BindingDB PrimarySearch

Found 56 Enz. Inhib. hit(s) with Target = 'Bromodomain-containing protein 4' and Ligand = 'BDBM50365463'

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

Curated by ChEMBL

Ki: 23nMAssay 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

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

Ki: 32nMAssay 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

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

Ki: 39nMAssay 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

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

Ki: 40nMAssay Description:Displacement of Alexa647-labeled JQ1 derivative from wild type BRD4 bromodomain 2 (44 to 460 residues) N433A mutant (unknown origin) incubated for 1 ...More data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

Ki: 46nMAssay 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

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

Ki: 50nMAssay Description:Displacement of Alexa647-labeled JQ1 derivative from wild type BRD4 bromodomain 1 (44 to 460 residues) N140A mutant (unknown origin) incubated for 1 ...More data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

Ki: 50nMAssay Description:Displacement of Alexa647-labeled JQ1 derivative from wild type BRD4 tandem domain (44 to 460 residues) (unknown origin) incubated for 1 hr by fluores...More data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

Ki: 66nMAssay Description:Binding affinity to human recombinant BRD4 BD2 (333 to 460 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

Ki: 74nMAssay Description:Binding affinity to human recombinant BRD4 BD1 (44 to 168 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

Ki: 94nMAssay 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

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

Ki: 163nMAssay 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

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

Ki: 200nMAssay Description:Inhibition of Cy5-linked JQ1 probe binding to recombinant human N-terminal TEV-cleavable hexa-histidine tagged BRD4 bromodomain1 after 60 mins by HTR...More data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 20nMAssay Description:Inhibition of N-terminal His-tagged BRD4 (BD2) (unknown origin) using biotinylated tetra-acetylated histone H4 peptide after 30 mins by alpha-screen ...More data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 33nMAssay Description:Displacement of tetra-acetylated Histone H4 peptide from BRD4 (unknown origin) incubated for 1 hr by FRET analysisMore data for this Ligand-Target Pair

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 33nMAssay Description:Inhibition of recombinant full length human N-terminal His6-tagged BRD4 (2 to 1362 residues) expressed in baculovirus infected insect cells using his...More data for this Ligand-Target Pair

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 36nMAssay Description:Inhibition of human His-tagged BRD4 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by FRET assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 36nMAssay Description:Inhibition of human His-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by FRET assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 36.1nMAssay Description:Displacement of tetra-acetylated H4 peptide from human Brd4 bromodomain BD12 after 1 hr by FRET analysisMore data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 36.1nMAssay Description:Displacement of acetylated histone peptide from BRD4-BD1,2 by FRET assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 40nMAssay Description:Inhibition of N-terminal His-tagged BRD4 (BD1) (unknown origin) using biotinylated tetra-acetylated histone H4 peptide after 30 mins by alpha-screen ...More data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 40nMAssay Description:Inhibition of N-terminal His-tagged BRD4 (BD1/BD2) (unknown origin) using biotinylated tetra-acetylated histone H4 peptide after 30 mins by alpha-scr...More data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 61nMAssay Description:Inhibition of BRD4 BD1-BD2 (unknown origin) using tetraacetylated histone peptide as substrate after 2 hrs by alphascreen assayMore data for this Ligand-Target Pair

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 68nMAssay Description:Inhibition of His-tagged human BRD4-BD1 using H4K5acK8acK12acK16ac as substrate preincubated for 30 mins followed by substrate addition measured afte...More data for this Ligand-Target Pair

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 78nMAssay 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

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 93nMAssay 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 Michigan

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 98nMAssay 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

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 120nMAssay Description:Displacement of biotinylated tetra-acetylated histone H4 from human his-tagged BRD4 bromodomain1 by FRET assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 120nMAssay 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

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 126nMAssay Description:Inhibition of BRD4 BD1 (unknown origin) measured by TR-FRET assayMore data for this Ligand-Target Pair

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 126nMAssay Description:Inhibition of BRD4 BD2 (unknown origin) measured by TR-FRET assayMore data for this Ligand-Target Pair

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 132nMAssay Description:Inhibition of BRD4-BD1 in human Raji cells assessed as downregulation of MYC gene expression by PCR methodMore data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 145nMAssay 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

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 156nMAssay 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

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 190nMAssay Description:Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrsMore data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 190nMAssay Description:Inhibition of His6-tagged BRD4-BD12 expressed in Escherichia coli assessed as inhibition of binding to SGRG-K(Ac)-GG-K(Ac)-GLG-K(Ac)-GGA-K(Ac)-RHGSGS...More data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 260nMAssay 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 Michigan

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 316nMAssay 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

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 320nMAssay Description:Displacement of APC-labeled biotinylated-avidin from Euphorium-chelated recombinant human N-terminal GST-tagged BRD4 bromodomain 1 expressed in Esche...More data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 590nMAssay Description:Inhibition of BRD4-BD1 (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 630nMAssay 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 Michigan

