Assay Detail
Binding
CHEMBL916638
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Displacement of [3H]DHT from human AR expressed in MDA-MB-453 cells
34
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDA-MB-453 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 7.87 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27769 | STANOLONE | 2.0 | 1 | 9.52 |
| CHEMBL224204 | — | — | 1 | 8.92 |
| CHEMBL227784 | — | — | 1 | 8.80 |
| CHEMBL226558 | — | — | 1 | 8.55 |
| CHEMBL227394 | — | — | 1 | 8.40 |
| CHEMBL227783 | — | — | 1 | 8.40 |
| CHEMBL227305 | — | — | 1 | 8.38 |
| CHEMBL224207 | — | — | 1 | 8.25 |
| CHEMBL227088 | — | — | 1 | 8.24 |
| CHEMBL1445 | FLUOXYMESTERONE | 4.0 | 1 | 8.24 |
| CHEMBL224263 | — | — | 1 | 8.15 |
| CHEMBL227440 | — | — | 1 | 8.11 |
| CHEMBL388997 | — | — | 1 | 8.03 |
| CHEMBL227590 | — | — | 1 | 8.02 |
| CHEMBL390728 | — | — | 1 | 7.96 |
| CHEMBL227408 | — | — | 3 | 7.82 |
| CHEMBL227030 | — | — | 1 | 7.82 |
| CHEMBL226609 | — | — | 1 | 7.80 |
| CHEMBL227645 | — | — | 1 | 7.77 |
| CHEMBL390746 | — | — | 1 | 7.72 |
| CHEMBL389481 | — | — | 1 | 7.64 |
| CHEMBL227749 | — | — | 1 | 7.57 |
| CHEMBL376360 | — | — | 1 | 7.52 |
| CHEMBL268589 | — | — | 1 | 7.48 |
| CHEMBL388831 | — | — | 1 | 7.47 |
| CHEMBL375907 | — | — | 1 | 7.32 |
| CHEMBL226559 | — | — | 1 | 7.29 |
| CHEMBL227463 | — | — | 1 | 7.24 |
| CHEMBL227695 | — | — | 1 | 6.96 |
| CHEMBL227033 | — | — | 1 | 6.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27769 | STANOLONE | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL224204 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL227784 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL226558 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL227783 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL227394 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL227305 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL224207 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL1445 | FLUOXYMESTERONE | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL227088 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL224263 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL227440 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL388997 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL227590 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL390728 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL227030 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL227408 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL226609 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL227645 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL390746 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL389481 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL227408 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL227749 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL376360 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL268589 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL388831 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL375907 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL226559 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL227463 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL227408 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL227695 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL227033 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL390577 | — | Ki | = | 206.0 | nM | 6.69 |
| CHEMBL390754 | — | Ki | > | 1000.0 | nM | - |