Assay Detail
Binding
CHEMBL828881
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Inhibition of [3H]-DHT binding to T877A androgen receptor of LNCaP cells
20
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | LNCaP |
| 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 | 8.32 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL181571 | — | — | 1 | 9.30 |
| CHEMBL361222 | — | — | 1 | 9.22 |
| CHEMBL178333 | — | — | 2 | 8.70 |
| CHEMBL180859 | — | — | 1 | 8.70 |
| CHEMBL491 | HYDROXYFLUTAMIDE | 2.0 | 1 | 8.70 |
| CHEMBL367364 | — | — | 2 | 8.70 |
| CHEMBL366924 | — | — | 1 | 8.47 |
| CHEMBL182236 | — | — | 1 | 8.44 |
| CHEMBL368906 | — | — | 1 | 8.30 |
| CHEMBL178886 | — | — | 1 | 8.22 |
| CHEMBL178469 | — | — | 1 | 8.15 |
| CHEMBL181674 | — | — | 1 | 7.96 |
| CHEMBL359911 | — | — | 1 | 7.96 |
| CHEMBL182186 | — | — | 1 | 7.92 |
| CHEMBL181722 | — | — | 1 | 7.89 |
| CHEMBL178957 | — | — | 1 | 7.62 |
| CHEMBL369509 | — | — | 1 | 7.50 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 7.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL181571 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL361222 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL367364 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL178333 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL178333 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL180859 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL491 | HYDROXYFLUTAMIDE | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL366924 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL367364 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL182236 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL368906 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL178886 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL178469 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL181674 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL359911 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL182186 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL181722 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL178957 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL369509 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL409 | BICALUTAMIDE | Ki | = | 35.0 | nM | 7.46 |