Assay Detail
Functional
CHEMBL916637
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human androgen receptor expressed in CV1 cells by transcriptional activation assay
38
Total Activities
17
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CV-1 |
| 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 |
|---|---|---|---|
| Efficacy | 19 | - | - |
| IC50 | 16 | 6.78 | 7.17 |
| EC50 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL227463 | — | — | 2 | 7.17 |
| CHEMBL390577 | — | — | 2 | 6.65 |
| CHEMBL390754 | — | — | 2 | 6.53 |
| CHEMBL227408 | — | — | 6 | - |
| CHEMBL376360 | — | — | 2 | - |
| CHEMBL388831 | — | — | 2 | - |
| CHEMBL227784 | — | — | 2 | - |
| CHEMBL227783 | — | — | 2 | - |
| CHEMBL375907 | — | — | 2 | - |
| CHEMBL227590 | — | — | 2 | - |
| CHEMBL27769 | STANOLONE | 2.0 | 2 | - |
| CHEMBL227030 | — | — | 2 | - |
| CHEMBL390728 | — | — | 2 | - |
| CHEMBL1445 | FLUOXYMESTERONE | 4.0 | 2 | - |
| CHEMBL268589 | — | — | 2 | - |
| CHEMBL227645 | — | — | 2 | - |
| CHEMBL224204 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL227463 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL390577 | — | IC50 | = | 224.0 | nM | 6.65 |
| CHEMBL390754 | — | IC50 | = | 296.0 | nM | 6.53 |
| CHEMBL227408 | — | Efficacy | < | 20.0 | % | - |
| CHEMBL224204 | — | Efficacy | < | 20.0 | % | - |
| CHEMBL227408 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL376360 | — | Efficacy | < | 20.0 | % | - |
| CHEMBL376360 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL388831 | — | Efficacy | < | 20.0 | % | - |
| CHEMBL388831 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL227408 | — | Efficacy | < | 20.0 | % | - |
| CHEMBL227408 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL27769 | STANOLONE | Efficacy | < | 20.0 | % | - |
| CHEMBL227784 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL227783 | — | Efficacy | < | 20.0 | % | - |
| CHEMBL227783 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL375907 | — | Efficacy | < | 20.0 | % | - |
| CHEMBL375907 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL227590 | — | Efficacy | < | 20.0 | % | - |
| CHEMBL227590 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL227408 | — | Efficacy | = | 29.0 | % | - |
| CHEMBL227030 | — | Efficacy | < | 20.0 | % | - |
| CHEMBL224204 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL227030 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL390728 | — | Efficacy | < | 20.0 | % | - |
| CHEMBL390728 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1445 | FLUOXYMESTERONE | Efficacy | < | 20.0 | % | - |
| CHEMBL1445 | FLUOXYMESTERONE | IC50 | > | 10000.0 | nM | - |
| CHEMBL390754 | — | Efficacy | = | 72.0 | % | - |
| CHEMBL27769 | STANOLONE | IC50 | > | 10000.0 | nM | - |
| CHEMBL227408 | — | EC50 | - | — | - | |
| CHEMBL227463 | — | Efficacy | = | 32.0 | % | - |
| CHEMBL268589 | — | Efficacy | = | 21.0 | % | - |
| CHEMBL268589 | — | EC50 | - | — | - | |
| CHEMBL390577 | — | Efficacy | = | 90.0 | % | - |
| CHEMBL227645 | — | Efficacy | = | 27.0 | % | - |
| CHEMBL227645 | — | EC50 | - | — | - | |
| CHEMBL227784 | — | Efficacy | < | 20.0 | % | - |