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Assay Detail

CHEMBL921466

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

Binding
Inhibition of Escherichia coli F plasmid TraI relaxase Y16F mutant assessed as oriT ssDNA cleavage by competitive inhibition assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Type IV secretion-like conjugative transfer relaxase protein TraI (CHEMBL4296318)
Type SINGLE PROTEIN
Organism Escherichia coli (strain SMS-3-5 / SECEC)

Publication

Disrupting antibiotic resistance propagation by inhibiting the conjugative DNA relaxase.
Lujan SA, Guogas LM, Ragonese H, Matson SW, Redinbo MR.
Proc Natl Acad Sci U S A (2007) 104 : 12282 -12287
PubMed 17630285 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.57 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL265450 IMIDODIPHOSPHATE 1 8.70
CHEMBL180570 MEDRONIC ACID 3.0 1 8.52
CHEMBL12318 CLODRONIC ACID 3.0 1 8.52
CHEMBL871 ETIDRONIC ACID 4.0 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL265450 IMIDODIPHOSPHATE Ki = 2.0 nM 8.70
CHEMBL180570 MEDRONIC ACID Ki = 3.0 nM 8.52
CHEMBL12318 CLODRONIC ACID Ki = 3.0 nM 8.52
CHEMBL871 ETIDRONIC ACID Ki = 3.0 nM 8.52