Assay Detail
Binding
CHEMBL4376263
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Pseudomonas aeruginosa tRNA (guanine(37)-N1)-methyltransferase (Leu5 to Asp25 residues) expressed in Escherichia coli BL21 Rosetta (DE3) assessed as reduction in S-adenosyl-L-homocysteine production preincubated for 15 mins followed by 15 uM of tRNALeu(CAG) substrate and SAM addition and measured after 45 mins by MTase-Glo assay
2
Total Activities
2
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
tRNA (guanine-N(1)-)-methyltransferase (CHEMBL4523932) ↗| Type | SINGLE PROTEIN |
| Organism | Pseudomonas aeruginosa (strain ATCC 15692 / DSM 22644 / CIP 104116 / JCM14847 / LMG 12228 / 1C / PRS 101 / PAO1) |
Publication
Thienopyrimidinone Derivatives That Inhibit Bacterial tRNA (Guanine37-<i>N</i><sup>1</sup>)-Methyltransferase (TrmD) by Restructuring the Active Site with a Tyrosine-Flipping Mechanism.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 6.33 | 6.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4517402 | — | — | 1 | 6.58 |
| CHEMBL2431997 | — | — | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4517402 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL2431997 | — | IC50 | = | 840.0 | nM | 6.08 |