Assay Detail
Binding
CHEMBL2072274
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Displacement of 3[H]R-PIA from human A1 adenosine receptor expressed in CHO cells after 60 mins by Liquid scintillation analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimization of adenosine 5'-carboxamide derivatives as adenosine receptor agonists using structure-based ligand design and fragment screening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 8.10 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL261482 | — | — | 1 | 8.72 |
| CHEMBL464859 | NECA | — | 1 | 8.52 |
| CHEMBL2070507 | — | — | 1 | 8.26 |
| CHEMBL1235128 | — | — | 1 | 7.92 |
| CHEMBL1234591 | — | — | 1 | 7.89 |
| CHEMBL2070398 | — | — | 1 | 7.82 |
| CHEMBL2070508 | — | — | 1 | 7.57 |
| CHEMBL2070506 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL261482 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL464859 | NECA | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL2070507 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL1235128 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1234591 | — | Ki | = | 12.8 | nM | 7.89 |
| CHEMBL2070398 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2070508 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL2070506 | — | Ki | > | 10000.0 | nM | - |