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Assay Detail

CHEMBL4615387

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

Binding
Binding affinity to BRD4 (1) (unknown origin) N-terminal bromodomain by TR-FRET assay
14
Total Activities
14
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 4 (CHEMBL1163125)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Application of Atypical Acetyl-lysine Methyl Mimetics in the Development of Selective Inhibitors of the Bromodomain-Containing Protein 7 (BRD7)/Bromodomain-Containing Protein 9 (BRD9) Bromodomains.
Clegg MA, Bamborough P, Chung CW, Craggs PD, Gordon L, Grandi P, Leveridge M, Lindon M, Liwicki GM, Michon AM, Molnar J, Rioja I, Soden PE, Theodoulou NH, Werner T, Tomkinson NCO, Prinjha RK, Humphreys PG.
J Med Chem (2020) 63 : 5816 -5840
PubMed 32410449 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 4.72 4.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4639281 1 4.90
CHEMBL4633192 1 4.90
CHEMBL4643455 1 4.90
CHEMBL4644816 1 4.80
CHEMBL4095646 1 4.70
CHEMBL4642945 1 4.70
CHEMBL4645392 1 4.70
CHEMBL4647246 1 4.60
CHEMBL4645268 1 4.60
CHEMBL4645137 1 4.40
CHEMBL4093233 1 -
CHEMBL4646728 1 -
CHEMBL4648548 1 -
CHEMBL4643740 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4639281 IC50 = 12589.25 nM 4.90
CHEMBL4633192 IC50 = 12589.25 nM 4.90
CHEMBL4643455 IC50 = 12589.25 nM 4.90
CHEMBL4644816 IC50 = 15848.93 nM 4.80
CHEMBL4095646 IC50 = 19952.62 nM 4.70
CHEMBL4642945 IC50 = 19952.62 nM 4.70
CHEMBL4645392 IC50 = 19952.62 nM 4.70
CHEMBL4647246 IC50 = 25118.86 nM 4.60
CHEMBL4645268 IC50 = 25118.86 nM 4.60
CHEMBL4645137 IC50 = 39810.72 nM 4.40
CHEMBL4093233 IC50 = 125892.54 nM -
CHEMBL4646728 IC50 > 50118.72 nM -
CHEMBL4648548 IC50 > 50118.72 nM -
CHEMBL4643740 IC50 > 50118.72 nM -