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Assay Detail

CHEMBL4151512

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

Binding
Inhibition of NorA in Staphylococcus aureus SA-1199B expressing GrlA A116E mutant assessed as reduction in EtBr efflux incubated for 5 mins by fluorescence based assay
44
Total Activities
44
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

2-Phenylquinoline S. aureus NorA Efflux Pump Inhibitors: Evaluation of the Importance of Methoxy Group Introduction.
Felicetti T, Cannalire R, Pietrella D, Latacz G, Lubelska A, Manfroni G, Barreca ML, Massari S, Tabarrini O, Kieć-Kononowicz K, Schindler BD, Kaatz GW, Cecchetti V, Sabatini S.
J Med Chem (2018) 61 : 7827 -7848
PubMed 30067360 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 5.28 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4171147 1 5.96
CHEMBL4175014 1 5.80
CHEMBL4172225 1 5.75
CHEMBL4163342 1 5.55
CHEMBL4170066 1 5.42
CHEMBL4169284 1 5.42
CHEMBL4164426 1 5.41
CHEMBL4161736 1 5.40
CHEMBL4175717 1 5.39
CHEMBL4162146 1 5.39
CHEMBL4162139 1 5.38
CHEMBL4176162 1 5.37
CHEMBL4168943 1 5.34
CHEMBL4174957 1 5.33
CHEMBL4172372 1 5.33
CHEMBL4164737 1 5.33
CHEMBL4167074 1 5.31
CHEMBL4172781 1 5.26
CHEMBL4168315 1 5.14
CHEMBL4170063 1 5.09
CHEMBL1651180 1 5.05
CHEMBL772 RESERPINE 4.0 1 5.04
CHEMBL4169246 1 5.03
CHEMBL4171241 1 5.00
CHEMBL4169390 1 4.92
CHEMBL4164881 1 4.86
CHEMBL4176869 1 4.81
CHEMBL4161319 1 4.72
CHEMBL4173506 1 -
CHEMBL4172633 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4171147 IC50 = 1100.0 nM 5.96
CHEMBL4175014 IC50 = 1600.0 nM 5.80
CHEMBL4172225 IC50 = 1800.0 nM 5.75
CHEMBL4163342 IC50 = 2800.0 nM 5.55
CHEMBL4170066 IC50 = 3800.0 nM 5.42
CHEMBL4169284 IC50 = 3800.0 nM 5.42
CHEMBL4164426 IC50 = 3900.0 nM 5.41
CHEMBL4161736 IC50 = 4000.0 nM 5.40
CHEMBL4175717 IC50 = 4100.0 nM 5.39
CHEMBL4162146 IC50 = 4100.0 nM 5.39
CHEMBL4162139 IC50 = 4200.0 nM 5.38
CHEMBL4176162 IC50 = 4300.0 nM 5.37
CHEMBL4168943 IC50 = 4600.0 nM 5.34
CHEMBL4164737 IC50 = 4700.0 nM 5.33
CHEMBL4172372 IC50 = 4700.0 nM 5.33
CHEMBL4174957 IC50 = 4700.0 nM 5.33
CHEMBL4167074 IC50 = 4900.0 nM 5.31
CHEMBL4172781 IC50 = 5500.0 nM 5.26
CHEMBL4168315 IC50 = 7300.0 nM 5.14
CHEMBL4170063 IC50 = 8100.0 nM 5.09
CHEMBL1651180 IC50 = 8900.0 nM 5.05
CHEMBL772 RESERPINE IC50 = 9200.0 nM 5.04
CHEMBL4169246 IC50 = 9400.0 nM 5.03
CHEMBL4171241 IC50 = 9900.0 nM 5.00
CHEMBL4169390 IC50 = 11900.0 nM 4.92
CHEMBL4164881 IC50 = 13700.0 nM 4.86
CHEMBL4176869 IC50 = 15600.0 nM 4.81
CHEMBL4161319 IC50 = 19100.0 nM 4.72
CHEMBL4160603 IC50 - -
CHEMBL4176571 IC50 - -
CHEMBL4165958 IC50 - -
CHEMBL4161465 IC50 - -
CHEMBL4172302 IC50 - -
CHEMBL4169005 IC50 - -
CHEMBL4171219 IC50 - -
CHEMBL4165580 IC50 - -
CHEMBL4173512 IC50 - -
CHEMBL4165585 IC50 - -
CHEMBL4163206 IC50 - -
CHEMBL4173927 IC50 - -
CHEMBL4166649 IC50 - -
CHEMBL4177278 IC50 - -
CHEMBL4172633 IC50 - -
CHEMBL4173506 IC50 - -