Assay Detail
Binding
CHEMBL2072277
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Displacement of 3[H]R-PIA from rat A1 adenosine receptor expressed in CHO cells after 60 min by Liquid scintillation analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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 | 7 | 6.76 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL261482 | — | — | 1 | 8.19 |
| CHEMBL2070507 | — | — | 1 | 7.37 |
| CHEMBL464859 | NECA | — | 1 | 7.20 |
| CHEMBL2070399 | — | — | 1 | 6.61 |
| CHEMBL2070508 | — | — | 1 | 6.11 |
| CHEMBL2070398 | — | — | 1 | 5.92 |
| CHEMBL1235128 | — | — | 1 | 5.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL261482 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL2070507 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL464859 | NECA | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL2070399 | — | Ki | = | 248.0 | nM | 6.61 |
| CHEMBL2070508 | — | Ki | = | 770.0 | nM | 6.11 |
| CHEMBL2070398 | — | Ki | = | 1190.0 | nM | 5.92 |
| CHEMBL1235128 | — | Ki | = | 1240.0 | nM | 5.91 |