7795 (2018) 1
- ACS Med Chem Lett 9: 1199-1204 (2018) 1
- J Med Chem 60: 4533-4558 (2017) 1
Institutions 11▿
- The Institute Of Cancer Research 3
- Chinese Academy Of Sciences 3
- Moffitt Cancer Center 3
- University Of Maryland 3
- Dana Farber Cancer Institute 2
- The University Of Sydney 2
- Dart Neuroscience 2
- West China Hospital 1
- University Of Massachusetts-Boston 1
- University of Texas Medical Branch 1
- Southwest Jiaotong University 1
Affinity: 1.2 to 3.0E+2 nM▿
- Ki 1
- IC50 13
- Kd 10
- Affinity ≤ nM
Xtal structures: 1
Docked structures: 0
Catalog Cmpds: 1