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Assay Detail

CHEMBL4612484

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

Binding
Binding affinity to human partial length BRD3 bromodomain 1 and 2 (P24 to P416 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 3 (CHEMBL1795186)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib.
Li Y, Zhao J, Gutgesell LM, Shen Z, Ratia K, Dye K, Dubrovskyi O, Zhao H, Huang F, Tonetti DA, Thatcher GRJ, Xiong R.
J Med Chem (2020) 63 : 7186 -7210
PubMed 32453591 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 9.57 9.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4648912 1 9.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4648912 Kd = 0.27 nM 9.57