Assay Detail
Binding
CHEMBL647487
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Displacement of specific [3H]-SCH- 58261 binding at human Adenosine A2A receptor expressed in HEK293 cells.
19
Total Activities
19
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
7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 8.71 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL22202 | — | — | 1 | 9.92 |
| CHEMBL22320 | — | — | 1 | 9.89 |
| CHEMBL2112948 | — | — | 1 | 9.74 |
| CHEMBL281805 | — | — | 1 | 9.66 |
| CHEMBL22200 | — | — | 1 | 9.37 |
| CHEMBL278805 | — | — | 1 | 9.23 |
| CHEMBL22241 | — | — | 1 | 9.00 |
| CHEMBL17127 | SCH-58261 | — | 1 | 8.96 |
| CHEMBL278812 | — | — | 1 | 8.96 |
| CHEMBL17121 | SCH-63390 | — | 1 | 8.92 |
| CHEMBL23745 | — | — | 1 | 8.88 |
| CHEMBL442338 | — | — | 1 | 8.40 |
| CHEMBL281601 | — | — | 1 | 8.36 |
| CHEMBL279254 | — | — | 1 | 8.33 |
| CHEMBL22500 | — | — | 1 | 8.32 |
| CHEMBL22822 | — | — | 1 | 8.22 |
| CHEMBL22316 | — | — | 1 | 7.26 |
| CHEMBL22191 | — | — | 1 | 7.07 |
| CHEMBL22968 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL22202 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL22320 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL2112948 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL281805 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL22200 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL278805 | — | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL22241 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL17127 | SCH-58261 | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL278812 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL17121 | SCH-63390 | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL23745 | — | Ki | = | 1.31 | nM | 8.88 |
| CHEMBL442338 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL281601 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL279254 | — | Ki | = | 4.63 | nM | 8.33 |
| CHEMBL22500 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL22822 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL22316 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL22191 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL22968 | — | Ki | = | 100.0 | nM | 7.00 |