Assay Detail
Binding
CHEMBL1015331
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Displacement of [3H]HEMADO from human recombinant adenosine A3 receptor expressed in CHO cells
19
Total Activities
19
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
N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine receptor with antinociceptive effects in mice.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 5.89 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL489640 | — | — | 1 | 7.00 |
| CHEMBL490250 | — | — | 1 | 6.89 |
| CHEMBL477666 | — | — | 1 | 6.53 |
| CHEMBL477444 | — | — | 1 | 6.42 |
| CHEMBL477445 | — | — | 1 | 6.38 |
| CHEMBL477667 | — | — | 1 | 6.32 |
| CHEMBL489638 | — | — | 1 | 6.13 |
| CHEMBL489226 | — | — | 1 | 5.94 |
| CHEMBL449575 | — | — | 1 | 5.89 |
| CHEMBL514541 | — | — | 1 | 5.85 |
| CHEMBL523934 | — | — | 1 | 5.84 |
| CHEMBL522095 | — | — | 1 | 5.60 |
| CHEMBL478071 | — | — | 1 | 5.52 |
| CHEMBL489428 | — | — | 1 | 5.46 |
| CHEMBL489628 | — | — | 1 | 5.36 |
| CHEMBL489639 | — | — | 1 | 5.35 |
| CHEMBL514701 | — | — | 1 | 5.23 |
| CHEMBL515330 | — | — | 1 | 5.17 |
| CHEMBL477665 | — | — | 1 | 4.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL489640 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL490250 | — | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL477666 | — | Ki | = | 296.0 | nM | 6.53 |
| CHEMBL477444 | — | Ki | = | 376.0 | nM | 6.42 |
| CHEMBL477445 | — | Ki | = | 417.0 | nM | 6.38 |
| CHEMBL477667 | — | Ki | = | 479.0 | nM | 6.32 |
| CHEMBL489638 | — | Ki | = | 746.0 | nM | 6.13 |
| CHEMBL489226 | — | Ki | = | 1150.0 | nM | 5.94 |
| CHEMBL449575 | — | Ki | = | 1290.0 | nM | 5.89 |
| CHEMBL514541 | — | Ki | = | 1410.0 | nM | 5.85 |
| CHEMBL523934 | — | Ki | = | 1440.0 | nM | 5.84 |
| CHEMBL522095 | — | Ki | = | 2520.0 | nM | 5.60 |
| CHEMBL478071 | — | Ki | = | 3030.0 | nM | 5.52 |
| CHEMBL489428 | — | Ki | = | 3480.0 | nM | 5.46 |
| CHEMBL489628 | — | Ki | = | 4350.0 | nM | 5.36 |
| CHEMBL489639 | — | Ki | = | 4490.0 | nM | 5.35 |
| CHEMBL514701 | — | Ki | = | 5900.0 | nM | 5.23 |
| CHEMBL515330 | — | Ki | = | 6740.0 | nM | 5.17 |
| CHEMBL477665 | — | Ki | = | 11600.0 | nM | 4.94 |