Assay Detail
Binding
CHEMBL636766
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Binding affinity against adenosine A1 receptor from rat brain using [3H]CHA 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 | 6.54 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL284969 | — | — | 1 | 8.89 |
| CHEMBL464859 | NECA | — | 1 | 7.98 |
| CHEMBL604019 | — | — | 1 | 7.56 |
| CHEMBL604851 | — | — | 1 | 7.56 |
| CHEMBL603809 | — | — | 1 | 7.45 |
| CHEMBL2113449 | — | — | 1 | 7.45 |
| CHEMBL604026 | — | — | 1 | 7.28 |
| CHEMBL605265 | — | — | 1 | 7.07 |
| CHEMBL604440 | — | — | 1 | 7.04 |
| CHEMBL606318 | — | — | 1 | 6.94 |
| CHEMBL410873 | — | — | 1 | 6.89 |
| CHEMBL603812 | — | — | 1 | 6.86 |
| CHEMBL606319 | — | — | 1 | 6.75 |
| CHEMBL2113450 | — | — | 1 | 6.68 |
| CHEMBL605056 | — | — | 1 | 6.51 |
| CHEMBL604849 | — | — | 1 | 6.38 |
| CHEMBL603389 | — | — | 1 | 6.37 |
| CHEMBL605690 | — | — | 1 | 6.35 |
| CHEMBL605685 | — | — | 1 | 6.30 |
| CHEMBL603602 | — | — | 1 | 6.30 |
| CHEMBL331372 | CGS-21680 | — | 1 | 6.25 |
| CHEMBL604023 | — | — | 1 | 6.22 |
| CHEMBL604649 | — | — | 1 | 6.22 |
| CHEMBL223270 | — | — | 1 | 6.16 |
| CHEMBL604234 | — | — | 1 | 6.05 |
| CHEMBL603596 | — | — | 1 | 6.00 |
| CHEMBL605055 | — | — | 1 | 5.84 |
| CHEMBL605264 | — | — | 1 | 5.79 |
| CHEMBL604647 | — | — | 1 | 5.61 |
| CHEMBL605691 | — | — | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL284969 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL464859 | NECA | Ki | = | 10.4 | nM | 7.98 |
| CHEMBL604851 | — | Ki | = | 27.4 | nM | 7.56 |
| CHEMBL604019 | — | Ki | = | 27.5 | nM | 7.56 |
| CHEMBL603809 | — | Ki | = | 35.9 | nM | 7.45 |
| CHEMBL2113449 | — | Ki | = | 35.4 | nM | 7.45 |
| CHEMBL604026 | — | Ki | = | 52.8 | nM | 7.28 |
| CHEMBL605265 | — | Ki | = | 85.4 | nM | 7.07 |
| CHEMBL604440 | — | Ki | = | 90.5 | nM | 7.04 |
| CHEMBL606318 | — | Ki | = | 114.0 | nM | 6.94 |
| CHEMBL410873 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL603812 | — | Ki | = | 139.0 | nM | 6.86 |
| CHEMBL606319 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL2113450 | — | Ki | = | 209.0 | nM | 6.68 |
| CHEMBL605056 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL604849 | — | Ki | = | 414.0 | nM | 6.38 |
| CHEMBL603389 | — | Ki | = | 428.0 | nM | 6.37 |
| CHEMBL605690 | — | Ki | = | 448.0 | nM | 6.35 |
| CHEMBL605685 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL603602 | — | Ki | = | 497.0 | nM | 6.30 |
| CHEMBL331372 | CGS-21680 | Ki | = | 569.0 | nM | 6.25 |
| CHEMBL604023 | — | Ki | = | 599.0 | nM | 6.22 |
| CHEMBL604649 | — | Ki | = | 597.0 | nM | 6.22 |
| CHEMBL223270 | — | Ki | = | 698.0 | nM | 6.16 |
| CHEMBL604234 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL603596 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL605055 | — | Ki | = | 1435.0 | nM | 5.84 |
| CHEMBL605264 | — | Ki | = | 1603.0 | nM | 5.79 |
| CHEMBL604647 | — | Ki | = | 2432.0 | nM | 5.61 |
| CHEMBL605691 | — | Ki | = | 3312.0 | nM | 5.48 |
| CHEMBL605057 | — | Ki | = | 4463.0 | nM | 5.35 |
| CHEMBL605473 | — | Ki | = | 6864.0 | nM | 5.16 |
| CHEMBL606315 | — | Ki | = | 7498.0 | nM | 5.12 |
| CHEMBL603808 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL605065 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL605478 | — | Ki | > | 10000.0 | nM | - |