Assay Detail
Binding
CHEMBL981950
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]astemizole from human ERG potassium channel expressed in HEK293 cell membrane
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.39 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL482056 | — | — | 1 | 6.30 |
| CHEMBL481863 | — | — | 1 | 6.00 |
| CHEMBL482058 | — | — | 1 | 6.00 |
| CHEMBL470929 | — | — | 1 | 5.75 |
| CHEMBL470753 | — | — | 1 | 5.70 |
| CHEMBL472138 | — | — | 1 | 5.57 |
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 1 | 5.57 |
| CHEMBL446514 | — | — | 1 | 5.52 |
| CHEMBL482057 | — | — | 1 | 5.30 |
| CHEMBL520942 | — | — | 1 | 5.05 |
| CHEMBL480130 | — | — | 1 | 4.82 |
| CHEMBL480131 | — | — | 1 | 4.70 |
| CHEMBL518155 | — | — | 1 | 4.62 |
| CHEMBL479382 | — | — | 1 | 4.52 |
| CHEMBL454760 | — | — | 1 | - |
| CHEMBL479752 | — | — | 1 | - |
| CHEMBL517533 | — | — | 1 | - |
| CHEMBL511292 | — | — | 1 | - |
| CHEMBL479383 | — | — | 1 | - |
| CHEMBL481280 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL482056 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL481863 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL482058 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL470929 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL470753 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL472138 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL296419 | ASTEMIZOLE | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL446514 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL482057 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL520942 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL480130 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL480131 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL518155 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL479382 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL454760 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL479752 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL517533 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL511292 | — | IC50 | - | — | - | |
| CHEMBL479383 | — | IC50 | > | 16000.0 | nM | - |
| CHEMBL481280 | — | IC50 | > | 30000.0 | nM | - |