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Assay Detail

CHEMBL1001307

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

Binding
Inhibition of TNF-induced NF-kappaB-mediated IL6 promoter expression in mouse L929sA cells by luciferase reporter gene assay
5
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type L929sA
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Withaferin a strongly elicits IkappaB kinase beta hyperphosphorylation concomitant with potent inhibition of its kinase activity.
Kaileh M, Vanden Berghe W, Heyerick A, Horion J, Piette J, Libert C, De Keukeleire D, Essawi T, Haegeman G.
J Biol Chem (2007) 282 : 4253 -4264
PubMed 17150968 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.14 6.60
Efficacy 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL517080 WITHAFERIN A 1.0 2 6.60
CHEMBL338474 HELENALIN 1 5.60
CHEMBL445041 WITHANOLIDE A 1 4.30
CHEMBL382378 1 4.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL517080 WITHAFERIN A IC50 = 250.0 nM 6.60
CHEMBL338474 HELENALIN IC50 = 2500.0 nM 5.60
CHEMBL445041 WITHANOLIDE A IC50 = 50000.0 nM 4.30
CHEMBL382378 IC50 = 90000.0 nM 4.05
CHEMBL517080 WITHAFERIN A Efficacy = 95.0 % -