Assay Detail
ADMET
CHEMBL4623819
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Inhibition of human NaV1.5/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method
20
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HEK293-A |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium channel protein type 5 subunit alpha/beta-1/beta-2 (CHEMBL4630763) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Discovery of DS-1971a, a Potent, Selective Na<sub>V</sub>1.7 Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 4.20 | 4.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4632675 | — | — | 1 | 4.55 |
| CHEMBL4642571 | — | — | 1 | 4.40 |
| CHEMBL4633573 | — | — | 1 | 4.20 |
| CHEMBL2325622 | — | — | 1 | 4.12 |
| CHEMBL4648771 | — | — | 1 | 4.08 |
| CHEMBL4633566 | DS-1971 | 2.0 | 2 | 4.03 |
| CHEMBL4642940 | — | — | 1 | 4.02 |
| CHEMBL2325014 | PF-05089771 | 2.0 | 1 | - |
| CHEMBL4644497 | — | — | 1 | - |
| CHEMBL4641238 | — | — | 1 | - |
| CHEMBL4635030 | — | — | 1 | - |
| CHEMBL4642726 | — | — | 1 | - |
| CHEMBL4647897 | — | — | 1 | - |
| CHEMBL4645788 | — | — | 1 | - |
| CHEMBL4648397 | — | — | 1 | - |
| CHEMBL4637909 | — | — | 1 | - |
| CHEMBL4637488 | — | — | 1 | - |
| CHEMBL4639987 | — | — | 1 | - |
| CHEMBL4640756 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4632675 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL4642571 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL4633573 | — | IC50 | = | 63000.0 | nM | 4.20 |
| CHEMBL2325622 | — | IC50 | = | 75000.0 | nM | 4.12 |
| CHEMBL4648771 | — | IC50 | = | 84000.0 | nM | 4.08 |
| CHEMBL4633566 | DS-1971 | IC50 | = | 93000.0 | nM | 4.03 |
| CHEMBL4642940 | — | IC50 | = | 96000.0 | nM | 4.02 |
| CHEMBL2325014 | PF-05089771 | IC50 | > | 100000.0 | nM | - |
| CHEMBL4644497 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4641238 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4635030 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4642726 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4640756 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4645788 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4648397 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4637909 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4633566 | DS-1971 | IC50 | > | 100000.0 | nM | - |
| CHEMBL4637488 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4639987 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4647897 | — | IC50 | - | — | - |