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Assay Detail

CHEMBL4155968

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

Binding
Inhibition of Staphylococcus aureus SA-1199B NorA assessed as reduction in EtBr efflux measured over 5 mins by fluorescence assay
13
Total Activities
13
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

Quinolone resistance protein NorA (CHEMBL5114)
Type SINGLE PROTEIN
Organism Staphylococcus aureus

Publication

Studies on 2-phenylquinoline Staphylococcus aureus NorA efflux pump inhibitors: New insights on the C-6 position.
Felicetti T, Cannalire R, Nizi MG, Tabarrini O, Massari S, Barreca ML, Manfroni G, Schindler BD, Cecchetti V, Kaatz GW, Sabatini S.
Eur J Med Chem (2018) 155 : 428 -433
PubMed 29908437 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.25 5.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4177330 1 5.66
CHEMBL4164053 1 5.48
CHEMBL4171010 1 5.48
CHEMBL4175374 1 5.36
CHEMBL4168471 1 5.30
CHEMBL4167087 1 5.28
CHEMBL4170494 1 5.24
CHEMBL1651181 1 5.14
CHEMBL4164750 1 5.14
CHEMBL4160250 1 5.06
CHEMBL1651180 1 5.05
CHEMBL772 RESERPINE 4.0 1 5.04
CHEMBL4174235 1 4.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4177330 IC50 = 2200.0 nM 5.66
CHEMBL4164053 IC50 = 3300.0 nM 5.48
CHEMBL4171010 IC50 = 3300.0 nM 5.48
CHEMBL4175374 IC50 = 4400.0 nM 5.36
CHEMBL4168471 IC50 = 5000.0 nM 5.30
CHEMBL4167087 IC50 = 5200.0 nM 5.28
CHEMBL4170494 IC50 = 5800.0 nM 5.24
CHEMBL1651181 IC50 = 7300.0 nM 5.14
CHEMBL4164750 IC50 = 7200.0 nM 5.14
CHEMBL4160250 IC50 = 8800.0 nM 5.06
CHEMBL1651180 IC50 = 8900.0 nM 5.05
CHEMBL772 RESERPINE IC50 = 9200.0 nM 5.04
CHEMBL4174235 IC50 = 10600.0 nM 4.97