Assay Detail

CHEMBL5650358

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Binding

Inhibition of N-terminal 6His-Flag tagged p300-BHC domain (1036 to 1822 residues) (unknown origin) expressed in Sf9 cells using the Bac-to-Bac baculovirus system using biotinylated synthetic Histone-H4 peptide incubated for 30 mins followed by substrate addition and measured after 1hr by TR-FRET assay

ChEMBL ↗

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Target

Histone acetyltransferase p300 (CHEMBL3784) ↗

Open DB target context

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Histone acetyltransferase p300 (CHEMBL3784) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Histone acetyltransferase p300

CHEMBL3784

Anchored from Assay target.

Protein identity Histone acetyltransferase p300

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
Cell Type	Sf9
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Histone acetyltransferase p300 (CHEMBL3784) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours.

Lasko LM, Jakob CG, Edalji RP, Qiu W, Montgomery D, Digiammarino EL, Hansen TM, Risi RM, Frey R, Manaves V, Shaw B, Algire M, Hessler P, Lam LT, Uziel T, Faivre E, Ferguson D, Buchanan FG, Martin RL, Torrent M, Chiang GG, Karukurichi K, Langston JW, Weinert BT, Choudhary C, de Vries P, Van Drie JH, McElligott D, Kesicki E, Marmorstein R, Sun C, Cole PA, Rosenberg SH, Michaelides MR, Lai A, Bromberg KD.
Nature (2017) 550 : 128 -132
PubMed 28953875 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	8.01	8.01

Assay Parameters

Parameter	Type	Value	Units	Text
EFO_ID	EFO_ID	-	—	MONDO:0004992
EFO_ID	EFO_ID	-	—	MONDO:0021259
EFO_TERM	EFO_TERM	-	—	cancer
EFO_TERM	EFO_TERM	-	—	prostate neoplasm

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4282264	A-485	—	1	8.01

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4282264	A-485	IC50	=	9.8	nM	8.01