Assay Detail
Binding
CHEMBL5045078
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human androgen receptor expressed in human LNCap cells trasfected with ARR2PB-eGFP cells incubated for 3 days by fluorescence based AR transcription assay
28
Total Activities
28
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
Discovery of <i>N</i>-(4-(Benzyloxy)-phenyl)-sulfonamide Derivatives as Novel Antagonists of the Human Androgen Receptor Targeting the Activation Function 2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 5.68 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1082407 | ENZALUTAMIDE | 4.0 | 1 | 7.16 |
| CHEMBL5074175 | — | — | 1 | 6.96 |
| CHEMBL5085066 | — | — | 1 | 6.33 |
| CHEMBL5074767 | — | — | 1 | 5.81 |
| CHEMBL5077543 | — | — | 1 | 5.80 |
| CHEMBL5081582 | — | — | 1 | 5.75 |
| CHEMBL5074003 | — | — | 1 | 5.65 |
| CHEMBL5075240 | — | — | 1 | 5.64 |
| CHEMBL5090667 | — | — | 1 | 5.47 |
| CHEMBL5077404 | — | — | 1 | 5.38 |
| CHEMBL5085212 | — | — | 1 | 5.30 |
| CHEMBL5090685 | — | — | 1 | 5.24 |
| CHEMBL1463660 | — | — | 1 | 5.21 |
| CHEMBL5075580 | — | — | 1 | 5.15 |
| CHEMBL5086603 | — | — | 1 | 5.10 |
| CHEMBL5078718 | — | — | 1 | 4.94 |
| CHEMBL5084672 | — | — | 1 | - |
| CHEMBL5082552 | — | — | 1 | - |
| CHEMBL5088810 | — | — | 1 | - |
| CHEMBL5087539 | — | — | 1 | - |
| CHEMBL5074318 | — | — | 1 | - |
| CHEMBL5090120 | — | — | 1 | - |
| CHEMBL5078897 | — | — | 1 | - |
| CHEMBL5076171 | — | — | 1 | - |
| CHEMBL5088542 | — | — | 1 | - |
| CHEMBL5081224 | — | — | 1 | - |
| CHEMBL5091772 | — | — | 1 | - |
| CHEMBL5077660 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1082407 | ENZALUTAMIDE | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5074175 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5085066 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL5074767 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL5077543 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL5081582 | — | IC50 | = | 1770.0 | nM | 5.75 |
| CHEMBL5074003 | — | IC50 | = | 2250.0 | nM | 5.65 |
| CHEMBL5075240 | — | IC50 | = | 2270.0 | nM | 5.64 |
| CHEMBL5090667 | — | IC50 | = | 3370.0 | nM | 5.47 |
| CHEMBL5077404 | — | IC50 | = | 4160.0 | nM | 5.38 |
| CHEMBL5085212 | — | IC50 | = | 5020.0 | nM | 5.30 |
| CHEMBL5090685 | — | IC50 | = | 5730.0 | nM | 5.24 |
| CHEMBL1463660 | — | IC50 | = | 6110.0 | nM | 5.21 |
| CHEMBL5075580 | — | IC50 | = | 7050.0 | nM | 5.15 |
| CHEMBL5086603 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL5078718 | — | IC50 | = | 11520.0 | nM | 4.94 |
| CHEMBL5084672 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5082552 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5088810 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5087539 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5074318 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5090120 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5078897 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5076171 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5088542 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5081224 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5091772 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5077660 | — | IC50 | > | 50000.0 | nM | - |