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Assay Detail

CHEMBL4121615

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

Binding
Inhibition of Staphylococcus aureus SrtA deltaN24 mutant transpeptidation activity using abz-LPATG-dnp as substrate preincubated for 10 mins followed by substrate addition measured every 2 mins for 20 mins by FRET assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sortase A (CHEMBL5362)
Type SINGLE PROTEIN
Organism Staphylococcus aureus

Publication

Quinone skeleton as a new class of irreversible inhibitors against Staphylococcus aureus sortase A.
Hou X, Wang M, Wen Y, Ni T, Guan X, Lan L, Zhang N, Zhang A, Yang CG.
Bioorg Med Chem Lett (2018) 28 : 1864 -1869
PubMed 29650293 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.72 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9470 SHIKONIN 1 6.52
CHEMBL4127840 1 6.44
CHEMBL4125701 1 5.21
CHEMBL4129079 1 4.71
CHEMBL4127684 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9470 SHIKONIN IC50 = 300.0 nM 6.52
CHEMBL4127840 IC50 = 360.0 nM 6.44
CHEMBL4125701 IC50 = 6200.0 nM 5.21
CHEMBL4129079 IC50 = 19400.0 nM 4.71
CHEMBL4127684 IC50 > 50000.0 nM -