Assay Detail
Functional
CHEMBL768810
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonistic activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells.
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | CV-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 |
|---|---|---|---|
| IC50 | 37 | 6.19 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1276308 | MIFEPRISTONE | 4.0 | 1 | 9.74 |
| CHEMBL160451 | — | — | 1 | 7.31 |
| CHEMBL346487 | — | — | 1 | 6.96 |
| CHEMBL345342 | — | — | 1 | 6.87 |
| CHEMBL156142 | — | — | 1 | 6.64 |
| CHEMBL160386 | — | — | 1 | 6.63 |
| CHEMBL156982 | — | — | 1 | 6.56 |
| CHEMBL156641 | — | — | 1 | 6.51 |
| CHEMBL6874 | — | — | 1 | 6.48 |
| CHEMBL160665 | — | — | 1 | 6.46 |
| CHEMBL157344 | — | — | 1 | 6.44 |
| CHEMBL350877 | — | — | 1 | 6.41 |
| CHEMBL349539 | — | — | 1 | 6.41 |
| CHEMBL157407 | — | — | 1 | 6.40 |
| CHEMBL351148 | — | — | 1 | 6.26 |
| CHEMBL156278 | — | — | 1 | 6.23 |
| CHEMBL160257 | — | — | 1 | 6.13 |
| CHEMBL156806 | — | — | 1 | 6.06 |
| CHEMBL160230 | — | — | 1 | 5.96 |
| CHEMBL160713 | — | — | 1 | 5.94 |
| CHEMBL346827 | — | — | 1 | 5.91 |
| CHEMBL347870 | — | — | 1 | 5.78 |
| CHEMBL160239 | — | — | 1 | 5.75 |
| CHEMBL345854 | — | — | 1 | 5.74 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 5.74 |
| CHEMBL491 | HYDROXYFLUTAMIDE | 2.0 | 1 | 5.70 |
| CHEMBL435651 | — | — | 1 | 5.66 |
| CHEMBL350465 | — | — | 1 | 5.63 |
| CHEMBL160250 | — | — | 1 | 5.57 |
| CHEMBL352002 | — | — | 1 | 5.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1276308 | MIFEPRISTONE | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL160451 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL346487 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL345342 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL156142 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL160386 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL156982 | — | IC50 | = | 274.0 | nM | 6.56 |
| CHEMBL156641 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL6874 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL160665 | — | IC50 | = | 348.0 | nM | 6.46 |
| CHEMBL157344 | — | IC50 | = | 362.0 | nM | 6.44 |
| CHEMBL350877 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL349539 | — | IC50 | = | 393.0 | nM | 6.41 |
| CHEMBL157407 | — | IC50 | = | 398.0 | nM | 6.40 |
| CHEMBL351148 | — | IC50 | = | 543.0 | nM | 6.26 |
| CHEMBL156278 | — | IC50 | = | 585.0 | nM | 6.23 |
| CHEMBL160257 | — | IC50 | = | 735.0 | nM | 6.13 |
| CHEMBL156806 | — | IC50 | = | 876.0 | nM | 6.06 |
| CHEMBL160230 | — | IC50 | = | 1105.0 | nM | 5.96 |
| CHEMBL160713 | — | IC50 | = | 1144.0 | nM | 5.94 |
| CHEMBL346827 | — | IC50 | = | 1239.0 | nM | 5.91 |
| CHEMBL347870 | — | IC50 | = | 1678.0 | nM | 5.78 |
| CHEMBL160239 | — | IC50 | = | 1763.0 | nM | 5.75 |
| CHEMBL345854 | — | IC50 | = | 1828.0 | nM | 5.74 |
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 1819.0 | nM | 5.74 |
| CHEMBL491 | HYDROXYFLUTAMIDE | IC50 | = | 2013.0 | nM | 5.70 |
| CHEMBL435651 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL350465 | — | IC50 | = | 2334.0 | nM | 5.63 |
| CHEMBL160250 | — | IC50 | = | 2708.0 | nM | 5.57 |
| CHEMBL352002 | — | IC50 | = | 2931.0 | nM | 5.53 |
| CHEMBL156751 | — | IC50 | = | 3162.0 | nM | 5.50 |
| CHEMBL422707 | — | IC50 | = | 3277.0 | nM | 5.49 |
| CHEMBL157703 | — | IC50 | = | 3346.0 | nM | 5.47 |
| CHEMBL347910 | — | IC50 | = | 3726.0 | nM | 5.43 |
| CHEMBL160923 | — | IC50 | = | 4395.0 | nM | 5.36 |
| CHEMBL139835 | CYPROTERONE ACETATE | IC50 | > | 1000.0 | nM | - |
| CHEMBL156312 | — | IC50 | > | 10000.0 | nM | - |