Assay Detail
Binding
CHEMBL3294033
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG by patch clamp electrophysiological analysis
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 4.61 | 5.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3286436 | — | — | 1 | 5.60 |
| CHEMBL3290338 | — | — | 1 | 5.28 |
| CHEMBL3290342 | — | — | 1 | 5.00 |
| CHEMBL3290345 | — | — | 1 | 4.92 |
| CHEMBL3290347 | — | — | 1 | 4.89 |
| CHEMBL3290336 | — | — | 1 | 4.68 |
| CHEMBL3290339 | — | — | 1 | 4.58 |
| CHEMBL3290343 | — | — | 1 | 4.48 |
| CHEMBL2165062 | — | — | 1 | 4.36 |
| CHEMBL3290341 | — | — | 1 | 4.30 |
| CHEMBL3290346 | — | — | 1 | 4.16 |
| CHEMBL3290340 | — | — | 1 | 4.16 |
| CHEMBL3290344 | — | — | 1 | 4.13 |
| CHEMBL3290351 | — | — | 1 | 4.05 |
| CHEMBL3290337 | — | — | 1 | - |
| CHEMBL3290348 | — | — | 1 | - |
| CHEMBL3290349 | — | — | 1 | - |
| CHEMBL3290350 | — | — | 1 | - |
| CHEMBL3290352 | — | — | 1 | - |
| CHEMBL3290353 | — | — | 1 | - |
| CHEMBL3290354 | — | — | 1 | - |
| CHEMBL3290355 | — | — | 1 | - |
| CHEMBL3290356 | — | — | 1 | - |
| CHEMBL3290357 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3286436 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3290338 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL3290342 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3290345 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL3290347 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL3290336 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL3290339 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL3290343 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL2165062 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL3290341 | — | IC50 | = | 50600.0 | nM | 4.30 |
| CHEMBL3290346 | — | IC50 | = | 69000.0 | nM | 4.16 |
| CHEMBL3290340 | — | IC50 | = | 69000.0 | nM | 4.16 |
| CHEMBL3290344 | — | IC50 | = | 74000.0 | nM | 4.13 |
| CHEMBL3290351 | — | IC50 | = | 90000.0 | nM | 4.05 |
| CHEMBL3290337 | — | IC50 | - | — | - | |
| CHEMBL3290348 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3290349 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3290350 | — | IC50 | = | 133000.0 | nM | - |
| CHEMBL3290352 | — | IC50 | = | 151000.0 | nM | - |
| CHEMBL3290353 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3290354 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3290355 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3290356 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3290357 | — | IC50 | > | 100000.0 | nM | - |