Assay Detail
Functional
CHEMBL873340
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of L701H/T877A mutant androgen receptor of human prostate cancer MDAMB-PCa2b cell proliferation
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MDAMB-PCa2b |
| 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 | 12 | 6.55 | 7.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL366924 | — | — | 1 | 7.02 |
| CHEMBL180859 | — | — | 1 | 6.88 |
| CHEMBL178886 | — | — | 1 | 6.75 |
| CHEMBL182186 | — | — | 1 | 6.75 |
| CHEMBL178957 | — | — | 1 | 6.70 |
| CHEMBL367364 | — | — | 1 | 6.69 |
| CHEMBL181722 | — | — | 1 | 6.63 |
| CHEMBL181674 | — | — | 1 | 6.58 |
| CHEMBL359911 | — | — | 1 | 6.58 |
| CHEMBL178469 | — | — | 1 | 6.39 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.14 |
| CHEMBL369509 | — | — | 1 | 5.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL366924 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL180859 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL178886 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL182186 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL178957 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL367364 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL181722 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL181674 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL359911 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL178469 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 725.0 | nM | 6.14 |
| CHEMBL369509 | — | IC50 | = | 3639.0 | nM | 5.44 |