BindingDB PrimarySearch

Found 29 Enz. Inhib. hit(s) with Target = 'Bromodomain-containing protein 4' and Ligand = 'BDBM50380682'

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

Ki: 9nMAssay Description:Displacement of FAM-labeled ZBA248 from BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fl...More data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

Ki: 9nMAssay Description:Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 1 (44 to 168 residues) expressed in Rosetta2 DE...More data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

Ki: 61nMAssay Description:Inhibition of tetra-acetylated Histone H4 peptide binding to recombinant human N-terminal TEV-cleavable hexa-histidine tagged BRD4 bromodomain1 after...More data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

Ki: 75nMAssay Description:Displacement of FAM-labeled ZBA248 from BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by f...More data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

Ki: 75nMAssay Description:Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 2 (333 to 460 residues) expressed in Rosetta2 D...More data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

Ki: 385nMAssay Description:Inhibition of Cy5-linked JQ1 probe binding to recombinant human N-terminal TEV-cleavable hexa-histidine tagged BRD4 bromodomain2 after 60 mins by HTR...More data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

IC50: 18nMAssay 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

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

IC50: 18nMAssay 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

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

IC50: 18nMAssay Description:Inhibition of BRD4 bromodomain 1 (unknown origin)More data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

IC50: 25nMAssay Description:Displacement of Alexa Fluor 647 labelled ligand from recombinant human N-terminal 6His-tagged BRD4-BD1 Y390A mutant (1 to 477 residue) expressed in E...More data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

IC50: 25nMAssay Description:Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRD4 BD1 (1 to 477 residues)/BD2 Y390A mutant expressed in Escher...More data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

IC50: 32nMAssay Description:Displacement of FAM-labeled ZBA248 from BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fl...More data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

IC50: 32nMAssay Description:Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 1 (44 to 168 residues) expressed in Rosetta2 DE...More data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

IC50: 36nMAssay Description:Displacement of Alexa Fluor 647 labelled ligand from His6-thr-tagged BRD4 BD1 (1 to 477 residues)/BD2 Y390A mutant (unknown origin) after 30 mins by ...More data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

IC50: 100nMAssay Description:Inhibition of BRD4(1) (unknown origin) incubated for 4 hrs by (+)-JQ1 fluorescent ligand based fluorescence anisotrophyMore data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

IC50: 107nMAssay Description:Inhibition of BRD4 bromodomain-1 (unknown origin) by europium based LANCE TR-FRET assayMore data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

IC50: 130nMAssay Description:Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrsMore data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

IC50: 200nMAssay Description:Inhibition of BRD4 in human PBMC assessed as reduction in LPS-induced IL-6 secretion incubated for 18 to 24 hrs by MSD assayMore data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

IC50: 226nMAssay Description:Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 2 (333 to 460 residues) expressed in Rosetta2 D...More data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

IC50: 226nMAssay Description:Displacement of FAM-labeled ZBA248 from BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by f...More data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

IC50: 274nMAssay Description:Displacement of Alexa Fluor 647 labelled ligand from His6-tagged BRD4 BD2 (1 to 477 residues)/BD1 Y97A mutant (unknown origin) after 30 mins by TR-FR...More data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

IC50: 316nMAssay Description:Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRD4 BD2 (1 to 477 residues)/BD1 Y97A mutant expressed in Escheri...More data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

IC50: 790nMAssay Description:Inhibition of BRD4 (unknown origin) by fluorescence polarization assayMore data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

IC50: 790nMAssay Description:Inhibition of BRD4 (unknown origin) by fluorescence anisotrophyMore data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

IC50: 790nMAssay Description:Inhibition of BRD4 (unknown origin) by fluorescence anisotropy ligand displacement assayMore data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

IC50: 794nMAssay Description:Binding affinity to BRD4 assessed as inhibition of Alexa Fluor 488 binding after 60 mins by fluorescence anisotropic analysisMore data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

IC50: 1.26E+3nMAssay Description:Inhibition of BRD4 in human whole blood assessed as reduction in LPS-induced IL-6 secretion preincubated for 30 mins followed by LPS stimulation and ...More data for this Ligand-Target Pair

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

Kd: 215nMAssay 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

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

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

Curated by ChEMBL

BDBM50380682(CHEMBL2017291 | I-BET151 (16))

Kd: 53nMAssay 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

PDB Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar

Purchase CHEMBL MCE
MMDB PC cid PC sid PDB Similars

Details Article PubMed PDB

3D Structure (crystal)

Filter my 29 hits

Targets 1▿
- Bromodomain-containing protein 4 29
Publications 14▿
- J Med Chem 58: 4927-39 (2015) 6
- J Med Chem 60: 3887-3901 (2017) 4
- J Med Chem 64: 12200-12227 (2021) 3
- J Med Chem 63: 9045-9069 (2020) 2
- Bioorg Med Chem 27: 457-469 (2019) 2
- ACS Med Chem Lett 4: 835-40 (2013) 2
- J Med Chem 58: 1281-97 (2015) 2
- J Med Chem 63: 9020-9044 (2020) 2
- Bioorg Med Chem Lett 22: 2968-72 (2012) 1
- Bioorg Med Chem 23: 953-9 (2015) 1
- J Med Chem 59: 1271-98 (2016) 1
- Bioorg Med Chem Lett 27: 4051-4055 (2017) 1
- ACS Med Chem Lett 7: 145-50 (2016) 1
- Bioorg Med Chem 26: 2937-2957 (2018) 1
Institutions 10▿
- University Of Michigan 10
- Glaxosmithkline 6
- Constellation Pharmaceuticals 3
- Shanghai Institute Of Materia Medica 2
- Gilead Sciences 2
- Gsk 2
- The University Of Tokyo 1
- Genentech 1
- University Of Oxford 1
- Sichuan University and Collaborative Innovation Center 1
Affinity: 9 to 1.3E+3 nM▿
- Ki 6
- IC50 21
- Kd 2
- Affinity ≤ nM
Xtal structures: 1
Docked structures: 0
Catalog Cmpds: 1