Assay Detail
Binding
CHEMBL645215
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Ex vivo inhibition of guinea pig ileum twitch via Adenosine A1 receptor.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
The discovery and synthesis of highly potent, A2a receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.10 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL464859 | NECA | — | 1 | 9.00 |
| CHEMBL284969 | — | — | 1 | 9.00 |
| CHEMBL131280 | — | — | 1 | 8.70 |
| CHEMBL340674 | — | — | 1 | 7.10 |
| CHEMBL131535 | — | — | 1 | 7.08 |
| CHEMBL131242 | — | — | 1 | 6.58 |
| CHEMBL130830 | — | — | 1 | 6.58 |
| CHEMBL337080 | — | — | 1 | 6.43 |
| CHEMBL131457 | — | — | 1 | 6.41 |
| CHEMBL128176 | — | — | 1 | 6.26 |
| CHEMBL336608 | — | — | 1 | 6.17 |
| CHEMBL334336 | — | — | 1 | 5.83 |
| CHEMBL435188 | — | — | 1 | - |
| CHEMBL339522 | — | — | 1 | - |
| CHEMBL131175 | — | — | 1 | - |
| CHEMBL341031 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL464859 | NECA | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL284969 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL131280 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL340674 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL131535 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL131242 | — | Ki | = | 263.0 | nM | 6.58 |
| CHEMBL130830 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL337080 | — | Ki | = | 369.0 | nM | 6.43 |
| CHEMBL131457 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL128176 | — | Ki | = | 549.0 | nM | 6.26 |
| CHEMBL336608 | — | Ki | = | 672.0 | nM | 6.17 |
| CHEMBL334336 | — | Ki | = | 1470.0 | nM | 5.83 |
| CHEMBL435188 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL339522 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL131175 | — | Ki | > | 612.0 | nM | - |
| CHEMBL341031 | — | Ki | - | nM | - |