Assay Detail
Binding
CHEMBL647729
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Binding affinity against adenosine A2a receptor from rat striatum using [3H]-CGS- 21680 as a radioligand.
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
2-Aralkynyl and 2-heteroalkynyl derivatives of adenosine-5'-N-ethyluronamide as selective A2a adenosine receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 36 | 7.35 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2113450 | — | — | 1 | 8.92 |
| CHEMBL604851 | — | — | 1 | 8.80 |
| CHEMBL410873 | — | — | 1 | 8.66 |
| CHEMBL604019 | — | — | 1 | 8.37 |
| CHEMBL604026 | — | — | 1 | 8.23 |
| CHEMBL603596 | — | — | 1 | 8.20 |
| CHEMBL605690 | — | — | 1 | 8.15 |
| CHEMBL464859 | NECA | — | 1 | 8.11 |
| CHEMBL331372 | CGS-21680 | — | 1 | 7.96 |
| CHEMBL606319 | — | — | 1 | 7.78 |
| CHEMBL603809 | — | — | 1 | 7.72 |
| CHEMBL604649 | — | — | 1 | 7.71 |
| CHEMBL603602 | — | — | 1 | 7.69 |
| CHEMBL604234 | — | — | 1 | 7.67 |
| CHEMBL604440 | — | — | 1 | 7.56 |
| CHEMBL605685 | — | — | 1 | 7.44 |
| CHEMBL605265 | — | — | 1 | 7.38 |
| CHEMBL604849 | — | — | 1 | 7.28 |
| CHEMBL605264 | — | — | 1 | 7.26 |
| CHEMBL2113449 | — | — | 1 | 7.24 |
| CHEMBL605691 | — | — | 1 | 7.09 |
| CHEMBL603389 | — | — | 1 | 7.06 |
| CHEMBL606318 | — | — | 1 | 7.05 |
| CHEMBL604023 | — | — | 1 | 6.95 |
| CHEMBL223270 | — | — | 1 | 6.92 |
| CHEMBL605056 | — | — | 1 | 6.89 |
| CHEMBL605055 | — | — | 1 | 6.75 |
| CHEMBL603808 | — | — | 1 | 6.73 |
| CHEMBL603812 | — | — | 1 | 6.63 |
| CHEMBL604647 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2113450 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL604851 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL410873 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL604019 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL604026 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL603596 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL605690 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL464859 | NECA | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL331372 | CGS-21680 | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL606319 | — | Ki | = | 16.5 | nM | 7.78 |
| CHEMBL603809 | — | Ki | = | 19.1 | nM | 7.72 |
| CHEMBL604649 | — | Ki | = | 19.5 | nM | 7.71 |
| CHEMBL603602 | — | Ki | = | 20.6 | nM | 7.69 |
| CHEMBL604234 | — | Ki | = | 21.5 | nM | 7.67 |
| CHEMBL604440 | — | Ki | = | 27.4 | nM | 7.56 |
| CHEMBL605685 | — | Ki | = | 36.3 | nM | 7.44 |
| CHEMBL605265 | — | Ki | = | 41.3 | nM | 7.38 |
| CHEMBL604849 | — | Ki | = | 52.4 | nM | 7.28 |
| CHEMBL605264 | — | Ki | = | 54.8 | nM | 7.26 |
| CHEMBL2113449 | — | Ki | = | 57.8 | nM | 7.24 |
| CHEMBL605691 | — | Ki | = | 81.4 | nM | 7.09 |
| CHEMBL603389 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL606318 | — | Ki | = | 89.8 | nM | 7.05 |
| CHEMBL604023 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL223270 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL605056 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL605055 | — | Ki | = | 176.0 | nM | 6.75 |
| CHEMBL603808 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL603812 | — | Ki | = | 234.0 | nM | 6.63 |
| CHEMBL604647 | — | Ki | = | 315.0 | nM | 6.50 |
| CHEMBL605057 | — | Ki | = | 488.0 | nM | 6.31 |
| CHEMBL284969 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL605478 | — | Ki | = | 743.0 | nM | 6.13 |
| CHEMBL605473 | — | Ki | = | 1158.0 | nM | 5.94 |
| CHEMBL606315 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL605065 | — | Ki | > | 1000.0 | nM | - |