Assay Detail
Binding
CHEMBL830415
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Inhibition of [3H]DHT binding to androgen receptor of MDA-453 cells
20
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 20 | 6.90 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL181571 | — | — | 1 | 9.00 |
| CHEMBL178333 | — | — | 2 | 8.30 |
| CHEMBL491 | HYDROXYFLUTAMIDE | 2.0 | 1 | 7.37 |
| CHEMBL361222 | — | — | 1 | 7.34 |
| CHEMBL368906 | — | — | 1 | 7.26 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 7.19 |
| CHEMBL182236 | — | — | 1 | 6.90 |
| CHEMBL178886 | — | — | 1 | 6.80 |
| CHEMBL369509 | — | — | 1 | 6.79 |
| CHEMBL180859 | — | — | 1 | 6.75 |
| CHEMBL182186 | — | — | 1 | 6.72 |
| CHEMBL181674 | — | — | 1 | 6.55 |
| CHEMBL359911 | — | — | 1 | 6.55 |
| CHEMBL367364 | — | — | 2 | 6.50 |
| CHEMBL178957 | — | — | 1 | 6.40 |
| CHEMBL366924 | — | — | 1 | 6.40 |
| CHEMBL181722 | — | — | 1 | 6.28 |
| CHEMBL178469 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL181571 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL178333 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL491 | HYDROXYFLUTAMIDE | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL361222 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL368906 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL409 | BICALUTAMIDE | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL178333 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL182236 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL178886 | — | Ki | = | 158.0 | nM | 6.80 |
| CHEMBL369509 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL180859 | — | Ki | = | 177.0 | nM | 6.75 |
| CHEMBL182186 | — | Ki | = | 192.0 | nM | 6.72 |
| CHEMBL181674 | — | Ki | = | 284.0 | nM | 6.55 |
| CHEMBL359911 | — | Ki | = | 284.0 | nM | 6.55 |
| CHEMBL367364 | — | Ki | = | 319.0 | nM | 6.50 |
| CHEMBL178957 | — | Ki | = | 401.0 | nM | 6.40 |
| CHEMBL366924 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL181722 | — | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL178469 | — | Ki | = | 632.0 | nM | 6.20 |
| CHEMBL367364 | — | Ki | = | 1615.0 | nM | 5.79 |