Assay Detail
Binding
CHEMBL4040131
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of rat NaV1.7 expressed in HEK cells assessed as half inactivation potential at -120 mV holding potential by automated patch clamp method
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium channel protein type 9 subunit alpha (CHEMBL3312) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of NaV1.7.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.12 | 6.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2324411 | — | — | 1 | 6.91 |
| CHEMBL2325014 | PF-05089771 | 2.0 | 1 | 6.82 |
| CHEMBL2324753 | — | — | 1 | 6.09 |
| CHEMBL2324748 | PF-05150122 | 1.0 | 1 | 5.50 |
| CHEMBL2324776 | PF-05186462 | 1.0 | 1 | 5.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2324411 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL2325014 | PF-05089771 | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL2324753 | — | IC50 | = | 813.0 | nM | 6.09 |
| CHEMBL2324748 | PF-05150122 | IC50 | = | 3140.0 | nM | 5.50 |
| CHEMBL2324776 | PF-05186462 | IC50 | = | 5450.0 | nM | 5.26 |