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Assay Detail

CHEMBL4425547

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

Binding
Binding affinity to Staphylococcus aureus FabF C165Q mutant expressed in Escherichia coli BL21 (DE3) PlysS cells by intrinsic tryptophan fluorescence quenching-based fluorimetric method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Staphylococcus aureus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

3-oxoacyl-[acyl-carrier-protein] synthase 2 (CHEMBL5341)
Type SINGLE PROTEIN
Organism Staphylococcus aureus

Publication

Thiolactomycin-Based Inhibitors of Bacterial β-Ketoacyl-ACP Synthases with in Vivo Activity.
Bommineni GR, Kapilashrami K, Cummings JE, Lu Y, Knudson SE, Gu C, Walker SG, Slayden RA, Tonge PJ.
J Med Chem (2016) 59 : 5377 -5390
PubMed 27187871 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 8 4.43 4.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4578072 1 4.92
CHEMBL4459185 1 4.48
CHEMBL4454335 1 4.25
CHEMBL399043 THIOLACTOMYCIN 1 4.06
CHEMBL4458874 1 -
CHEMBL4556828 1 -
CHEMBL4569473 1 -
CHEMBL4532925 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4578072 Kd = 11900.0 nM 4.92
CHEMBL4459185 Kd = 33000.0 nM 4.48
CHEMBL4454335 Kd = 56200.0 nM 4.25
CHEMBL399043 THIOLACTOMYCIN Kd = 88000.0 nM 4.06
CHEMBL4458874 Kd - -
CHEMBL4556828 Kd - -
CHEMBL4569473 Kd - -
CHEMBL4532925 Kd - -