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Assay Detail

CHEMBL1959065

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

Binding
Binding affinity to BRD4-BD1 by isothermal titration calorimetry
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
Filippakopoulos P, Picaud S, Fedorov O, Keller M, Wrobel M, Morgenstern O, Bracher F, Knapp S.
Bioorg Med Chem (2012) 20 : 1878 -1886
PubMed 22137933 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 6.37 7.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1957266 1 7.31
CHEMBL1958337 1 6.19
CHEMBL661 ALPRAZOLAM 4.0 1 5.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1957266 Kd = 49.0 nM 7.31
CHEMBL1958337 Kd = 640.0 nM 6.19
CHEMBL661 ALPRAZOLAM Kd = 2460.0 nM 5.61