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Assay Detail

CHEMBL4709775

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

Binding
Inhibition of human His-tagged BRD4 bromodomain1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells using H4K5acK8acK12acK16ac as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by AlphaScreen 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

Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry.
Mäder P,Kattner L
J Med Chem (2020) 63 : 14243 -14275
PubMed 32870008 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.11 7.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3220211 1 7.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3220211 IC50 = 77.0 nM 7.11