Assay Detail
Functional
CHEMBL837992
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human androgen receptor of breast carcinoma MDA-453 cells in reporter gene assay
20
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MDA-453 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.52 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL178333 | — | — | 2 | 7.92 |
| CHEMBL491 | HYDROXYFLUTAMIDE | 2.0 | 1 | 7.58 |
| CHEMBL368906 | — | — | 1 | 6.92 |
| CHEMBL367364 | — | — | 2 | 6.90 |
| CHEMBL361222 | — | — | 1 | 6.84 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.76 |
| CHEMBL182236 | — | — | 1 | 6.66 |
| CHEMBL178886 | — | — | 1 | 6.51 |
| CHEMBL369509 | — | — | 1 | 6.38 |
| CHEMBL180859 | — | — | 1 | 6.29 |
| CHEMBL182186 | — | — | 1 | 6.18 |
| CHEMBL178469 | — | — | 1 | 6.13 |
| CHEMBL181722 | — | — | 1 | 5.98 |
| CHEMBL181674 | — | — | 1 | 5.92 |
| CHEMBL359911 | — | — | 1 | 5.92 |
| CHEMBL178957 | — | — | 1 | 5.76 |
| CHEMBL366924 | — | — | 1 | 5.70 |
| CHEMBL181571 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL178333 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL491 | HYDROXYFLUTAMIDE | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL178333 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL368906 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL367364 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL361222 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL182236 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL178886 | — | IC50 | = | 307.0 | nM | 6.51 |
| CHEMBL367364 | — | IC50 | = | 317.0 | nM | 6.50 |
| CHEMBL369509 | — | IC50 | = | 418.0 | nM | 6.38 |
| CHEMBL180859 | — | IC50 | = | 517.0 | nM | 6.29 |
| CHEMBL182186 | — | IC50 | = | 664.0 | nM | 6.18 |
| CHEMBL178469 | — | IC50 | = | 744.0 | nM | 6.13 |
| CHEMBL181722 | — | IC50 | = | 1038.0 | nM | 5.98 |
| CHEMBL181674 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL359911 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL178957 | — | IC50 | = | 1746.0 | nM | 5.76 |
| CHEMBL366924 | — | IC50 | = | 2014.0 | nM | 5.70 |
| CHEMBL181571 | — | IC50 | > | 5.0 | nM | - |