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Assay Detail

CHEMBL5653733

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

Functional
Antiinflammatory activity against LPS-induced human THP-1 cells assessed as reduction in IL-8 cytokine level preincubated for 1 hr followed by LPS-stimulation and measured after 6 hrs by enzyme immunoassay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

THP-1 (CHEMBL614245)
Type CELL-LINE
Organism Homo sapiens

Publication

BMS-345541 is a highly selective inhibitor of I kappa B kinase that binds at an allosteric site of the enzyme and blocks NF-kappa B-dependent transcription in mice.
Burke JR, Pattoli MA, Gregor KR, Brassil PJ, MacMaster JF, McIntyre KW, Yang X, Iotzova VS, Clarke W, Strnad J, Qiu Y, Zusi FC.
J Biol Chem (2003) 278 : 1450 -1456
PubMed 12403772 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.00 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL249697 BMS-345541 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL249697 BMS-345541 IC50 = 1000.0 nM 6.00