Assay Detail
Binding
CHEMBL5501650
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Binding affinity to human androgen receptor transfected in HEK293 cell membrane co-transfected with ARC1 assessed as inhibition of [3H]-methyltrienolone binding to receptor incubated for 30 mins by competitive ligand binding assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel selective agents for the degradation of AR/AR-V7 to treat advanced prostate cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 8.25 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5437141 | — | — | 1 | 8.82 |
| CHEMBL5555049 | — | — | 1 | 8.44 |
| CHEMBL5517689 | — | — | 1 | 8.34 |
| CHEMBL5532063 | — | — | 1 | 8.27 |
| CHEMBL5531958 | — | — | 1 | 8.24 |
| CHEMBL5557418 | — | — | 1 | 8.17 |
| CHEMBL5559204 | — | — | 1 | 8.04 |
| CHEMBL5557813 | — | — | 1 | 8.02 |
| CHEMBL5555724 | — | — | 1 | 7.91 |
| CHEMBL5532027 | — | — | 1 | - |
| CHEMBL5557950 | — | — | 1 | - |
| CHEMBL5512492 | — | — | 1 | - |
| CHEMBL5523394 | — | — | 1 | - |
| CHEMBL5558969 | — | — | 1 | - |
| CHEMBL5542581 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5437141 | — | IC50 | = | 1.52 | nM | 8.82 |
| CHEMBL5555049 | — | IC50 | = | 3.67 | nM | 8.44 |
| CHEMBL5517689 | — | IC50 | = | 4.55 | nM | 8.34 |
| CHEMBL5532063 | — | IC50 | = | 5.41 | nM | 8.27 |
| CHEMBL5531958 | — | IC50 | = | 5.72 | nM | 8.24 |
| CHEMBL5557418 | — | IC50 | = | 6.81 | nM | 8.17 |
| CHEMBL5559204 | — | IC50 | = | 9.22 | nM | 8.04 |
| CHEMBL5557813 | — | IC50 | = | 9.51 | nM | 8.02 |
| CHEMBL5555724 | — | IC50 | = | 12.36 | nM | 7.91 |
| CHEMBL5532027 | — | IC50 | - | — | - | |
| CHEMBL5557950 | — | IC50 | - | — | - | |
| CHEMBL5512492 | — | IC50 | - | — | - | |
| CHEMBL5523394 | — | IC50 | - | — | - | |
| CHEMBL5558969 | — | IC50 | - | — | - | |
| CHEMBL5542581 | — | IC50 | - | — | - |