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Assay Detail

CHEMBL2434715

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

Binding
Inhibition of Pseudomonas aeruginosa TrmD using S-[methyl-3H] adenosyl-L-methionine as substrate assessed as leucine-tRNA methylation after 1 hr by scintillation proximity assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Pseudomonas aeruginosa
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Selective inhibitors of bacterial t-RNA-(N(1)G37) methyltransferase (TrmD) that demonstrate novel ordering of the lid domain.
Hill PJ, Abibi A, Albert R, Andrews B, Gagnon MM, Gao N, Grebe T, Hajec LI, Huang J, Livchak S, Lahiri SD, McKinney DC, Thresher J, Wang H, Olivier N, Buurman ET.
J Med Chem (2013) 56 : 7278 -7288
PubMed 23981144 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.04 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2432010 1 7.36
CHEMBL2432016 1 7.20
CHEMBL2432011 1 7.17
CHEMBL2432000 1 7.01
CHEMBL2432017 1 6.92
CHEMBL2432013 1 6.60
CHEMBL2431997 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2432010 IC50 = 44.0 nM 7.36
CHEMBL2432016 IC50 = 63.0 nM 7.20
CHEMBL2432011 IC50 = 67.0 nM 7.17
CHEMBL2432000 IC50 = 98.0 nM 7.01
CHEMBL2432017 IC50 = 120.0 nM 6.92
CHEMBL2432013 IC50 = 250.0 nM 6.60
CHEMBL2431997 IC50 < 39.0 nM -