Assay Detail
Binding
CHEMBL644127
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Affinity for adenosine A1 receptor assayed in a competition assay in rat brain using [3H]-CHA as radioligand
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
2-Alkynyl derivatives of adenosine-5'-N-ethyluronamide: selective A2 adenosine receptor agonists with potent inhibitory activity on platelet aggregation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 7.33 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL284969 | — | — | 1 | 8.89 |
| CHEMBL2094083 | — | — | 1 | 8.60 |
| CHEMBL2113405 | — | — | 1 | 8.52 |
| CHEMBL2113404 | — | — | 1 | 8.40 |
| CHEMBL464859 | NECA | — | 1 | 7.98 |
| CHEMBL2113410 | — | — | 1 | 7.96 |
| CHEMBL2113483 | — | — | 1 | 7.85 |
| CHEMBL2113482 | — | — | 1 | 7.55 |
| CHEMBL2113399 | — | — | 1 | 7.49 |
| CHEMBL2113449 | — | — | 1 | 7.45 |
| CHEMBL2113412 | — | — | 1 | 7.42 |
| CHEMBL2113407 | — | — | 1 | 7.38 |
| CHEMBL2113414 | — | — | 1 | 7.33 |
| CHEMBL2113403 | — | — | 1 | 7.31 |
| CHEMBL2113408 | — | — | 1 | 7.16 |
| CHEMBL2113413 | — | — | 1 | 7.00 |
| CHEMBL410873 | — | — | 1 | 6.89 |
| CHEMBL2113417 | — | — | 1 | 6.78 |
| CHEMBL2113402 | — | — | 1 | 6.74 |
| CHEMBL2113411 | — | — | 1 | 6.63 |
| CHEMBL2113419 | — | — | 1 | 6.57 |
| CHEMBL2113486 | — | — | 1 | 6.40 |
| CHEMBL2113485 | — | — | 1 | 6.18 |
| CHEMBL2113416 | — | — | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL284969 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL2094083 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL2113405 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL2113404 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL464859 | NECA | Ki | = | 10.4 | nM | 7.98 |
| CHEMBL2113410 | — | Ki | = | 11.1 | nM | 7.96 |
| CHEMBL2113483 | — | Ki | = | 14.1 | nM | 7.85 |
| CHEMBL2113482 | — | Ki | = | 27.9 | nM | 7.55 |
| CHEMBL2113399 | — | Ki | = | 32.7 | nM | 7.49 |
| CHEMBL2113449 | — | Ki | = | 35.4 | nM | 7.45 |
| CHEMBL2113412 | — | Ki | = | 37.9 | nM | 7.42 |
| CHEMBL2113407 | — | Ki | = | 42.1 | nM | 7.38 |
| CHEMBL2113414 | — | Ki | = | 47.3 | nM | 7.33 |
| CHEMBL2113403 | — | Ki | = | 48.6 | nM | 7.31 |
| CHEMBL2113408 | — | Ki | = | 69.6 | nM | 7.16 |
| CHEMBL2113413 | — | Ki | = | 99.9 | nM | 7.00 |
| CHEMBL410873 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL2113417 | — | Ki | = | 167.0 | nM | 6.78 |
| CHEMBL2113402 | — | Ki | = | 184.0 | nM | 6.74 |
| CHEMBL2113411 | — | Ki | = | 236.0 | nM | 6.63 |
| CHEMBL2113419 | — | Ki | = | 267.0 | nM | 6.57 |
| CHEMBL2113486 | — | Ki | = | 398.0 | nM | 6.40 |
| CHEMBL2113485 | — | Ki | = | 656.0 | nM | 6.18 |
| CHEMBL2113416 | — | Ki | = | 3295.0 | nM | 5.48 |