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Assay Detail

CHEMBL4182592

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

Binding
Inactivation of Bacillus anthracis edema factor in mouse RAW264.7 cells assessed as reduction in cAMP production using cells exposed to edema factor for 30 mins before compound addition for 45 mins by immunoassay
10
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bacillus anthracis
Cell Type RAW264.7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Lethal factor (CHEMBL4372)
Type SINGLE PROTEIN
Organism Bacillus anthracis

Publication

Small molecule inhibitors of anthrax edema factor.
Jiao GS, Kim S, Moayeri M, Thai A, Cregar-Hernandez L, McKasson L, O'Malley S, Leppla SH, Johnson AT.
Bioorg Med Chem Lett (2018) 28 : 134 -139
PubMed 29198864 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 7.45 7.92
Inhibition 5 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4218073 2 7.92
CHEMBL4217380 2 7.62
CHEMBL4204554 2 7.50
CHEMBL4211713 2 7.22
CHEMBL4218072 2 6.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4218073 EC50 = 12.0 nM 7.92
CHEMBL4217380 EC50 = 23.7 nM 7.62
CHEMBL4204554 EC50 = 31.7 nM 7.50
CHEMBL4211713 EC50 = 60.0 nM 7.22
CHEMBL4218072 EC50 = 104.6 nM 6.98
CHEMBL4211713 Inhibition - % -
CHEMBL4218072 Inhibition - % -
CHEMBL4217380 Inhibition - % -
CHEMBL4218073 Inhibition - % -
CHEMBL4204554 Inhibition - % -