Assay Detail
Functional
CHEMBL863517
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of AR mediated transcriptional activation using reporter assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.37 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL197595 | — | — | 1 | 6.96 |
| CHEMBL439685 | — | — | 1 | 6.92 |
| CHEMBL201242 | — | — | 1 | 6.89 |
| CHEMBL199899 | — | — | 1 | 6.85 |
| CHEMBL381253 | — | — | 1 | 6.77 |
| CHEMBL201077 | — | — | 1 | 6.72 |
| CHEMBL200973 | — | — | 1 | 6.70 |
| CHEMBL202990 | — | — | 1 | 6.70 |
| CHEMBL202660 | — | — | 1 | 6.68 |
| CHEMBL201069 | — | — | 1 | 6.66 |
| CHEMBL381776 | — | — | 1 | 6.60 |
| CHEMBL201757 | — | — | 1 | 6.48 |
| CHEMBL379465 | — | — | 1 | 6.43 |
| CHEMBL381558 | — | — | 1 | 6.36 |
| CHEMBL201327 | — | — | 1 | 6.33 |
| CHEMBL381358 | — | — | 1 | 6.30 |
| CHEMBL199284 | — | — | 1 | 6.17 |
| CHEMBL202710 | — | — | 1 | 6.14 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.05 |
| CHEMBL203423 | — | — | 1 | 6.00 |
| CHEMBL197648 | — | — | 1 | 5.92 |
| CHEMBL372390 | — | — | 1 | 5.89 |
| CHEMBL203085 | — | — | 1 | 5.34 |
| CHEMBL201167 | — | — | 1 | 5.11 |
| CHEMBL201126 | — | — | 1 | - |
| CHEMBL265785 | — | — | 1 | - |
| CHEMBL382426 | — | — | 1 | - |
| CHEMBL201488 | — | — | 1 | - |
| CHEMBL201314 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL197595 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL439685 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL201242 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL199899 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL381253 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL201077 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL200973 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL202990 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL202660 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL201069 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL381776 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL201757 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL379465 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL381558 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL201327 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL381358 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL199284 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL202710 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL203423 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL197648 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL372390 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL203085 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL201167 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL201126 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL265785 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL382426 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL201488 | — | IC50 | - | — | - | |
| CHEMBL201314 | — | IC50 | - | — | - |