Assay Detail
Binding
CHEMBL918609
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]CGS-21680 from human adenosine A2A receptor expressed in CHO cells
35
Total Activities
35
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 | 35 | 6.78 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL224874 | — | — | 1 | 8.70 |
| CHEMBL464859 | NECA | — | 1 | 8.66 |
| CHEMBL374685 | — | — | 1 | 8.03 |
| CHEMBL225233 | — | — | 1 | 7.96 |
| CHEMBL225287 | — | — | 1 | 7.88 |
| CHEMBL374760 | — | — | 1 | 7.79 |
| CHEMBL222907 | — | — | 1 | 7.53 |
| CHEMBL434377 | — | — | 1 | 7.40 |
| CHEMBL223366 | — | — | 1 | 7.35 |
| CHEMBL426928 | — | — | 1 | 7.25 |
| CHEMBL225535 | — | — | 1 | 7.24 |
| CHEMBL225593 | — | — | 1 | 7.16 |
| CHEMBL222945 | — | — | 1 | 7.02 |
| CHEMBL225459 | — | — | 1 | 6.82 |
| CHEMBL223729 | — | — | 1 | 6.60 |
| CHEMBL223845 | — | — | 1 | 6.60 |
| CHEMBL2113271 | — | — | 1 | 6.56 |
| CHEMBL2113270 | — | — | 1 | 6.46 |
| CHEMBL223846 | — | — | 1 | 6.44 |
| CHEMBL373478 | — | — | 1 | 6.43 |
| CHEMBL374461 | — | — | 1 | 6.43 |
| CHEMBL222442 | — | — | 1 | 6.41 |
| CHEMBL222392 | — | — | 1 | 6.38 |
| CHEMBL222500 | — | — | 1 | 6.35 |
| CHEMBL374151 | — | — | 1 | 6.30 |
| CHEMBL222194 | — | — | 1 | 6.30 |
| CHEMBL387324 | — | — | 1 | 6.29 |
| CHEMBL387354 | — | — | 1 | 6.24 |
| CHEMBL376542 | — | — | 1 | 6.20 |
| CHEMBL139000 | (R)-PIA | — | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL224874 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL464859 | NECA | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL374685 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL225233 | — | Ki | = | 10.9 | nM | 7.96 |
| CHEMBL225287 | — | Ki | = | 13.3 | nM | 7.88 |
| CHEMBL374760 | — | Ki | = | 16.1 | nM | 7.79 |
| CHEMBL222907 | — | Ki | = | 29.3 | nM | 7.53 |
| CHEMBL434377 | — | Ki | = | 39.7 | nM | 7.40 |
| CHEMBL223366 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL426928 | — | Ki | = | 56.8 | nM | 7.25 |
| CHEMBL225535 | — | Ki | = | 58.1 | nM | 7.24 |
| CHEMBL225593 | — | Ki | = | 69.3 | nM | 7.16 |
| CHEMBL222945 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL225459 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL223845 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL223729 | — | Ki | = | 252.0 | nM | 6.60 |
| CHEMBL2113271 | — | Ki | = | 277.0 | nM | 6.56 |
| CHEMBL2113270 | — | Ki | = | 344.0 | nM | 6.46 |
| CHEMBL223846 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL373478 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL374461 | — | Ki | = | 373.0 | nM | 6.43 |
| CHEMBL222442 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL222392 | — | Ki | = | 413.0 | nM | 6.38 |
| CHEMBL222500 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL374151 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL222194 | — | Ki | = | 502.0 | nM | 6.30 |
| CHEMBL387324 | — | Ki | = | 519.0 | nM | 6.29 |
| CHEMBL387354 | — | Ki | = | 579.0 | nM | 6.24 |
| CHEMBL376542 | — | Ki | = | 628.0 | nM | 6.20 |
| CHEMBL139000 | (R)-PIA | Ki | = | 884.0 | nM | 6.05 |
| CHEMBL222748 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL374028 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL221777 | — | Ki | = | 2570.0 | nM | 5.59 |
| CHEMBL375080 | — | Ki | = | 2670.0 | nM | 5.57 |
| CHEMBL221363 | — | Ki | = | 3870.0 | nM | 5.41 |