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Assay Detail

CHEMBL3389868

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

Binding
Inhibition of Staphylococcus aureus sortase A using dabcyl-QALPETGEE-edans as substrate incubated for 1 hr prior to substrate addition measured at 1 min interval for 1 hr by FRET analysis
22
Total Activities
22
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

Discovery and structure-activity relationship studies of irreversible benzisothiazolinone-based inhibitors against Staphylococcus aureus sortase A transpeptidase.
Zhulenkovs D, Rudevica Z, Jaudzems K, Turks M, Leonchiks A.
Bioorg Med Chem (2014) 22 : 5988 -6003
PubMed 25282649 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 5.27 5.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3343843 1 5.47
CHEMBL3343832 1 5.42
CHEMBL3343842 1 5.42
CHEMBL3343831 1 5.41
CHEMBL3343837 1 5.40
CHEMBL3343839 1 5.40
CHEMBL3343838 1 5.39
CHEMBL3341779 1 5.38
CHEMBL3343833 1 5.33
CHEMBL3343830 1 5.30
CHEMBL3343841 1 5.30
CHEMBL3343836 1 5.29
CHEMBL1471698 1 5.21
CHEMBL3343840 1 5.20
CHEMBL3343835 1 5.19
CHEMBL3343834 1 5.15
CHEMBL3343844 1 4.89
CHEMBL264166 1 4.77
CHEMBL165058 (ETHENYLSULFONYL)BENZENE 1 -
CHEMBL1569 AMANTADINE HYDROCHLORIDE 4.0 1 -
CHEMBL3343845 1 -
CHEMBL3343846 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3343843 IC50 = 3390.0 nM 5.47
CHEMBL3343832 IC50 = 3810.0 nM 5.42
CHEMBL3343842 IC50 = 3800.0 nM 5.42
CHEMBL3343831 IC50 = 3870.0 nM 5.41
CHEMBL3343837 IC50 = 4010.0 nM 5.40
CHEMBL3343839 IC50 = 3960.0 nM 5.40
CHEMBL3343838 IC50 = 4070.0 nM 5.39
CHEMBL3341779 IC50 = 4220.0 nM 5.38
CHEMBL3343833 IC50 = 4620.0 nM 5.33
CHEMBL3343830 IC50 = 4990.0 nM 5.30
CHEMBL3343841 IC50 = 5060.0 nM 5.30
CHEMBL3343836 IC50 = 5080.0 nM 5.29
CHEMBL1471698 IC50 = 6110.0 nM 5.21
CHEMBL3343840 IC50 = 6260.0 nM 5.20
CHEMBL3343835 IC50 = 6440.0 nM 5.19
CHEMBL3343834 IC50 = 7060.0 nM 5.15
CHEMBL3343844 IC50 = 12780.0 nM 4.89
CHEMBL264166 IC50 = 16910.0 nM 4.77
CHEMBL165058 (ETHENYLSULFONYL)BENZENE IC50 = 736000.0 nM -
CHEMBL1569 AMANTADINE HYDROCHLORIDE IC50 - -
CHEMBL3343845 IC50 - -
CHEMBL3343846 IC50 - -