Assay Detail
ADMET
CHEMBL4040124
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Inhibition of human NaV1.5 expressed in HEK cells assessed as half inactivation potential at -120 mV holding potential by automated patch clamp method
26
Total Activities
26
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 5 subunit alpha (CHEMBL1980) ↗| 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 | 26 | 4.67 | 4.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2325601 | — | — | 1 | 4.98 |
| CHEMBL2325619 | — | — | 1 | 4.96 |
| CHEMBL2325627 | — | — | 1 | 4.84 |
| CHEMBL2324411 | — | — | 1 | 4.82 |
| CHEMBL2325330 | — | — | 1 | 4.77 |
| CHEMBL2324396 | — | — | 1 | 4.65 |
| CHEMBL2325350 | — | — | 1 | 4.65 |
| CHEMBL2324742 | — | — | 1 | 4.60 |
| CHEMBL2324405 | — | — | 1 | 4.59 |
| CHEMBL2323100 | — | — | 1 | 4.59 |
| CHEMBL2323074 | — | — | 1 | 4.59 |
| CHEMBL2325622 | — | — | 1 | 4.53 |
| CHEMBL2325021 | — | — | 1 | 4.45 |
| CHEMBL2323073 | — | — | 1 | 4.36 |
| CHEMBL2324748 | PF-05150122 | 1.0 | 1 | - |
| CHEMBL2325317 | — | — | 1 | - |
| CHEMBL2324753 | — | — | 1 | - |
| CHEMBL2325014 | PF-05089771 | 2.0 | 1 | - |
| CHEMBL2325020 | — | — | 1 | - |
| CHEMBL2324776 | PF-05186462 | 1.0 | 1 | - |
| CHEMBL2325013 | — | — | 1 | - |
| CHEMBL2325038 | — | — | 1 | - |
| CHEMBL2324391 | — | — | 1 | - |
| CHEMBL2324388 | — | — | 1 | - |
| CHEMBL2322421 | — | — | 1 | - |
| CHEMBL2324755 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2325601 | — | IC50 | = | 10549.0 | nM | 4.98 |
| CHEMBL2325619 | — | IC50 | = | 11102.0 | nM | 4.96 |
| CHEMBL2325627 | — | IC50 | = | 14413.0 | nM | 4.84 |
| CHEMBL2324411 | — | IC50 | = | 15060.0 | nM | 4.82 |
| CHEMBL2325330 | — | IC50 | = | 17060.0 | nM | 4.77 |
| CHEMBL2324396 | — | IC50 | = | 22451.0 | nM | 4.65 |
| CHEMBL2325350 | — | IC50 | = | 22210.0 | nM | 4.65 |
| CHEMBL2324742 | — | IC50 | = | 25231.0 | nM | 4.60 |
| CHEMBL2324405 | — | IC50 | = | 25786.0 | nM | 4.59 |
| CHEMBL2323100 | — | IC50 | = | 25448.0 | nM | 4.59 |
| CHEMBL2323074 | — | IC50 | = | 25578.0 | nM | 4.59 |
| CHEMBL2325622 | — | IC50 | = | 29291.0 | nM | 4.53 |
| CHEMBL2325021 | — | IC50 | = | 35118.0 | nM | 4.45 |
| CHEMBL2323073 | — | IC50 | = | 43699.0 | nM | 4.36 |
| CHEMBL2324748 | PF-05150122 | IC50 | > | 30000.0 | nM | - |
| CHEMBL2325317 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2324753 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2325014 | PF-05089771 | IC50 | > | 10000.0 | nM | - |
| CHEMBL2325020 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2324776 | PF-05186462 | IC50 | > | 30000.0 | nM | - |
| CHEMBL2325013 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2325038 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2324391 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2324388 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2322421 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2324755 | — | IC50 | > | 30000.0 | nM | - |