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Assay Detail

CHEMBL5713484

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

Binding
Inhibition of BRD4 BD2 (unknown origin) using acetylated H4 K5/8/12/16 as substrate incubated for 60 mins by alpha-screen assay
3
Total Activities
3
Compounds Tested
1
Activity Types
4
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bromodomain-containing protein 4 (CHEMBL1163125)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Sensitivity and engineered resistance of myeloid leukemia cells to BRD9 inhibition.
Hohmann AF, Martin LJ, Minder JL, Roe JS, Shi J, Steurer S, Bader G, McConnell D, Pearson M, Gerstberger T, Gottschamel T, Thompson D, Suzuki Y, Koegl M, Vakoc CR.
Nat Chem Biol (2016) 12 : 672 -679
PubMed 27376689 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.56 4.56

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - EFO:0000222
EFO_ID EFO_ID - EFO:0000222
EFO_TERM EFO_TERM - acute myeloid leukemia
EFO_TERM EFO_TERM - acute myeloid leukemia

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3824146 1 4.56
CHEMBL3823478 1 -
CHEMBL3823697 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3824146 IC50 = 27330.0 nM 4.56
CHEMBL3823478 IC50 > 100000.0 nM -
CHEMBL3823697 IC50 > 100000.0 nM -