Assay Detail
Toxicity
CHEMBL5133258
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Displacement of MK499 from human ERG expressed in HEK membrane by radio ligand binding competition assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Toxicity |
| Organism | Homo sapiens |
| Cell Type | HEK |
| Subcellular | Cell membrane |
| 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
Design and discovery of C2-fluoroalkyl iminothiazine dioxides as BACE inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 4.71 | 5.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5204704 | — | — | 1 | 5.62 |
| CHEMBL3937515 | — | — | 1 | 5.13 |
| CHEMBL5208596 | — | — | 1 | 4.83 |
| CHEMBL5174392 | — | — | 1 | 4.80 |
| CHEMBL5203401 | — | — | 1 | 4.64 |
| CHEMBL5197842 | — | — | 1 | 4.62 |
| CHEMBL5170892 | — | — | 1 | 4.59 |
| CHEMBL5190011 | — | — | 1 | 4.57 |
| CHEMBL5195553 | — | — | 1 | 4.41 |
| CHEMBL5198665 | — | — | 1 | 4.32 |
| CHEMBL5194897 | — | — | 1 | 4.27 |
| CHEMBL5195634 | — | — | 1 | - |
| CHEMBL5203915 | — | — | 1 | - |
| CHEMBL5170080 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5204704 | — | IC50 | = | 2424.0 | nM | 5.62 |
| CHEMBL3937515 | — | IC50 | = | 7464.0 | nM | 5.13 |
| CHEMBL5208596 | — | IC50 | = | 14670.0 | nM | 4.83 |
| CHEMBL5174392 | — | IC50 | = | 15890.0 | nM | 4.80 |
| CHEMBL5203401 | — | IC50 | = | 23120.0 | nM | 4.64 |
| CHEMBL5197842 | — | IC50 | = | 24240.0 | nM | 4.62 |
| CHEMBL5170892 | — | IC50 | = | 25560.0 | nM | 4.59 |
| CHEMBL5190011 | — | IC50 | = | 26850.0 | nM | 4.57 |
| CHEMBL5195553 | — | IC50 | = | 38900.0 | nM | 4.41 |
| CHEMBL5198665 | — | IC50 | = | 48150.0 | nM | 4.32 |
| CHEMBL5194897 | — | IC50 | = | 54230.0 | nM | 4.27 |
| CHEMBL5195634 | — | IC50 | > | 55180.0 | nM | - |
| CHEMBL5203915 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL5170080 | — | IC50 | > | 60000.0 | nM | - |