Assay Detail
Binding
CHEMBL1015328
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Displacement of [3H]CCPA from human recombinant adenosine A1 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 | 7.68 | 9.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL449575 | — | — | 1 | 9.29 |
| CHEMBL489640 | — | — | 1 | 9.27 |
| CHEMBL477444 | — | — | 1 | 9.23 |
| CHEMBL490250 | — | — | 1 | 9.15 |
| CHEMBL477445 | — | — | 1 | 8.81 |
| CHEMBL514541 | — | — | 1 | 8.79 |
| CHEMBL522095 | — | — | 1 | 8.39 |
| CHEMBL489639 | — | — | 1 | 8.16 |
| CHEMBL514701 | — | — | 1 | 8.04 |
| CHEMBL477665 | — | — | 1 | 8.04 |
| CHEMBL478071 | — | — | 1 | 7.89 |
| CHEMBL515330 | — | — | 1 | 7.55 |
| CHEMBL477666 | — | — | 1 | 7.19 |
| CHEMBL489638 | — | — | 1 | 6.60 |
| CHEMBL477667 | — | — | 1 | 6.59 |
| CHEMBL489428 | — | — | 1 | 5.97 |
| CHEMBL523934 | — | — | 1 | 5.78 |
| CHEMBL489226 | — | — | 1 | 5.67 |
| CHEMBL489628 | — | — | 1 | 5.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL449575 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL489640 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL477444 | — | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL490250 | — | Ki | = | 0.71 | nM | 9.15 |
| CHEMBL477445 | — | Ki | = | 1.56 | nM | 8.81 |
| CHEMBL514541 | — | Ki | = | 1.61 | nM | 8.79 |
| CHEMBL522095 | — | Ki | = | 4.09 | nM | 8.39 |
| CHEMBL489639 | — | Ki | = | 6.96 | nM | 8.16 |
| CHEMBL514701 | — | Ki | = | 9.16 | nM | 8.04 |
| CHEMBL477665 | — | Ki | = | 9.13 | nM | 8.04 |
| CHEMBL478071 | — | Ki | = | 12.8 | nM | 7.89 |
| CHEMBL515330 | — | Ki | = | 28.4 | nM | 7.55 |
| CHEMBL477666 | — | Ki | = | 64.7 | nM | 7.19 |
| CHEMBL489638 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL477667 | — | Ki | = | 258.0 | nM | 6.59 |
| CHEMBL489428 | — | Ki | = | 1060.0 | nM | 5.97 |
| CHEMBL523934 | — | Ki | = | 1680.0 | nM | 5.78 |
| CHEMBL489226 | — | Ki | = | 2150.0 | nM | 5.67 |
| CHEMBL489628 | — | Ki | = | 2970.0 | nM | 5.53 |