Assay Detail
Binding
CHEMBL4809529
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Inhibition of sodium channel (unknown origin) expressed in HEK cells assessed as reduction in late inward sodium current by automated patch clamp method
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Antiarrhythmic Hit to Lead Refinement in a Dish Using Patient-Derived iPSC Cardiomyocytes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.36 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4862853 | — | — | 1 | 6.70 |
| CHEMBL4850036 | — | — | 1 | 6.19 |
| CHEMBL4851381 | — | — | 1 | 6.13 |
| CHEMBL4851821 | — | — | 1 | 6.12 |
| CHEMBL4875966 | — | — | 1 | 5.99 |
| CHEMBL4875397 | — | — | 1 | 5.99 |
| CHEMBL4876024 | — | — | 1 | 5.99 |
| CHEMBL4872490 | — | — | 1 | 5.98 |
| CHEMBL4860330 | — | — | 1 | 5.13 |
| CHEMBL4853576 | — | — | 1 | 5.00 |
| CHEMBL4741603 | — | — | 1 | 4.94 |
| CHEMBL4742143 | — | — | 1 | 4.93 |
| CHEMBL4848088 | — | — | 1 | 4.76 |
| CHEMBL147507 | (R)-MEXILETINE | — | 1 | 4.72 |
| CHEMBL558 | MEXILETINE | 4.0 | 1 | 4.65 |
| CHEMBL146855 | (S)-MEXILETINE | — | 1 | 4.52 |
| CHEMBL4855496 | — | — | 1 | 4.44 |
| CHEMBL4867322 | — | — | 1 | 4.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4862853 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4850036 | — | IC50 | = | 643.0 | nM | 6.19 |
| CHEMBL4851381 | — | IC50 | = | 747.0 | nM | 6.13 |
| CHEMBL4851821 | — | IC50 | = | 753.0 | nM | 6.12 |
| CHEMBL4875966 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL4875397 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL4876024 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL4872490 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL4860330 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL4853576 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4741603 | — | IC50 | = | 11400.0 | nM | 4.94 |
| CHEMBL4742143 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL4848088 | — | IC50 | = | 17300.0 | nM | 4.76 |
| CHEMBL147507 | (R)-MEXILETINE | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL558 | MEXILETINE | IC50 | = | 22500.0 | nM | 4.65 |
| CHEMBL146855 | (S)-MEXILETINE | IC50 | = | 29900.0 | nM | 4.52 |
| CHEMBL4855496 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL4867322 | — | IC50 | = | 51800.0 | nM | 4.29 |