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Assay Detail

CHEMBL888332

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Functional
Inhibition of LPS-induced TNFalpha production in PBMC
6
Total Activities
6
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

Synthesis and structure-activity relationship of imidazo(1,2-a)thieno(3,2-e)pyrazines as IKK-beta inhibitors.
Belema M, Bunker A, Nguyen VN, Beaulieu F, Ouellet C, Qiu Y, Zhang Y, Martel A, Burke JR, McIntyre KW, Pattoli MA, Daloisio C, Gillooly KM, Clarke WJ, Brassil PJ, Zusi FC, Vyas DM.
Bioorg Med Chem Lett (2007) 17 : 4284 -4289
PubMed 17540562 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.70 7.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL399486 1 7.19
CHEMBL400078 1 7.17
CHEMBL249280 1 7.02
CHEMBL251724 1 6.85
CHEMBL249697 BMS-345541 1 6.10
CHEMBL398253 1 5.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL399486 EC50 = 65.0 nM 7.19
CHEMBL400078 EC50 = 68.0 nM 7.17
CHEMBL249280 EC50 = 95.0 nM 7.02
CHEMBL251724 EC50 = 140.0 nM 6.85
CHEMBL249697 BMS-345541 EC50 = 800.0 nM 6.10
CHEMBL398253 EC50 = 1370.0 nM 5.86