Assay Detail
Binding
CHEMBL5045110
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Binding affinity to human AR LBD (663 to 920 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant in presence of DHT by biolayer interferometry assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of <i>N</i>-(4-(Benzyloxy)-phenyl)-sulfonamide Derivatives as Novel Antagonists of the Human Androgen Receptor Targeting the Activation Function 2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 2 | 4.12 | 4.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5085066 | — | — | 1 | 4.12 |
| CHEMBL1082407 | ENZALUTAMIDE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5085066 | — | Kd | = | 75870.0 | nM | 4.12 |
| CHEMBL1082407 | ENZALUTAMIDE | Kd | = | 295400.0 | nM | - |