Assay Detail
Binding
CHEMBL1015329
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Displacement of [3H]NECA from human recombinant adenosine A2A 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 | 5.35 | 6.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL490250 | — | — | 1 | 6.10 |
| CHEMBL477444 | — | — | 1 | 6.08 |
| CHEMBL489640 | — | — | 1 | 5.90 |
| CHEMBL449575 | — | — | 1 | 5.87 |
| CHEMBL514541 | — | — | 1 | 5.69 |
| CHEMBL477445 | — | — | 1 | 5.67 |
| CHEMBL477667 | — | — | 1 | 5.66 |
| CHEMBL477666 | — | — | 1 | 5.29 |
| CHEMBL522095 | — | — | 1 | 5.06 |
| CHEMBL489639 | — | — | 1 | 4.93 |
| CHEMBL478071 | — | — | 1 | 4.79 |
| CHEMBL489638 | — | — | 1 | 4.72 |
| CHEMBL477665 | — | — | 1 | 4.62 |
| CHEMBL514701 | — | — | 1 | 4.50 |
| CHEMBL523934 | — | — | 1 | - |
| CHEMBL489226 | — | — | 1 | - |
| CHEMBL489428 | — | — | 1 | - |
| CHEMBL489628 | — | — | 1 | - |
| CHEMBL515330 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL490250 | — | Ki | = | 797.0 | nM | 6.10 |
| CHEMBL477444 | — | Ki | = | 837.0 | nM | 6.08 |
| CHEMBL489640 | — | Ki | = | 1270.0 | nM | 5.90 |
| CHEMBL449575 | — | Ki | = | 1340.0 | nM | 5.87 |
| CHEMBL514541 | — | Ki | = | 2050.0 | nM | 5.69 |
| CHEMBL477445 | — | Ki | = | 2160.0 | nM | 5.67 |
| CHEMBL477667 | — | Ki | = | 2190.0 | nM | 5.66 |
| CHEMBL477666 | — | Ki | = | 5170.0 | nM | 5.29 |
| CHEMBL522095 | — | Ki | = | 8780.0 | nM | 5.06 |
| CHEMBL489639 | — | Ki | = | 11800.0 | nM | 4.93 |
| CHEMBL478071 | — | Ki | = | 16200.0 | nM | 4.79 |
| CHEMBL489638 | — | Ki | = | 18900.0 | nM | 4.72 |
| CHEMBL477665 | — | Ki | = | 24000.0 | nM | 4.62 |
| CHEMBL514701 | — | Ki | = | 31600.0 | nM | 4.50 |
| CHEMBL523934 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL489226 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL489428 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL489628 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL515330 | — | Ki | > | 100000.0 | nM | - |