Assay Detail
Binding
CHEMBL829686
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Inhibition constant against human Adenosine A2a receptor using [3H]-SCH- 58261 as radioligand expressed in HEK cell membranes
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
6-(2-Furanyl)-9H-purin-2-amine derivatives as A2A adenosine antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.89 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL195364 | — | — | 1 | 8.85 |
| CHEMBL372475 | — | — | 1 | 8.55 |
| CHEMBL195503 | — | — | 1 | 8.51 |
| CHEMBL17127 | SCH-58261 | — | 1 | 8.37 |
| CHEMBL371615 | — | — | 1 | 8.35 |
| CHEMBL193613 | — | — | 1 | 8.25 |
| CHEMBL195543 | — | — | 1 | 8.20 |
| CHEMBL193761 | — | — | 1 | 8.17 |
| CHEMBL193414 | — | — | 1 | 8.15 |
| CHEMBL195410 | — | — | 1 | 8.11 |
| CHEMBL197148 | — | — | 1 | 8.06 |
| CHEMBL195294 | — | — | 1 | 8.00 |
| CHEMBL371436 | — | — | 1 | 7.91 |
| CHEMBL424827 | — | — | 1 | 7.69 |
| CHEMBL195330 | — | — | 1 | 7.67 |
| CHEMBL195866 | — | — | 1 | 7.66 |
| CHEMBL372928 | — | — | 1 | 7.58 |
| CHEMBL196436 | — | — | 1 | 7.46 |
| CHEMBL439336 | — | — | 1 | 7.16 |
| CHEMBL194383 | — | — | 1 | 6.57 |
| CHEMBL372064 | — | — | 1 | 6.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL195364 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL372475 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL195503 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL17127 | SCH-58261 | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL371615 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL193613 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL195543 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL193761 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL193414 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL195410 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL197148 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL195294 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL371436 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL424827 | — | Ki | = | 20.5 | nM | 7.69 |
| CHEMBL195330 | — | Ki | = | 21.5 | nM | 7.67 |
| CHEMBL195866 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL372928 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL196436 | — | Ki | = | 34.9 | nM | 7.46 |
| CHEMBL439336 | — | Ki | = | 68.5 | nM | 7.16 |
| CHEMBL194383 | — | Ki | = | 270.5 | nM | 6.57 |
| CHEMBL372064 | — | Ki | = | 381.0 | nM | 6.42 |