Assay Detail
ADMET
CHEMBL4040132
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Inhibition of CYP3A4 (unknown origin)
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 |
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 | 5.84 | 6.69 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2325013 | — | — | 1 | 6.69 |
| CHEMBL2324742 | — | — | 1 | 6.40 |
| CHEMBL2325622 | — | — | 1 | 6.37 |
| CHEMBL2325330 | — | — | 1 | 6.30 |
| CHEMBL2324753 | — | — | 1 | 6.25 |
| CHEMBL2323073 | — | — | 1 | 6.21 |
| CHEMBL2325619 | — | — | 1 | 6.13 |
| CHEMBL2325038 | — | — | 1 | 6.08 |
| CHEMBL2323074 | — | — | 1 | 6.04 |
| CHEMBL2324391 | — | — | 1 | 5.98 |
| CHEMBL2325021 | — | — | 1 | 5.90 |
| CHEMBL2324755 | — | — | 1 | 4.96 |
| CHEMBL2324748 | PF-05150122 | 1.0 | 1 | 4.91 |
| CHEMBL2325317 | — | — | 1 | 4.82 |
| CHEMBL2324405 | — | — | 1 | 4.58 |
| CHEMBL2325014 | PF-05089771 | 2.0 | 1 | - |
| CHEMBL2325020 | — | — | 1 | - |
| CHEMBL2325601 | — | — | 1 | - |
| CHEMBL2325627 | — | — | 1 | - |
| CHEMBL2324396 | — | — | 1 | - |
| CHEMBL2324776 | PF-05186462 | 1.0 | 1 | - |
| CHEMBL2324388 | — | — | 1 | - |
| CHEMBL2322421 | — | — | 1 | - |
| CHEMBL2323100 | — | — | 1 | - |
| CHEMBL2325350 | — | — | 1 | - |
| CHEMBL2324411 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2325013 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL2324742 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2325622 | — | IC50 | = | 427.0 | nM | 6.37 |
| CHEMBL2325330 | — | IC50 | = | 505.0 | nM | 6.30 |
| CHEMBL2324753 | — | IC50 | = | 556.0 | nM | 6.25 |
| CHEMBL2323073 | — | IC50 | = | 616.0 | nM | 6.21 |
| CHEMBL2325619 | — | IC50 | = | 737.0 | nM | 6.13 |
| CHEMBL2325038 | — | IC50 | = | 827.0 | nM | 6.08 |
| CHEMBL2323074 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL2324391 | — | IC50 | = | 1058.0 | nM | 5.98 |
| CHEMBL2325021 | — | IC50 | = | 1271.0 | nM | 5.90 |
| CHEMBL2324755 | — | IC50 | = | 11068.0 | nM | 4.96 |
| CHEMBL2324748 | PF-05150122 | IC50 | = | 12239.0 | nM | 4.91 |
| CHEMBL2325317 | — | IC50 | = | 15124.0 | nM | 4.82 |
| CHEMBL2324405 | — | IC50 | = | 26588.0 | nM | 4.58 |
| CHEMBL2325014 | PF-05089771 | IC50 | > | 30000.0 | nM | - |
| CHEMBL2325020 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2325601 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2325627 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2324396 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2324776 | PF-05186462 | IC50 | > | 11248.0 | nM | - |
| CHEMBL2324388 | — | IC50 | - | — | - | |
| CHEMBL2322421 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2323100 | — | IC50 | - | — | - | |
| CHEMBL2325350 | — | IC50 | < | 30.0 | nM | - |
| CHEMBL2324411 | — | IC50 | - | — | - |