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Assay Detail

CHEMBL3089615

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

Binding
Displacement of fluorescein-labeled MS239 from recombinant human SMARCA4 bromodomain after 1 hr by fluorescence anisotropy assay
4
Total Activities
4
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

Transcription activator BRG1 (CHEMBL3085620)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains.
Zhang G, Plotnikov AN, Rusinova E, Shen T, Morohashi K, Joshua J, Zeng L, Mujtaba S, Ohlmeyer M, Zhou MM.
J Med Chem (2013) 56 : 9251 -9264
PubMed 24144283 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.10 5.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3086883 1 5.10
CHEMBL3086885 1 -
CHEMBL3086884 1 -
CHEMBL3087052 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3086883 Ki = 7970.0 nM 5.10
CHEMBL3086885 Ki < 6560.0 nM -
CHEMBL3086884 Ki < 6560.0 nM -
CHEMBL3087052 Ki < 6560.0 nM -