Assay Detail
Functional
CHEMBL649556
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory concentration against human androgen receptor (AR) dependent transcriptional activity in co-transfected mammalian CV-1 cells
33
Total Activities
33
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
Effects of isosteric pyridone replacements in androgen receptor antagonists based on 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6-g]quin olines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 6.67 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL335316 | — | — | 1 | 8.05 |
| CHEMBL133503 | — | — | 1 | 7.66 |
| CHEMBL6874 | — | — | 1 | 7.57 |
| CHEMBL133331 | — | — | 1 | 7.52 |
| CHEMBL133792 | — | — | 1 | 7.52 |
| CHEMBL132803 | — | — | 1 | 7.51 |
| CHEMBL491 | HYDROXYFLUTAMIDE | 2.0 | 1 | 7.37 |
| CHEMBL132427 | — | — | 1 | 7.35 |
| CHEMBL134209 | — | — | 1 | 7.20 |
| CHEMBL133167 | — | — | 1 | 7.14 |
| CHEMBL134140 | — | — | 1 | 7.14 |
| CHEMBL133465 | — | — | 1 | 6.76 |
| CHEMBL338922 | — | — | 1 | 6.67 |
| CHEMBL133054 | — | — | 1 | 6.61 |
| CHEMBL133289 | — | — | 1 | 6.60 |
| CHEMBL132295 | — | — | 1 | 6.47 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.47 |
| CHEMBL132516 | — | — | 1 | 6.47 |
| CHEMBL132205 | — | — | 1 | 6.33 |
| CHEMBL132635 | — | — | 1 | 6.32 |
| CHEMBL134180 | — | — | 1 | 6.30 |
| CHEMBL134303 | — | — | 1 | 6.20 |
| CHEMBL131963 | — | — | 1 | 6.17 |
| CHEMBL132609 | — | — | 1 | 6.14 |
| CHEMBL134242 | — | — | 1 | 6.12 |
| CHEMBL134056 | — | — | 1 | 6.11 |
| CHEMBL132354 | — | — | 1 | 6.05 |
| CHEMBL133329 | — | — | 1 | 5.94 |
| CHEMBL133825 | — | — | 1 | 5.84 |
| CHEMBL133715 | — | — | 1 | 5.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL335316 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL133503 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL6874 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL133331 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL133792 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL132803 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL491 | HYDROXYFLUTAMIDE | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL132427 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL134209 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL133167 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL134140 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL133465 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL338922 | — | IC50 | = | 212.0 | nM | 6.67 |
| CHEMBL133054 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL133289 | — | IC50 | = | 251.0 | nM | 6.60 |
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 338.0 | nM | 6.47 |
| CHEMBL132516 | — | IC50 | = | 336.0 | nM | 6.47 |
| CHEMBL132295 | — | IC50 | = | 335.0 | nM | 6.47 |
| CHEMBL132205 | — | IC50 | = | 467.0 | nM | 6.33 |
| CHEMBL132635 | — | IC50 | = | 479.0 | nM | 6.32 |
| CHEMBL134180 | — | IC50 | = | 503.0 | nM | 6.30 |
| CHEMBL134303 | — | IC50 | = | 636.0 | nM | 6.20 |
| CHEMBL131963 | — | IC50 | = | 675.0 | nM | 6.17 |
| CHEMBL132609 | — | IC50 | = | 725.0 | nM | 6.14 |
| CHEMBL134242 | — | IC50 | = | 751.0 | nM | 6.12 |
| CHEMBL134056 | — | IC50 | = | 785.0 | nM | 6.11 |
| CHEMBL132354 | — | IC50 | = | 889.0 | nM | 6.05 |
| CHEMBL133329 | — | IC50 | = | 1159.0 | nM | 5.94 |
| CHEMBL133825 | — | IC50 | = | 1448.0 | nM | 5.84 |
| CHEMBL133715 | — | IC50 | = | 1866.0 | nM | 5.73 |
| CHEMBL134117 | — | IC50 | = | 3217.0 | nM | 5.49 |
| CHEMBL132131 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL335948 | — | IC50 | > | 10000.0 | nM | - |