Assay Detail
Toxicity
CHEMBL5387422
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Inhibition of hERG fluorescence polarization assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Toxicity |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Amide containing NBTI antibacterials with reduced hERG inhibition, retained antimicrobial activity against gram-positive bacteria and in vivo efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.15 | 7.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5420593 | — | — | 1 | 7.02 |
| CHEMBL5441103 | — | — | 1 | 6.91 |
| CHEMBL5395597 | — | — | 1 | 6.75 |
| CHEMBL4873479 | — | — | 1 | 6.53 |
| CHEMBL5428752 | — | — | 1 | 5.70 |
| CHEMBL5402120 | — | — | 1 | 5.33 |
| CHEMBL5417501 | — | — | 1 | 4.79 |
| CHEMBL5432283 | — | — | 1 | - |
| CHEMBL5431772 | — | — | 1 | - |
| CHEMBL5429864 | — | — | 1 | - |
| CHEMBL5394250 | — | — | 1 | - |
| CHEMBL5406927 | — | — | 1 | - |
| CHEMBL5421348 | — | — | 1 | - |
| CHEMBL3317856 | GEPOTIDACIN | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5420593 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL5441103 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL5395597 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL4873479 | — | IC50 | = | 296.0 | nM | 6.53 |
| CHEMBL5428752 | — | IC50 | = | 2020.0 | nM | 5.70 |
| CHEMBL5402120 | — | IC50 | = | 4628.0 | nM | 5.33 |
| CHEMBL5417501 | — | IC50 | = | 16070.0 | nM | 4.79 |
| CHEMBL5432283 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5431772 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5429864 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5394250 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5406927 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5421348 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3317856 | GEPOTIDACIN | IC50 | > | 30000.0 | nM | - |