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Assay Detail

CHEMBL5162565

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

Binding
Binding affinity to His6-fused BRD2 BD1 (unknown origin) assessed as dissociation constant in PBS incubated for 1 hrs by biolayer interferometry analysis
2
Total Activities
2
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

Structure-Based Discovery and Optimization of Furo[3,2-<i>c</i>]pyridin-4(5<i>H</i>)-one Derivatives as Potent and Second Bromodomain (BD2)-Selective Bromo and Extra Terminal Domain (BET) Inhibitors.
Li J, Zhang C, Xu H, Wang C, Dong R, Shen H, Zhuang X, Chen X, Li Q, Lu J, Zhang M, Wu X, Loomes KM, Zhou Y, Zhang Y, Liu J, Xu Y.
J Med Chem (2022) 65 : 5760 -5799
PubMed 35333526 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 5.95 5.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5204783 1 5.97
CHEMBL5206088 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5204783 Kd = 1069.0 nM 5.97
CHEMBL5206088 Kd = 1201.0 nM 5.92