Assay Detail
Binding
CHEMBL830974
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Displacement of [3H]R-1881 from Androgen receptor of PC3-AR cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PC3-AR |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.17 | 6.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL77789 | — | — | 1 | 6.62 |
| CHEMBL74606 | — | — | 1 | 6.44 |
| CHEMBL77062 | — | — | 1 | 6.43 |
| CHEMBL75474 | — | — | 1 | 6.42 |
| CHEMBL806 | FLUTAMIDE | 4.0 | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL77789 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL74606 | — | IC50 | = | 366.0 | nM | 6.44 |
| CHEMBL77062 | — | IC50 | = | 374.0 | nM | 6.43 |
| CHEMBL75474 | — | IC50 | = | 384.0 | nM | 6.42 |
| CHEMBL806 | FLUTAMIDE | IC50 | = | 10985.0 | nM | 4.96 |