Assay Detail
Binding
CHEMBL3626368
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at wild type AR expressed in human SC cells assessed as inhibition of 1 nM DHT-induced cell proliferation after 3 days by WST-8 assay
30
Total Activities
30
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
Design and synthesis of 4-benzyl-1-(2H)-phthalazinone derivatives as novel androgen receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 5.74 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL491 | HYDROXYFLUTAMIDE | 2.0 | 1 | 6.75 |
| CHEMBL3622589 | — | — | 1 | 6.75 |
| CHEMBL3622579 | — | — | 1 | 6.66 |
| CHEMBL3622578 | — | — | 1 | 6.28 |
| CHEMBL3622590 | — | — | 1 | 6.04 |
| CHEMBL3622581 | — | — | 1 | 6.00 |
| CHEMBL378274 | — | — | 1 | 5.90 |
| CHEMBL3622587 | — | — | 1 | 5.86 |
| CHEMBL3622583 | — | — | 1 | 5.78 |
| CHEMBL3622585 | — | — | 1 | 5.71 |
| CHEMBL3622576 | — | — | 1 | 5.43 |
| CHEMBL3622584 | — | — | 1 | 5.43 |
| CHEMBL3622588 | — | — | 1 | 5.42 |
| CHEMBL66761 | — | — | 1 | 5.27 |
| CHEMBL3622586 | — | — | 1 | 5.04 |
| CHEMBL3622574 | — | — | 1 | 5.02 |
| CHEMBL3622573 | — | — | 1 | 5.02 |
| CHEMBL3622575 | — | — | 1 | 4.98 |
| CHEMBL3622570 | — | — | 1 | - |
| CHEMBL3622580 | — | — | 1 | - |
| CHEMBL3622569 | — | — | 1 | - |
| CHEMBL3622582 | — | — | 1 | - |
| CHEMBL3622568 | — | — | 1 | - |
| CHEMBL3622567 | — | — | 1 | - |
| CHEMBL3622566 | — | — | 1 | - |
| CHEMBL3622571 | — | — | 1 | - |
| CHEMBL3622565 | — | — | 1 | - |
| CHEMBL3622577 | — | — | 1 | - |
| CHEMBL1353965 | — | — | 1 | - |
| CHEMBL3622572 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL491 | HYDROXYFLUTAMIDE | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3622589 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3622579 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3622578 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL3622590 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL3622581 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL378274 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL3622587 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL3622583 | — | IC50 | = | 1660.0 | nM | 5.78 |
| CHEMBL3622585 | — | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL3622576 | — | IC50 | = | 3670.0 | nM | 5.43 |
| CHEMBL3622584 | — | IC50 | = | 3710.0 | nM | 5.43 |
| CHEMBL3622588 | — | IC50 | = | 3760.0 | nM | 5.42 |
| CHEMBL66761 | — | IC50 | = | 5370.0 | nM | 5.27 |
| CHEMBL3622586 | — | IC50 | = | 9020.0 | nM | 5.04 |
| CHEMBL3622574 | — | IC50 | = | 9590.0 | nM | 5.02 |
| CHEMBL3622573 | — | IC50 | = | 9540.0 | nM | 5.02 |
| CHEMBL3622575 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL3622570 | — | IC50 | - | — | - | |
| CHEMBL3622580 | — | IC50 | - | — | - | |
| CHEMBL3622569 | — | IC50 | - | — | - | |
| CHEMBL3622582 | — | IC50 | - | — | - | |
| CHEMBL3622568 | — | IC50 | - | — | - | |
| CHEMBL3622567 | — | IC50 | - | — | - | |
| CHEMBL3622566 | — | IC50 | - | — | - | |
| CHEMBL3622571 | — | IC50 | - | — | - | |
| CHEMBL3622565 | — | IC50 | - | — | - | |
| CHEMBL3622577 | — | IC50 | - | — | - | |
| CHEMBL1353965 | — | IC50 | - | — | - | |
| CHEMBL3622572 | — | IC50 | - | — | - |