Assay Detail
Binding
CHEMBL947864
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]CCPA from rat brain cortex adenosine A1 receptor
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 6.74 | 7.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL520830 | — | — | 1 | 7.47 |
| CHEMBL486282 | — | — | 1 | 7.42 |
| CHEMBL520617 | — | — | 1 | 7.41 |
| CHEMBL518972 | — | — | 1 | 7.33 |
| CHEMBL488542 | — | — | 1 | 7.11 |
| CHEMBL486893 | — | — | 1 | 7.10 |
| CHEMBL482855 | — | — | 1 | 7.08 |
| CHEMBL519556 | — | — | 1 | 7.06 |
| CHEMBL486281 | — | — | 1 | 7.04 |
| CHEMBL482638 | — | — | 1 | 7.01 |
| CHEMBL484900 | — | — | 1 | 6.96 |
| CHEMBL483469 | — | — | 1 | 6.75 |
| CHEMBL519813 | — | — | 1 | 6.60 |
| CHEMBL212625 | — | — | 1 | 6.58 |
| CHEMBL483065 | — | — | 1 | 6.57 |
| CHEMBL486688 | — | — | 1 | 6.56 |
| CHEMBL520297 | — | — | 1 | 6.53 |
| CHEMBL482648 | — | — | 1 | 6.45 |
| CHEMBL484899 | — | — | 1 | 6.45 |
| CHEMBL482436 | — | — | 1 | 6.41 |
| CHEMBL486479 | — | — | 1 | 6.33 |
| CHEMBL519390 | — | — | 1 | 6.25 |
| CHEMBL519253 | — | — | 1 | 5.84 |
| CHEMBL483261 | — | — | 1 | 5.56 |
| CHEMBL486478 | — | — | 1 | - |
| CHEMBL483487 | — | — | 1 | - |
| CHEMBL483688 | — | — | 1 | - |
| CHEMBL520899 | — | — | 1 | - |
| CHEMBL486481 | — | — | 1 | - |
| CHEMBL488541 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL520830 | — | Ki | = | 33.8 | nM | 7.47 |
| CHEMBL486282 | — | Ki | = | 38.5 | nM | 7.42 |
| CHEMBL520617 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL518972 | — | Ki | = | 46.7 | nM | 7.33 |
| CHEMBL488542 | — | Ki | = | 77.1 | nM | 7.11 |
| CHEMBL486893 | — | Ki | = | 79.4 | nM | 7.10 |
| CHEMBL482855 | — | Ki | = | 83.8 | nM | 7.08 |
| CHEMBL519556 | — | Ki | = | 86.8 | nM | 7.06 |
| CHEMBL486281 | — | Ki | = | 91.1 | nM | 7.04 |
| CHEMBL482638 | — | Ki | = | 96.7 | nM | 7.01 |
| CHEMBL484900 | — | Ki | = | 111.0 | nM | 6.96 |
| CHEMBL483469 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL519813 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL212625 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL483065 | — | Ki | = | 272.0 | nM | 6.57 |
| CHEMBL486688 | — | Ki | = | 273.0 | nM | 6.56 |
| CHEMBL520297 | — | Ki | = | 296.0 | nM | 6.53 |
| CHEMBL482648 | — | Ki | = | 354.0 | nM | 6.45 |
| CHEMBL484899 | — | Ki | = | 359.0 | nM | 6.45 |
| CHEMBL482436 | — | Ki | = | 386.0 | nM | 6.41 |
| CHEMBL486479 | — | Ki | = | 463.0 | nM | 6.33 |
| CHEMBL519390 | — | Ki | = | 564.0 | nM | 6.25 |
| CHEMBL519253 | — | Ki | = | 1440.0 | nM | 5.84 |
| CHEMBL483261 | — | Ki | = | 2730.0 | nM | 5.56 |
| CHEMBL486478 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL483487 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL483688 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL520899 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL486481 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL488541 | — | Ki | > | 10000.0 | nM | - |