Assay Detail

CHEMBL5696918

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Binding

Binding affinity to His6-tagged BRD3 (1 to 434 residues) (unknown origin) at pH 5 to 6.5 assessed as dissociation constant by surface plasmon resonance assay

ChEMBL ↗

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Target

Bromodomain-containing protein 3 (CHEMBL1795186) ↗

Open DB target context

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Bromodomain-containing protein 3 (CHEMBL1795186) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Bromodomain-containing protein 3

CHEMBL1795186

Anchored from Assay target.

Protein identity Bromodomain-containing protein 3

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 3 (CHEMBL1795186) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.

Dawson MA, Prinjha RK, Dittmann A, Giotopoulos G, Bantscheff M, Chan WI, Robson SC, Chung CW, Hopf C, Savitski MM, Huthmacher C, Gudgin E, Lugo D, Beinke S, Chapman TD, Roberts EJ, Soden PE, Auger KR, Mirguet O, Doehner K, Delwel R, Burnett AK, Jeffrey P, Drewes G, Lee K, Huntly BJ, Kouzarides T.
Nature (2011) 478 : 529 -533
PubMed 21964340 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Kd	2	7.20	7.70

Assay Parameters

Parameter	Type	Value	Units	Text
EFO_ID	EFO_ID	-	—	EFO:0000565
EFO_TERM	EFO_TERM	-	—	leukemia

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2017291	—	—	1	7.70
CHEMBL1232461	MOLIBRESIB	2.0	1	6.70

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2017291	—	Kd	=	20.0	nM	7.70
CHEMBL1232461	MOLIBRESIB	Kd	=	200.0	nM	6.70