Assay Detail
Binding
CHEMBL649775
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Displacement of [3H]-CGS- 21680 from adenosine A2a receptor of bovine striatal membrane
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
3-Aryl[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: a new class of selective A1 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 6.04 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL464859 | NECA | — | 1 | 7.80 |
| CHEMBL7608 | — | — | 1 | 6.62 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.47 |
| CHEMBL307199 | — | — | 1 | 6.40 |
| CHEMBL269112 | — | — | 1 | 5.99 |
| CHEMBL109691 | — | — | 1 | 5.92 |
| CHEMBL113518 | — | — | 1 | 5.91 |
| CHEMBL7327 | — | — | 1 | 5.89 |
| CHEMBL7113 | — | — | 1 | 5.54 |
| CHEMBL7334 | — | — | 1 | 5.46 |
| CHEMBL7953 | — | — | 1 | 5.30 |
| CHEMBL7098 | — | — | 1 | 5.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL464859 | NECA | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL7608 | — | Ki | = | 241.0 | nM | 6.62 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 337.0 | nM | 6.47 |
| CHEMBL307199 | — | Ki | = | 401.0 | nM | 6.40 |
| CHEMBL269112 | — | Ki | = | 1023.0 | nM | 5.99 |
| CHEMBL109691 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL113518 | — | Ki | = | 1236.0 | nM | 5.91 |
| CHEMBL7327 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL7113 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL7334 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL7953 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL7098 | — | Ki | = | 6300.0 | nM | 5.20 |