Assay Detail
Binding
CHEMBL642180
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Binding affinity for adenosine A2A receptor was determined by displacement of [3H]-DPCPX from rat striatal membranes.
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
N-cycloalkyl derivatives of adenosine and 1-deazaadenosine as agonists and partial agonists of the A(1) adenosine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 5.52 | 6.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL569275 | — | — | 1 | 6.38 |
| CHEMBL2113520 | — | — | 1 | 6.34 |
| CHEMBL2113423 | — | — | 1 | 6.29 |
| CHEMBL2113517 | — | — | 1 | 6.23 |
| CHEMBL45891 | — | — | 1 | 6.22 |
| CHEMBL284969 | — | — | 1 | 6.19 |
| CHEMBL608306 | — | — | 1 | 5.96 |
| CHEMBL2113518 | — | — | 1 | 5.69 |
| CHEMBL2113390 | — | — | 1 | 5.55 |
| CHEMBL2113477 | — | — | 1 | 5.51 |
| CHEMBL2113430 | — | — | 1 | 5.50 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 5.47 |
| CHEMBL2113424 | — | — | 1 | 5.38 |
| CHEMBL607729 | — | — | 1 | 5.37 |
| CHEMBL312981 | — | — | 1 | 5.31 |
| CHEMBL2113387 | — | — | 1 | 5.29 |
| CHEMBL2113391 | — | — | 1 | 5.28 |
| CHEMBL2113516 | — | — | 1 | 5.18 |
| CHEMBL611851 | — | — | 1 | 5.04 |
| CHEMBL2113521 | — | — | 1 | 5.02 |
| CHEMBL2113389 | — | — | 1 | 5.00 |
| CHEMBL606228 | — | — | 1 | 4.86 |
| CHEMBL2113478 | — | — | 1 | 4.79 |
| CHEMBL604965 | — | — | 1 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL569275 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL2113520 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL2113423 | — | Ki | = | 510.0 | nM | 6.29 |
| CHEMBL2113517 | — | Ki | = | 590.0 | nM | 6.23 |
| CHEMBL45891 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL284969 | — | Ki | = | 640.0 | nM | 6.19 |
| CHEMBL608306 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL2113518 | — | Ki | = | 2060.0 | nM | 5.69 |
| CHEMBL2113390 | — | Ki | = | 2840.0 | nM | 5.55 |
| CHEMBL2113477 | — | Ki | = | 3110.0 | nM | 5.51 |
| CHEMBL2113430 | — | Ki | = | 3150.0 | nM | 5.50 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 3370.0 | nM | 5.47 |
| CHEMBL2113424 | — | Ki | = | 4180.0 | nM | 5.38 |
| CHEMBL607729 | — | Ki | = | 4230.0 | nM | 5.37 |
| CHEMBL312981 | — | Ki | = | 4870.0 | nM | 5.31 |
| CHEMBL2113387 | — | Ki | = | 5120.0 | nM | 5.29 |
| CHEMBL2113391 | — | Ki | = | 5210.0 | nM | 5.28 |
| CHEMBL2113516 | — | Ki | = | 6550.0 | nM | 5.18 |
| CHEMBL611851 | — | Ki | = | 9200.0 | nM | 5.04 |
| CHEMBL2113521 | — | Ki | = | 9640.0 | nM | 5.02 |
| CHEMBL2113389 | — | Ki | = | 10100.0 | nM | 5.00 |
| CHEMBL606228 | — | Ki | = | 13700.0 | nM | 4.86 |
| CHEMBL2113478 | — | Ki | = | 16400.0 | nM | 4.79 |
| CHEMBL604965 | — | Ki | = | 20000.0 | nM | 4.70 |