Assay Detail
Binding
CHEMBL651953
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Binding affinity for human androgen receptor in transiently-transfected COS-1 cells.
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | COS-1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 37 | 7.07 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL345854 | — | — | 1 | 8.05 |
| CHEMBL160230 | — | — | 1 | 8.00 |
| CHEMBL139835 | CYPROTERONE ACETATE | 3.0 | 1 | 7.85 |
| CHEMBL435651 | — | — | 1 | 7.77 |
| CHEMBL1276308 | MIFEPRISTONE | 4.0 | 1 | 7.66 |
| CHEMBL6874 | — | — | 1 | 7.58 |
| CHEMBL491 | HYDROXYFLUTAMIDE | 2.0 | 1 | 7.57 |
| CHEMBL351148 | — | — | 1 | 7.54 |
| CHEMBL345342 | — | — | 1 | 7.41 |
| CHEMBL352002 | — | — | 1 | 7.40 |
| CHEMBL156278 | — | — | 1 | 7.34 |
| CHEMBL156982 | — | — | 1 | 7.27 |
| CHEMBL346827 | — | — | 1 | 7.25 |
| CHEMBL346487 | — | — | 1 | 7.21 |
| CHEMBL422707 | — | — | 1 | 7.16 |
| CHEMBL160713 | — | — | 1 | 7.16 |
| CHEMBL160665 | — | — | 1 | 7.14 |
| CHEMBL156142 | — | — | 1 | 7.12 |
| CHEMBL157407 | — | — | 1 | 7.11 |
| CHEMBL160386 | — | — | 1 | 7.09 |
| CHEMBL157703 | — | — | 1 | 7.09 |
| CHEMBL347910 | — | — | 1 | 7.07 |
| CHEMBL350877 | — | — | 1 | 7.07 |
| CHEMBL160250 | — | — | 1 | 6.99 |
| CHEMBL160451 | — | — | 1 | 6.94 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.93 |
| CHEMBL160257 | — | — | 1 | 6.82 |
| CHEMBL156312 | — | — | 1 | 6.77 |
| CHEMBL156806 | — | — | 1 | 6.72 |
| CHEMBL350465 | — | — | 1 | 6.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL345854 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL160230 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL139835 | CYPROTERONE ACETATE | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL435651 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL1276308 | MIFEPRISTONE | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL6874 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL491 | HYDROXYFLUTAMIDE | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL351148 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL345342 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL352002 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL156278 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL156982 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL346827 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL346487 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL160713 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL422707 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL160665 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL156142 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL157407 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL157703 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL160386 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL347910 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL350877 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL160250 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL160451 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL409 | BICALUTAMIDE | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL160257 | — | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL156312 | — | Ki | = | 169.0 | nM | 6.77 |
| CHEMBL156806 | — | Ki | = | 189.0 | nM | 6.72 |
| CHEMBL350465 | — | Ki | = | 251.0 | nM | 6.60 |
| CHEMBL349539 | — | Ki | = | 268.0 | nM | 6.57 |
| CHEMBL157344 | — | Ki | = | 358.0 | nM | 6.45 |
| CHEMBL156641 | — | Ki | = | 456.0 | nM | 6.34 |
| CHEMBL156751 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL160239 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL347870 | — | Ki | = | 695.0 | nM | 6.16 |
| CHEMBL160923 | — | Ki | = | 874.0 | nM | 6.06 |