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Assay Detail

CHEMBL5317641

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

Binding
Binding affinity to human partial length BRD3 BD2 (G306 to P416 residues) expressed in bacterial expression system using H4K5acIC8acK12acK16ac-biotinylated peptide as substrate preincubated for 30 mins followed by substrate addition by AlphaScreen assay
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 3 (CHEMBL1795186)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Physachenolide C is a Potent, Selective BET Inhibitor.
Zerio CJ, Sivinski J, Wijeratne EMK, Xu YM, Ngo DT, Ambrose AJ, Villa-Celis L, Ghadirian N, Clarkson MW, Zhang DD, Horton NC, Gunatilaka AAL, Fromme R, Chapman E.
J Med Chem (2023) 66 : 913 -933
PubMed 36577036 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.55 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1957266 1 8.12
CHEMBL3605565 1 6.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1957266 IC50 = 7.57 nM 8.12
CHEMBL3605565 IC50 = 108.0 nM 6.97