Assay Detail
Toxicity
CHEMBL5167326
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of hERG expressed in CHO cells stably at -80 mV holding potential by automated patch clamp method
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Toxicity |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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
Multiparameter Optimization of Naphthyridine Derivatives as Selective α5-GABA<sub>A</sub> Receptor Negative Allosteric Modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 5.19 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5189787 | — | — | 1 | 5.96 |
| CHEMBL5174424 | — | — | 1 | 5.75 |
| CHEMBL5176939 | — | — | 1 | 5.60 |
| CHEMBL5180133 | — | — | 1 | 5.54 |
| CHEMBL5179759 | — | — | 1 | 5.54 |
| CHEMBL5176141 | — | — | 1 | 5.50 |
| CHEMBL5170797 | — | — | 1 | 5.46 |
| CHEMBL5181374 | — | — | 1 | 5.44 |
| CHEMBL5207799 | — | — | 1 | 5.42 |
| CHEMBL5200752 | — | — | 1 | 5.38 |
| CHEMBL5208183 | — | — | 1 | 5.36 |
| CHEMBL5202280 | — | — | 1 | 5.28 |
| CHEMBL5189320 | — | — | 1 | 5.24 |
| CHEMBL5193778 | — | — | 1 | 5.24 |
| CHEMBL5186978 | — | — | 1 | 5.21 |
| CHEMBL5200451 | — | — | 1 | 5.19 |
| CHEMBL5174560 | — | — | 1 | 5.08 |
| CHEMBL5176630 | — | — | 1 | 5.04 |
| CHEMBL5185502 | — | — | 1 | 5.00 |
| CHEMBL5208332 | — | — | 1 | 5.00 |
| CHEMBL5178153 | — | — | 1 | 5.00 |
| CHEMBL5184265 | — | — | 1 | 4.68 |
| CHEMBL5195083 | — | — | 1 | 4.52 |
| CHEMBL5206831 | — | — | 1 | 4.52 |
| CHEMBL5192467 | — | — | 1 | 4.52 |
| CHEMBL5179688 | — | — | 1 | 4.52 |
| CHEMBL5197478 | — | — | 1 | - |
| CHEMBL5197481 | — | — | 1 | - |
| CHEMBL5200620 | — | — | 1 | - |
| CHEMBL5207798 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5189787 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5174424 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL5176939 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5180133 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL5179759 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL5176141 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL5170797 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL5181374 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL5207799 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL5200752 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL5208183 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL5202280 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL5189320 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL5193778 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL5186978 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL5200451 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL5174560 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL5176630 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL5185502 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL5208332 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL5178153 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL5184265 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL5195083 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL5206831 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL5192467 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL5179688 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL5197478 | — | IC50 | - | — | - | |
| CHEMBL5197481 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5200620 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5207798 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5199140 | — | IC50 | - | — | - | |
| CHEMBL5181673 | — | IC50 | - | — | - | |
| CHEMBL5193523 | — | IC50 | > | 10000.0 | nM | - |