Assay Detail
Binding
CHEMBL896728
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DHT from human androgen receptor in MDA453 cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDA453 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis and SAR of tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues as highly potent selective androgen receptor modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 8.07 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1170 | TESTOSTERONE PROPIONATE | 4.0 | 1 | 9.60 |
| CHEMBL233773 | — | — | 1 | 9.35 |
| CHEMBL229264 | — | — | 1 | 8.68 |
| CHEMBL425646 | — | — | 1 | 8.49 |
| CHEMBL391768 | — | — | 1 | 8.09 |
| CHEMBL234185 | — | — | 1 | 7.85 |
| CHEMBL391770 | — | — | 1 | 7.70 |
| CHEMBL233774 | — | — | 1 | 7.54 |
| CHEMBL234394 | — | — | 1 | 7.44 |
| CHEMBL391769 | — | — | 1 | 7.36 |
| CHEMBL233977 | — | — | 1 | 6.72 |
| CHEMBL393048 | — | — | 1 | - |
| CHEMBL234187 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1170 | TESTOSTERONE PROPIONATE | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL233773 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL229264 | — | Ki | = | 2.11 | nM | 8.68 |
| CHEMBL425646 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL391768 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL234185 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL391770 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL233774 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL234394 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL391769 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL233977 | — | Ki | = | 189.0 | nM | 6.72 |
| CHEMBL393048 | — | Ki | - | — | - | |
| CHEMBL234187 | — | Ki | - | — | - |