Assay Detail
Toxicity
CHEMBL5041728
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Inhibition of hERG expressed in HEK293 cells at -80 mV holding potential by automated patch-clamp method
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Toxicity |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
A Brain-Penetrant and Bioavailable Pyrazolopiperazine BACE1 Inhibitor Elicits Sustained Reduction of Amyloid β In Vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.39 | 5.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4521954 | — | — | 1 | 5.75 |
| CHEMBL5085412 | — | — | 1 | 5.48 |
| CHEMBL4525199 | — | — | 1 | 5.38 |
| CHEMBL5084378 | — | — | 1 | 5.34 |
| CHEMBL5085521 | — | — | 1 | 5.18 |
| CHEMBL5093303 | — | — | 1 | 5.18 |
| CHEMBL2152899 | — | — | 1 | - |
| CHEMBL5088449 | — | — | 1 | - |
| CHEMBL5075933 | — | — | 1 | - |
| CHEMBL5073381 | — | — | 1 | - |
| CHEMBL5093195 | — | — | 1 | - |
| CHEMBL5077699 | — | — | 1 | - |
| CHEMBL5082406 | — | — | 1 | - |
| CHEMBL5074068 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4521954 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL5085412 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4525199 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL5084378 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL5085521 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL5093303 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL2152899 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5088449 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5075933 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5073381 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5093195 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5077699 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5082406 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5074068 | — | IC50 | > | 10000.0 | nM | - |