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Assay Detail

CHEMBL3879155

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Binding
Inhibition of Staphylococcus aureus 1199B NorA assessed as inhibition of ethidium bromide efflux measured after 5 mins by fluorometric 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

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

Publication

Improved Potency of Indole-Based NorA Efflux Pump Inhibitors: From Serendipity toward Rational Design and Development.
Buonerba F, Lepri S, Goracci L, Schindler BD, Seo SM, Kaatz GW, Cruciani G.
J Med Chem (2017) 60 : 517 -523
PubMed 27977195 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.22 5.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3929187 1 5.75
CHEMBL3956740 1 5.70
CHEMBL3948087 1 5.42
CHEMBL3955315 1 5.31
CHEMBL3775105 1 5.22
CHEMBL3775841 1 4.90
CHEMBL3775507 1 4.77
CHEMBL3945575 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3929187 IC50 = 1800.0 nM 5.75
CHEMBL3956740 IC50 = 2020.0 nM 5.70
CHEMBL3948087 IC50 = 3830.0 nM 5.42
CHEMBL3955315 IC50 = 4930.0 nM 5.31
CHEMBL3775105 IC50 = 6000.0 nM 5.22
CHEMBL3775841 IC50 = 12500.0 nM 4.90
CHEMBL3775507 IC50 = 17100.0 nM 4.77
CHEMBL3945575 IC50 = 19900.0 nM 4.70