Assay Detail

CHEMBL4020255

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Binding

Binding affinity to BRD2 BD1 to BD2 (G73 to A560 residues) (unknown origin)

ChEMBL ↗

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Target

Bromodomain-containing protein 2 (CHEMBL1293289) ↗

Open DB target context

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Bromodomain-containing protein 2 (CHEMBL1293289) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Bromodomain-containing protein 2

CHEMBL1293289

Anchored from Assay target.

Protein identity Bromodomain-containing protein 2

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 2 (CHEMBL1293289) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.

McDaniel KF, Wang L, Soltwedel T, Fidanze SD, Hasvold LA, Liu D, Mantei RA, Pratt JK, Sheppard GS, Bui MH, Faivre EJ, Huang X, Li L, Lin X, Wang R, Warder SE, Wilcox D, Albert DH, Magoc TJ, Rajaraman G, Park CH, Hutchins CW, Shen JJ, Edalji RP, Sun CC, Martin R, Gao W, Wong S, Fang G, Elmore SW, Shen Y, Kati WM.
J Med Chem (2017) 60 : 8369 -8384
PubMed 28949521 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	1	9.00	9.00

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3987016	MIVEBRESIB	2.0	1	9.00

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3987016	MIVEBRESIB	Ki	=	1.0	nM	9.00