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Assay Detail

CHEMBL5166123

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

Binding
Binding affinity to human BRD4 BD1 (44 to 168 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 4 (CHEMBL1163125)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor.
Miller DC, Reuillon T, Molyneux L, Blackburn T, Cook SJ, Edwards N, Endicott JA, Golding BT, Griffin RJ, Hardcastle I, Harnor SJ, Heptinstall A, Lochhead P, Martin MP, Martin NC, Myers S, Newell DR, Noble RA, Phillips N, Rigoreau L, Thomas H, Tucker JA, Wang LZ, Waring MJ, Wong AC, Wedge SR, Noble MEM, Cano C.
J Med Chem (2022) 65 : 6513 -6540
PubMed 35468293 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 5.44 5.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4541479 1 5.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4541479 Kd = 3600.0 nM 5.44