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Assay Detail

CHEMBL2390113

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

Binding
Inhibition of NorA in Staphylococcus aureus 1199B harboring grlA A116E mutant assessed as inhibition of ethidium bromide efflux measured for 5 mins by fluorometric analysis
28
Total Activities
28
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

Re-evolution of the 2-phenylquinolines: ligand-based design, synthesis, and biological evaluation of a potent new class of Staphylococcus aureus NorA efflux pump inhibitors to combat antimicrobial resistance.
Sabatini S, Gosetto F, Iraci N, Barreca ML, Massari S, Sancineto L, Manfroni G, Tabarrini O, Dimovska M, Kaatz GW, Cecchetti V.
J Med Chem (2013) 56 : 4975 -4989
PubMed 23710549 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 5.08 5.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2385690 1 5.42
CHEMBL2385681 1 5.41
CHEMBL2385684 1 5.19
CHEMBL2385677 1 5.12
CHEMBL2385678 1 5.10
CHEMBL2385688 1 5.08
CHEMBL2385680 1 5.08
CHEMBL2385667 1 5.07
CHEMBL1651180 1 5.05
CHEMBL772 RESERPINE 4.0 1 5.04
CHEMBL2385691 1 5.04
CHEMBL2385683 1 5.03
CHEMBL2385675 1 5.03
CHEMBL2385689 1 5.01
CHEMBL2385670 1 5.00
CHEMBL2385682 1 4.97
CHEMBL2385676 1 4.88
CHEMBL2385679 1 4.83
CHEMBL2385668 1 -
CHEMBL2385692 1 -
CHEMBL2385687 1 -
CHEMBL2385686 1 -
CHEMBL2385685 1 -
CHEMBL2385674 1 -
CHEMBL2385673 1 -
CHEMBL2385672 1 -
CHEMBL2385671 1 -
CHEMBL2385669 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2385690 IC50 = 3800.0 nM 5.42
CHEMBL2385681 IC50 = 3900.0 nM 5.41
CHEMBL2385684 IC50 = 6400.0 nM 5.19
CHEMBL2385677 IC50 = 7500.0 nM 5.12
CHEMBL2385678 IC50 = 8000.0 nM 5.10
CHEMBL2385688 IC50 = 8300.0 nM 5.08
CHEMBL2385680 IC50 = 8300.0 nM 5.08
CHEMBL2385667 IC50 = 8500.0 nM 5.07
CHEMBL1651180 IC50 = 8900.0 nM 5.05
CHEMBL772 RESERPINE IC50 = 9200.0 nM 5.04
CHEMBL2385691 IC50 = 9200.0 nM 5.04
CHEMBL2385683 IC50 = 9300.0 nM 5.03
CHEMBL2385675 IC50 = 9300.0 nM 5.03
CHEMBL2385689 IC50 = 9700.0 nM 5.01
CHEMBL2385670 IC50 = 9900.0 nM 5.00
CHEMBL2385682 IC50 = 10700.0 nM 4.97
CHEMBL2385676 IC50 = 13300.0 nM 4.88
CHEMBL2385679 IC50 = 14800.0 nM 4.83
CHEMBL2385668 IC50 - -
CHEMBL2385692 IC50 - -
CHEMBL2385687 IC50 - -
CHEMBL2385686 IC50 - -
CHEMBL2385685 IC50 - -
CHEMBL2385674 IC50 - -
CHEMBL2385673 IC50 - -
CHEMBL2385672 IC50 - -
CHEMBL2385671 IC50 - -
CHEMBL2385669 IC50 - -