Assay Detail
Binding
CHEMBL4429191
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Binding affinity to 16S rRNA A-site in Escherichia coli S30 extract assessed as inhibition of translation measured after 30 mins by coupled transcription/translation-based luciferase reporter gene assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Escherichia coli |
| Confidence | 3 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Effects of 5-O-Ribosylation of Aminoglycosides on Antimicrobial Activity and Selective Perturbation of Bacterial Translation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.75 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4462988 | — | — | 1 | 7.52 |
| CHEMBL176 | BEKANAMYCIN | 3.0 | 1 | 7.40 |
| CHEMBL177 | AMIKACIN | 4.0 | 1 | 7.16 |
| CHEMBL1747 | TOBRAMYCIN | 4.0 | 1 | 7.16 |
| CHEMBL4441386 | — | — | 1 | 7.10 |
| CHEMBL221572 | RIBOSTAMYCIN | 2.0 | 1 | 7.05 |
| CHEMBL1384 | KANAMYCIN | 4.0 | 1 | 7.00 |
| CHEMBL4554609 | — | — | 1 | 6.96 |
| CHEMBL4582037 | — | — | 1 | 6.37 |
| CHEMBL427409 | NEAMINE | — | 1 | 6.34 |
| CHEMBL4575515 | — | — | 1 | 5.71 |
| CHEMBL4470029 | — | — | 1 | 5.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4462988 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL176 | BEKANAMYCIN | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL177 | AMIKACIN | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1747 | TOBRAMYCIN | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4441386 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL221572 | RIBOSTAMYCIN | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1384 | KANAMYCIN | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4554609 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4582037 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL427409 | NEAMINE | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL4575515 | — | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL4470029 | — | IC50 | = | 6440.0 | nM | 5.19 |