Assay Detail
Binding
CHEMBL4479399
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Inhibition of DHT-induced androgen receptor transactivation in human LNCaP cells after 24 hrs by luciferase reporter gene assay relative to control
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | LNCaP |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of Novel Steroidal Androgen Receptor Degrading Agents Inspired by Galeterone 3β-Imidazole Carbamate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 6.40 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1082407 | ENZALUTAMIDE | 4.0 | 1 | 6.75 |
| CHEMBL4591875 | — | — | 1 | 6.72 |
| CHEMBL4539707 | — | — | 1 | 6.33 |
| CHEMBL4541575 | — | — | 1 | 5.78 |
| CHEMBL4532487 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1082407 | ENZALUTAMIDE | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4591875 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4539707 | — | EC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4541575 | — | EC50 | = | 1650.0 | nM | 5.78 |
| CHEMBL4532487 | — | EC50 | > | 100.0 | nM | - |