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Assay Detail

CHEMBL5539627

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

Binding
Inhibition of Staphylococcus aureus Sortase A N24 deletion mutant transpeptidation using IsdA64-323 as substrate preincubated for 20 mins followed by substrate addition and measured after 1.5 hrs by SDS-PAGE analysis
10
Total Activities
10
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

Sortase A (CHEMBL5362)
Type SINGLE PROTEIN
Organism Staphylococcus aureus

Publication

Structure-Guided Design, Synthesis, and Antivirulence Assessment of Covalent <i>Staphylococcus aureus</i> Sortase A Inhibitors.
Yue C, Yuan Z, Xu G, Guan XN, Wei B, Yao H, Yang CG, Zhang T.
J Med Chem (2024) 67 : 1127 -1146
PubMed 38170998 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.00 5.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5570289 1 5.28
CHEMBL5174805 1 5.13
CHEMBL5569180 1 5.13
CHEMBL270142 1 5.09
CHEMBL5569374 1 5.09
CHEMBL5574464 1 5.05
CHEMBL5574890 1 5.05
CHEMBL5573262 1 4.82
CHEMBL5564769 1 4.79
CHEMBL5565857 1 4.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5570289 IC50 = 5200.0 nM 5.28
CHEMBL5174805 IC50 = 7400.0 nM 5.13
CHEMBL5569180 IC50 = 7400.0 nM 5.13
CHEMBL270142 IC50 = 8200.0 nM 5.09
CHEMBL5569374 IC50 = 8100.0 nM 5.09
CHEMBL5574464 IC50 = 9000.0 nM 5.05
CHEMBL5574890 IC50 = 8900.0 nM 5.05
CHEMBL5573262 IC50 = 15300.0 nM 4.82
CHEMBL5564769 IC50 = 16100.0 nM 4.79
CHEMBL5565857 IC50 = 24600.0 nM 4.61