Assay Detail
Binding
CHEMBL918607
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Displacement of [3H]CPPA from human adenosine A1 receptor expressed in CHO cells
32
Total Activities
32
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 | Expert |
Publication
Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 6.71 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL139000 | (R)-PIA | — | 1 | 8.70 |
| CHEMBL224874 | — | — | 1 | 8.68 |
| CHEMBL464859 | NECA | — | 1 | 8.17 |
| CHEMBL376542 | — | — | 1 | 8.15 |
| CHEMBL2113271 | — | — | 1 | 7.13 |
| CHEMBL222442 | — | — | 1 | 6.89 |
| CHEMBL374760 | — | — | 1 | 6.85 |
| CHEMBL222907 | — | — | 1 | 6.84 |
| CHEMBL223366 | — | — | 1 | 6.83 |
| CHEMBL373478 | — | — | 1 | 6.82 |
| CHEMBL225233 | — | — | 1 | 6.76 |
| CHEMBL223845 | — | — | 1 | 6.72 |
| CHEMBL374461 | — | — | 1 | 6.71 |
| CHEMBL223729 | — | — | 1 | 6.68 |
| CHEMBL222945 | — | — | 1 | 6.66 |
| CHEMBL374685 | — | — | 1 | 6.66 |
| CHEMBL225459 | — | — | 1 | 6.60 |
| CHEMBL225287 | — | — | 1 | 6.55 |
| CHEMBL222500 | — | — | 1 | 6.51 |
| CHEMBL225593 | — | — | 1 | 6.51 |
| CHEMBL225535 | — | — | 1 | 6.48 |
| CHEMBL222748 | — | — | 1 | 6.46 |
| CHEMBL222194 | — | — | 1 | 6.45 |
| CHEMBL434377 | — | — | 1 | 6.35 |
| CHEMBL426928 | — | — | 1 | 6.33 |
| CHEMBL223002 | — | — | 1 | 6.24 |
| CHEMBL261515 | — | — | 1 | 6.19 |
| CHEMBL374151 | — | — | 1 | 6.02 |
| CHEMBL222392 | — | — | 1 | 5.81 |
| CHEMBL374028 | — | — | 1 | 5.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL139000 | (R)-PIA | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL224874 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL464859 | NECA | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL376542 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL2113271 | — | Ki | = | 73.6 | nM | 7.13 |
| CHEMBL222442 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL374760 | — | Ki | = | 141.0 | nM | 6.85 |
| CHEMBL222907 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL223366 | — | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL373478 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL225233 | — | Ki | = | 174.0 | nM | 6.76 |
| CHEMBL223845 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL374461 | — | Ki | = | 197.0 | nM | 6.71 |
| CHEMBL223729 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL374685 | — | Ki | = | 221.0 | nM | 6.66 |
| CHEMBL222945 | — | Ki | = | 218.0 | nM | 6.66 |
| CHEMBL225459 | — | Ki | = | 253.0 | nM | 6.60 |
| CHEMBL225287 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL222500 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL225593 | — | Ki | = | 312.0 | nM | 6.51 |
| CHEMBL225535 | — | Ki | = | 331.0 | nM | 6.48 |
| CHEMBL222748 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL222194 | — | Ki | = | 358.0 | nM | 6.45 |
| CHEMBL434377 | — | Ki | = | 443.0 | nM | 6.35 |
| CHEMBL426928 | — | Ki | = | 467.0 | nM | 6.33 |
| CHEMBL223002 | — | Ki | = | 579.0 | nM | 6.24 |
| CHEMBL261515 | — | Ki | = | 640.0 | nM | 6.19 |
| CHEMBL374151 | — | Ki | = | 960.0 | nM | 6.02 |
| CHEMBL222392 | — | Ki | = | 1560.0 | nM | 5.81 |
| CHEMBL374028 | — | Ki | = | 1820.0 | nM | 5.74 |
| CHEMBL387324 | — | Ki | = | 2060.0 | nM | 5.69 |
| CHEMBL223846 | — | Ki | = | 2640.0 | nM | 5.58 |