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Assay Detail

CHEMBL4038422

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity to BRD2 BD1-BD2 (G73 to A560 residues) (unknown origin) after 1 hr by Alexa-647-conjugated probe based TR-FRET assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
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

Methylpyrrole inhibitors of BET bromodomains.
Hasvold LA, Sheppard GS, Wang L, Fidanze SD, Liu D, Pratt JK, Mantei RA, Wada CK, Hubbard R, Shen Y, Lin X, Huang X, Warder SE, Wilcox D, Li L, Buchanan FG, Smithee L, Albert DH, Magoc TJ, Park CH, Petros AM, Panchal SC, Sun C, Kovar P, Soni NB, Elmore SW, Kati WM, McDaniel KF.
Bioorg Med Chem Lett (2017) 27 : 2225 -2233
PubMed 28268136 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.41 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4063051 1 7.85
CHEMBL3786012 1 7.57
CHEMBL4088466 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4063051 Ki = 14.0 nM 7.85
CHEMBL3786012 Ki = 27.0 nM 7.57
CHEMBL4088466 Ki = 160.0 nM 6.80