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 630nMAssay Description:Inhibition of BRD4 (unknown origin) by fluorescence anisotrophyMore data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 631nMAssay 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

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 631nMAssay Description:Inhibition of BRD4 bromodomain-1 (unknown origin) by FRET assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 631nMAssay Description:Binding affinity to His6-tagged BRD4 (unknown origin) after 60 mins by fluorescence anisotropy binding AssayMore data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

IC50: 740nMAssay Description:Inhibition of His6-tagged BRD4 expressed in Escherichia coli after 60 mins by fluorescence anisotropy assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

EC50: 440nMAssay Description:Inhibition of BRD4 in human PBMC assessed as reduction in LPS-induced TNFalpha secretion preincubated for 1 hr followed by LPS-stimulation and measur...More data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

Kd: 41nMAssay Description:Binding affinity to human partial length BRD4-BD1 (N44 to E168 residues) expressed in bacterial expression system by BROMOscan methodMore data for this Ligand-Target Pair

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

Kd: 19nMAssay Description:Binding affinity to human partial length BRD4-BD2 (K333 to E460 residues) expressed in bacterial expression system by BROMOscan methodMore data for this Ligand-Target Pair

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

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3D Structure (crystal)

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

Curated by ChEMBL

BDBM50365463(CHEMBL1232461)

Kd: 37nMAssay Description:Displacement of biotinylated acetylated peptide from recombinant human partial length BRD4 long isoform bromodomain 1/2 (N44 to E460 residues) expres...More data for this Ligand-Target Pair

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

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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

BDBM50365463(CHEMBL1232461)

Kd: 37nMAssay Description:Inhibition of human GST-tagged TAF1 BD2 (1519 to 1651 residues) expressed in Escherichia coli BL21 (DE3)-R3-pRARE2 preincubated for 15 mins followed ...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)

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Filter my 56 hits

Targets 1▿
- Bromodomain-containing protein 4 56
Publications 29▿
- J Med Chem 58: 4927-39 (2015) 6
- Bioorg Med Chem 34: (2021) 4
- J Med Chem 60: 3887-3901 (2017) 4
- J Med Chem 55: 587-96 (2012) 3
- Bioorg Med Chem 27: 457-469 (2019) 3
- J Med Chem 59: 7801-17 (2016) 3
- J Med Chem 61: 8202-8211 (2018) 3
- J Med Chem 64: 12200-12227 (2021) 2
- J Med Chem 65: 15174-15207 (2022) 2
- J Med Chem 59: 1492-500 (2016) 2
- J Med Chem 59: 1565-79 (2016) 2
- Bioorg Med Chem Lett 28: 1811-1816 (2018) 2
- Eur J Med Chem 182: (2019) 2
- ACS Med Chem Lett 4: 835-40 (2013) 2
- Bioorg Med Chem 20: 1887-92 (2012) 2
- Bioorg Med Chem Lett 29: 1220-1226 (2019) 1
- J Med Chem 56: 7501-15 (2013) 1
- Eur J Med Chem 163: 281-294 (2019) 1
- J Med Chem 54: 3827-38 (2011) 1
- J Med Chem 63: 14243-14275 (2020) 1
- Eur J Med Chem 152: 542-559 (2018) 1
- Bioorg Med Chem Lett 27: 4606-4613 (2017) 1
- Bioorg Med Chem 26: 3399-3405 (2018) 1
- Eur J Med Chem 150: 156-175 (2018) 1
- Eur J Med Chem 137: 176-195 (2017) 1
- J Med Chem 59: 1271-98 (2016) 1
- J Med Chem 58: 1281-97 (2015) 1
- Bioorg Med Chem 28: (2020) 1
- Bioorg Med Chem Lett 28: 3483-3488 (2018) 1
Institutions 21▿
- University Of Michigan 10
- Glaxosmithkline 7
- Chinese Academy Of Sciences 4
- Kyorin Pharmaceutical 4
- Astrazeneca 3
- Zenith Epigenetics 3
- Gilead Sciences 3
- Celgene Quanticel Research 2
- Japan Science And Technology Agency 2
- University Of Chinese Academy Of Sciences 2
- University Of Dundee 2
- National Institutes Of Health 2
- Guangzhou Institutes Of Biomedicine And Health 2
- Constellation Pharmaceuticals 2
- Gsk 2
- Shanghai Institute Of Materia Medica 1
- Genentech 1
- China Pharmaceutical University 1
- Endotherm 1
- Korea Research Institute Of Chemical Technology 1
- Bienta/Enamine 1
Affinity: 19 to 7.4E+2 nM▿
- Ki 12
- IC50 33
- Kd 10
- EC50 1
- Affinity ≤ nM
Xtal structures: 1
Docked structures: 0
Catalog Cmpds: 1