Assay Detail
Binding
CHEMBL1826239
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Inhibition of human AR AF2 site expressed in human LNCap cells coexpressing eGFP -ARR2PB assessed as inhibition of transcriptional activity
9
Total Activities
6
Compounds Tested
2
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
Inhibitors of androgen receptor activation function-2 (AF2) site identified through virtual screening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 4.87 | 5.34 |
| Inhibition | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1302748 | — | — | 1 | 5.34 |
| CHEMBL1527972 | — | — | 1 | 5.23 |
| CHEMBL591628 | — | — | 1 | 4.96 |
| CHEMBL1822156 | — | — | 2 | 4.73 |
| CHEMBL1822157 | — | — | 2 | 4.48 |
| CHEMBL1822155 | — | — | 2 | 4.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1302748 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL1527972 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL591628 | — | IC50 | = | 11100.0 | nM | 4.96 |
| CHEMBL1822156 | — | IC50 | = | 18640.0 | nM | 4.73 |
| CHEMBL1822157 | — | IC50 | = | 33400.0 | nM | 4.48 |
| CHEMBL1822155 | — | IC50 | = | 34400.0 | nM | 4.46 |
| CHEMBL1822155 | — | Inhibition | - | % | - | |
| CHEMBL1822156 | — | Inhibition | - | % | - | |
| CHEMBL1822157 | — | Inhibition | - | % | - |