Assay Detail

CHEMBL3383416

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Binding

Inhibition of human BRD4 bromodomain 1/2 by BROMOscan assay

ChEMBL ↗

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Target

Bromodomain-containing protein 4 (CHEMBL1163125) ↗

Open DB target context

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Bromodomain-containing protein 4 (CHEMBL1163125) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Bromodomain-containing protein 4

CHEMBL1163125

Anchored from Assay target.

Protein identity Bromodomain-containing protein 4

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Bromodomain-containing protein 4 (CHEMBL1163125) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.

Gosmini R, Nguyen VL, Toum J, Simon C, Brusq JM, Krysa G, Mirguet O, Riou-Eymard AM, Boursier EV, Trottet L, Bamborough P, Clark H, Chung CW, Cutler L, Demont EH, Kaur R, Lewis AJ, Schilling MB, Soden PE, Taylor S, Walker AL, Walker MD, Prinjha RK, Nicodème E.
J Med Chem (2014) 57 : 8111 -8131
PubMed 25249180 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	9.40	9.40

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2177300	—	—	1	9.40

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2177300	—	IC50	=	0.3981	nM	9.40