Assay Detail
ADMET
CHEMBL4040126
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human NaV1.1 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 | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium channel protein type 1 subunit alpha (CHEMBL1845) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 5.97 | 6.67 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2324411 | — | — | 1 | 6.67 |
| CHEMBL2325014 | PF-05089771 | 2.0 | 1 | 6.17 |
| CHEMBL2324776 | PF-05186462 | 1.0 | 1 | 5.06 |
| CHEMBL2324753 | — | — | 1 | - |
| CHEMBL2324748 | PF-05150122 | 1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2324411 | — | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL2325014 | PF-05089771 | IC50 | = | 677.0 | nM | 6.17 |
| CHEMBL2324776 | PF-05186462 | IC50 | = | 8750.0 | nM | 5.06 |
| CHEMBL2324753 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL2324748 | PF-05150122 | IC50 | > | 10000.0 | nM | - |