Assay Detail
Functional
CHEMBL2020474
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Negative inotropic activity in guinea pig left atria assessed as decrease of 1 Hz current-induced developed tension
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Cardiac atrium |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Synthesis and toxicopharmacological evaluation of m-hydroxymexiletine, the first metabolite of mexiletine more potent than the parent compound on voltage-gated sodium channels.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 7.09 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL569 | PROCAINE | 4.0 | 1 | 7.85 |
| CHEMBL79 | LIDOCAINE | 4.0 | 1 | 7.77 |
| CHEMBL558 | MEXILETINE | 4.0 | 1 | 7.35 |
| CHEMBL2018453 | — | — | 1 | 7.01 |
| CHEMBL1294 | QUINIDINE | 4.0 | 1 | 5.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL569 | PROCAINE | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL79 | LIDOCAINE | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL558 | MEXILETINE | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL2018453 | — | EC50 | = | 98.0 | nM | 7.01 |
| CHEMBL1294 | QUINIDINE | EC50 | = | 3380.0 | nM | 5.47 |