Assay Detail
Functional
CHEMBL837993
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of T877A androgen receptor of human prostate cancer cells in reporter gene assay
13
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Cancer cell lines |
| 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 | 13 | 7.28 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL367364 | — | — | 2 | 8.15 |
| CHEMBL366924 | — | — | 1 | 8.00 |
| CHEMBL182186 | — | — | 1 | 7.52 |
| CHEMBL180859 | — | — | 1 | 7.48 |
| CHEMBL178469 | — | — | 1 | 7.46 |
| CHEMBL178886 | — | — | 1 | 7.39 |
| CHEMBL181722 | — | — | 1 | 7.28 |
| CHEMBL178957 | — | — | 1 | 7.14 |
| CHEMBL181674 | — | — | 1 | 7.08 |
| CHEMBL359911 | — | — | 1 | 7.08 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.40 |
| CHEMBL369509 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL367364 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL366924 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL367364 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL182186 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL180859 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL178469 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL178886 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL181722 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL178957 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL181674 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL359911 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL369509 | — | IC50 | = | 1790.0 | nM | 5.75 |