Assay Detail
Binding
CHEMBL649103
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Inhibition of [3H]CHA binding to adenosine A1 receptor from rat brain membranes
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Nucleosides and nucleotides. 107. 2-(cycloalkylalkynyl)adenosines: adenosine A2 receptor agonists with potent antihypertensive effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.18 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2092941 | — | — | 1 | 8.47 |
| CHEMBL2113503 | — | — | 1 | 8.08 |
| CHEMBL608299 | — | — | 1 | 7.96 |
| CHEMBL608899 | — | — | 1 | 7.96 |
| CHEMBL2113506 | — | — | 1 | 7.82 |
| CHEMBL608594 | — | — | 1 | 7.80 |
| CHEMBL2113497 | — | — | 1 | 7.68 |
| CHEMBL2113501 | — | — | 1 | 7.57 |
| CHEMBL2113505 | — | — | 1 | 7.50 |
| CHEMBL2113498 | — | — | 1 | 7.25 |
| CHEMBL2113504 | — | — | 1 | 7.06 |
| CHEMBL2094089 | — | — | 1 | 6.97 |
| CHEMBL319387 | — | — | 1 | 6.90 |
| CHEMBL2113496 | — | — | 1 | 6.88 |
| CHEMBL610362 | — | — | 1 | 6.87 |
| CHEMBL609493 | — | — | 1 | 6.86 |
| CHEMBL2113499 | — | — | 1 | 6.79 |
| CHEMBL610651 | — | — | 1 | 6.68 |
| CHEMBL608298 | — | — | 1 | 6.50 |
| CHEMBL2113500 | — | — | 1 | 6.40 |
| CHEMBL375190 | — | — | 1 | 6.15 |
| CHEMBL331372 | CGS-21680 | — | 1 | 5.91 |
| CHEMBL612161 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2092941 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL2113503 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL608299 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL608899 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2113506 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL608594 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2113497 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL2113501 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL2113505 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL2113498 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL2113504 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL2094089 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL319387 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL2113496 | — | Ki | = | 133.0 | nM | 6.88 |
| CHEMBL610362 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL609493 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL2113499 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL610651 | — | Ki | = | 208.0 | nM | 6.68 |
| CHEMBL608298 | — | Ki | = | 313.0 | nM | 6.50 |
| CHEMBL2113500 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL375190 | — | Ki | = | 701.0 | nM | 6.15 |
| CHEMBL331372 | CGS-21680 | Ki | = | 1232.0 | nM | 5.91 |
| CHEMBL612161 | — | Ki | > | 229.0 | nM | - |