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Assay Detail

CHEMBL4626971

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

Functional
Antiinflammatory activity in human PBMC assessed as reduction in LPS-induced IL-6 production incubated for 18 to 24 hrs by mesoscale assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PBMC
Confidence 1 — Organism
Curated By Autocuration

Target

PBMC (CHEMBL613107)
Type CELL-LINE
Organism Homo sapiens

Publication

Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype.
Wellaway CR, Bamborough P, Bernard SG, Chung CW, Craggs PD, Cutler L, Demont EH, Evans JP, Gordon L, Karamshi B, Lewis AJ, Lindon MJ, Mitchell DJ, Rioja I, Soden PE, Taylor S, Watson RJ, Willis R, Woolven JM, Wyspiańska BS, Kerr WJ, Prinjha RK.
J Med Chem (2020) 63 : 9020 -9044
PubMed 32787145 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.87 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4639128 GSK778 1 7.20
CHEMBL2017291 1 6.90
CHEMBL4638144 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4639128 GSK778 IC50 = 63.1 nM 7.20
CHEMBL2017291 IC50 = 125.89 nM 6.90
CHEMBL4638144 IC50 = 316.23 nM 6.50