Assay Detail
Binding
CHEMBL4376261
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 (DE3) Rosetta T1R cells assessed as reduction in S-adenosyl-L-homocysteine production preincubated for 15 mins followed by 1.5 uM of tRNALeu(CAG) substrate and SAM addition and measured after 45 mins by MTase-Glo assay
26
Total Activities
26
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 | 26 | 6.41 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4517402 | — | — | 1 | 7.62 |
| CHEMBL4513615 | — | — | 1 | 7.60 |
| CHEMBL4447065 | — | — | 1 | 7.10 |
| CHEMBL4463176 | — | — | 1 | 7.07 |
| CHEMBL4555967 | — | — | 1 | 6.96 |
| CHEMBL4543513 | — | — | 1 | 6.96 |
| CHEMBL4580116 | — | — | 1 | 6.89 |
| CHEMBL4437560 | — | — | 1 | 6.85 |
| CHEMBL4469887 | — | — | 1 | 6.82 |
| CHEMBL2431997 | — | — | 1 | 6.75 |
| CHEMBL4460223 | — | — | 1 | 6.68 |
| CHEMBL4458857 | — | — | 1 | 6.43 |
| CHEMBL4544475 | — | — | 1 | 6.42 |
| CHEMBL4442893 | — | — | 1 | 6.35 |
| CHEMBL4435700 | — | — | 1 | 6.31 |
| CHEMBL4547571 | — | — | 1 | 6.16 |
| CHEMBL4453557 | — | — | 1 | 6.14 |
| CHEMBL4439772 | — | — | 1 | 6.14 |
| CHEMBL4584637 | — | — | 1 | 6.10 |
| CHEMBL4464383 | — | — | 1 | 5.96 |
| CHEMBL4446167 | — | — | 1 | 5.89 |
| CHEMBL4459537 | — | — | 1 | 5.75 |
| CHEMBL4448124 | — | — | 1 | 5.66 |
| CHEMBL4541348 | — | — | 1 | 5.66 |
| CHEMBL4585250 | — | — | 1 | 5.52 |
| CHEMBL4564647 | — | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4517402 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4513615 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4447065 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4463176 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4555967 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4543513 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4580116 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4437560 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4469887 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2431997 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4460223 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4458857 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4544475 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4442893 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4435700 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4547571 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4453557 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL4439772 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL4584637 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL4464383 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4446167 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4459537 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4448124 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4541348 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4585250 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4564647 | — | IC50 | = | 12000.0 | nM | 4.92 |