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Assay Detail

CHEMBL4405073

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

Binding
Binding affinity to human partial length BRD2 BD2 isoform 1 (E348 to D455 residues) expressed in bacterial expression system by bromoscan assay
1
Total Activities
1
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

Discovery of 8-Methyl-pyrrolo[1,2-a]pyrazin-1(2H)-one Derivatives as Highly Potent and Selective Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitors.
Li Z, Xiao S, Yang Y, Chen C, Lu T, Chen Z, Jiang H, Chen S, Luo C, Zhou B.
J Med Chem (2020) 63 : 3956 -3975
PubMed 32208600 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 8.89 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4440098 1 8.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4440098 Kd = 1.3 nM 8.89