Assay Detail
Binding
CHEMBL4017717
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at full length human androgen receptor expressed in mammalian expression system measured after 22 to 24 hrs by luciferase reporter gene assay
5
Total Activities
5
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
Novel small molecule guanidine Sigma1 inhibitors for advanced prostate cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 5.12 | 6.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1082407 | ENZALUTAMIDE | 4.0 | 1 | 6.38 |
| CHEMBL299499 | — | — | 1 | 5.02 |
| CHEMBL4084182 | — | — | 1 | 4.90 |
| CHEMBL271227 | ABIRATERONE ACETATE | 4.0 | 1 | 4.77 |
| CHEMBL4092687 | — | — | 1 | 4.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1082407 | ENZALUTAMIDE | EC50 | = | 420.0 | nM | 6.38 |
| CHEMBL299499 | — | EC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL4084182 | — | EC50 | = | 12680.0 | nM | 4.90 |
| CHEMBL271227 | ABIRATERONE ACETATE | EC50 | = | 17050.0 | nM | 4.77 |
| CHEMBL4092687 | — | EC50 | = | 28130.0 | nM | 4.55 |