Assay Detail
Binding
CHEMBL995892
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Inhibition of Kca2.3 channel expressed in HEK293 cells by thallium flux assay
25
Total Activities
25
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Small conductance calcium-activated potassium channel protein 3 (CHEMBL3381) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Preliminary SAR studies on non-apamin-displacing 4-(aminomethylaryl)pyrrazolopyrimidine K(Ca) channel blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 5.51 | 9.78 |
| Activity | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL525408 | APAMIN | — | 1 | 9.78 |
| CHEMBL472452 | — | — | 1 | 6.46 |
| CHEMBL469732 | — | — | 1 | 6.00 |
| CHEMBL452406 | — | — | 1 | 5.96 |
| CHEMBL469756 | — | — | 1 | 5.28 |
| CHEMBL513544 | — | — | 1 | 5.12 |
| CHEMBL471826 | — | — | 1 | 5.10 |
| CHEMBL509297 | — | — | 1 | 5.00 |
| CHEMBL511783 | — | — | 1 | 4.97 |
| CHEMBL469540 | — | — | 1 | 4.96 |
| CHEMBL470804 | — | — | 1 | 4.84 |
| CHEMBL469539 | — | — | 1 | 4.84 |
| CHEMBL471192 | — | — | 1 | 4.81 |
| CHEMBL443165 | — | — | 1 | 4.80 |
| CHEMBL513561 | — | — | 1 | 4.72 |
| CHEMBL471852 | — | — | 1 | - |
| CHEMBL472028 | — | — | 1 | - |
| CHEMBL512698 | — | — | 1 | - |
| CHEMBL471193 | — | — | 1 | - |
| CHEMBL510479 | — | — | 1 | - |
| CHEMBL471194 | — | — | 1 | - |
| CHEMBL469731 | — | — | 1 | - |
| CHEMBL445782 | — | — | 1 | - |
| CHEMBL472402 | — | — | 1 | - |
| CHEMBL502413 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL525408 | APAMIN | IC50 | = | 0.168 | nM | 9.78 |
| CHEMBL472452 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL469732 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL452406 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL469756 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL513544 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL471826 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL509297 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL511783 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL469540 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL470804 | — | IC50 | = | 14600.0 | nM | 4.84 |
| CHEMBL469539 | — | IC50 | = | 14600.0 | nM | 4.84 |
| CHEMBL471192 | — | IC50 | = | 15400.0 | nM | 4.81 |
| CHEMBL443165 | — | IC50 | = | 15900.0 | nM | 4.80 |
| CHEMBL513561 | — | IC50 | = | 19100.0 | nM | 4.72 |
| CHEMBL471852 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL472028 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL512698 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL471193 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL510479 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL471194 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL469731 | — | Activity | - | — | - | |
| CHEMBL445782 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL472402 | — | Activity | - | — | - | |
| CHEMBL502413 | — | IC50 | > | 30000.0 | nM | - |