Assay Detail
Binding
CHEMBL872368
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity for human androgen receptor transfected into mammalian COS-1 cells
33
Total Activities
33
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
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 |
|---|---|---|---|
| Ki | 33 | 7.15 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL338922 | — | — | 1 | 8.30 |
| CHEMBL133503 | — | — | 1 | 7.96 |
| CHEMBL134209 | — | — | 1 | 7.70 |
| CHEMBL335316 | — | — | 1 | 7.66 |
| CHEMBL6874 | — | — | 1 | 7.58 |
| CHEMBL491 | HYDROXYFLUTAMIDE | 2.0 | 1 | 7.47 |
| CHEMBL132803 | — | — | 1 | 7.24 |
| CHEMBL133792 | — | — | 1 | 7.08 |
| CHEMBL132427 | — | — | 1 | 7.07 |
| CHEMBL133465 | — | — | 1 | 7.02 |
| CHEMBL132295 | — | — | 1 | 7.02 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.93 |
| CHEMBL134140 | — | — | 1 | 6.80 |
| CHEMBL133289 | — | — | 1 | 6.53 |
| CHEMBL133331 | — | — | 1 | 6.50 |
| CHEMBL133167 | — | — | 1 | 6.37 |
| CHEMBL134180 | — | — | 1 | 6.24 |
| CHEMBL133825 | — | — | 1 | - |
| CHEMBL132635 | — | — | 1 | - |
| CHEMBL132609 | — | — | 1 | - |
| CHEMBL132205 | — | — | 1 | - |
| CHEMBL132354 | — | — | 1 | - |
| CHEMBL131963 | — | — | 1 | - |
| CHEMBL134117 | — | — | 1 | - |
| CHEMBL132131 | — | — | 1 | - |
| CHEMBL134242 | — | — | 1 | - |
| CHEMBL134056 | — | — | 1 | - |
| CHEMBL335948 | — | — | 1 | - |
| CHEMBL134303 | — | — | 1 | - |
| CHEMBL133329 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL338922 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL133503 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL134209 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL335316 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL6874 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL491 | HYDROXYFLUTAMIDE | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL132803 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL133792 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL132427 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL133465 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL132295 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL409 | BICALUTAMIDE | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL134140 | — | Ki | = | 159.0 | nM | 6.80 |
| CHEMBL133289 | — | Ki | = | 294.0 | nM | 6.53 |
| CHEMBL133331 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL133167 | — | Ki | = | 426.0 | nM | 6.37 |
| CHEMBL134180 | — | Ki | = | 572.0 | nM | 6.24 |
| CHEMBL133825 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL132635 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL132609 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL132205 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL132354 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL131963 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL134117 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL132131 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL134242 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL134056 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL335948 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL134303 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL133329 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL133054 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL132516 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL133715 | — | Ki | > | 1000.0 | nM | - |