Assay Detail
Binding
CHEMBL644322
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Displacement of specific [3H]DPCPX binding at human Adenosine A1 receptor expressed in CHO cells.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous 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 | 6.07 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL22822 | — | — | 1 | 7.22 |
| CHEMBL22316 | — | — | 1 | 7.12 |
| CHEMBL22202 | — | — | 1 | 6.91 |
| CHEMBL2112948 | — | — | 1 | 6.75 |
| CHEMBL22968 | — | — | 1 | 6.72 |
| CHEMBL17121 | SCH-63390 | — | 1 | 6.46 |
| CHEMBL22500 | — | — | 1 | 6.38 |
| CHEMBL17127 | SCH-58261 | — | 1 | 6.26 |
| CHEMBL278812 | — | — | 1 | 6.25 |
| CHEMBL22320 | — | — | 1 | 6.24 |
| CHEMBL22241 | — | — | 1 | 5.99 |
| CHEMBL281805 | — | — | 1 | 5.67 |
| CHEMBL23745 | — | — | 1 | 5.58 |
| CHEMBL22200 | — | — | 1 | 5.38 |
| CHEMBL442338 | — | — | 1 | 5.35 |
| CHEMBL279254 | — | — | 1 | 5.31 |
| CHEMBL281601 | — | — | 1 | 5.30 |
| CHEMBL278805 | — | — | 1 | 5.28 |
| CHEMBL22191 | — | — | 1 | 5.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL22822 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL22316 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL22202 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL2112948 | — | Ki | = | 179.0 | nM | 6.75 |
| CHEMBL22968 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL17121 | SCH-63390 | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL22500 | — | Ki | = | 419.0 | nM | 6.38 |
| CHEMBL17127 | SCH-58261 | Ki | = | 549.0 | nM | 6.26 |
| CHEMBL278812 | — | Ki | = | 558.0 | nM | 6.25 |
| CHEMBL22320 | — | Ki | = | 576.0 | nM | 6.24 |
| CHEMBL22241 | — | Ki | = | 1026.0 | nM | 5.99 |
| CHEMBL281805 | — | Ki | = | 2160.0 | nM | 5.67 |
| CHEMBL23745 | — | Ki | = | 2630.0 | nM | 5.58 |
| CHEMBL22200 | — | Ki | = | 4197.0 | nM | 5.38 |
| CHEMBL442338 | — | Ki | = | 4494.0 | nM | 5.35 |
| CHEMBL279254 | — | Ki | = | 4927.0 | nM | 5.31 |
| CHEMBL281601 | — | Ki | = | 4965.0 | nM | 5.30 |
| CHEMBL278805 | — | Ki | = | 5297.0 | nM | 5.28 |
| CHEMBL22191 | — | Ki | = | 6496.0 | nM | 5.19 |