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Assay Detail

CHEMBL4404074

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

Binding
Inhibition of LasR in Pseudomonas aeruginosa PAO-JP2 harboring plasI-LVAgfp incubated for 6 hrs by fluorescence method
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Pseudomonas aeruginosa
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Transcriptional activator protein LasR (CHEMBL1075207)
Type SINGLE PROTEIN
Organism Pseudomonas aeruginosa (strain ATCC 15692 / PAO1 / 1C / PRS 101 / LMG12228)

Publication

Impact of the structure-activity relationship of AHL analogues on quorum sensing in Gram-negative bacteria.
Chbib C.
Bioorg Med Chem (2020) 28 : 115282 -115282
PubMed 31918952 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 4.90 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1818523 1 5.60
CHEMBL468624 1 5.52
CHEMBL1823942 1 5.28
CHEMBL463321 1 5.26
CHEMBL4549418 1 5.01
CHEMBL264944 1 4.92
CHEMBL1615001 1 4.68
CHEMBL458201 1 4.40
CHEMBL1823945 1 4.16
CHEMBL473592 1 4.14
CHEMBL2229607 N-CYCLOPENTYLDECANAMIDE 1 -
CHEMBL584972 1 -
CHEMBL575294 1 -
CHEMBL448002 1 -
CHEMBL4544667 1 -
CHEMBL4522587 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1818523 IC50 = 2500.0 nM 5.60
CHEMBL468624 IC50 = 3000.0 nM 5.52
CHEMBL1823942 IC50 = 5200.0 nM 5.28
CHEMBL463321 IC50 = 5500.0 nM 5.26
CHEMBL4549418 IC50 = 9700.0 nM 5.01
CHEMBL264944 IC50 = 12000.0 nM 4.92
CHEMBL1615001 IC50 = 21000.0 nM 4.68
CHEMBL458201 IC50 = 40000.0 nM 4.40
CHEMBL1823945 IC50 = 69000.0 nM 4.16
CHEMBL473592 IC50 = 73000.0 nM 4.14
CHEMBL2229607 N-CYCLOPENTYLDECANAMIDE IC50 > 50000.0 nM -
CHEMBL584972 IC50 > 100000.0 nM -
CHEMBL575294 IC50 = 116000.0 nM -
CHEMBL448002 IC50 = 175000.0 nM -
CHEMBL4544667 IC50 > 200000.0 nM -
CHEMBL4522587 IC50 > 100000.0 nM -