Assay Detail
Binding
CHEMBL873042
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Inhibitory activity at Adenosine A2A receptor by inhibition of [3H]-CGS- 21680 binding to bovine striatal membranes.
16
Total Activities
16
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
2'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.40 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL251997 | — | — | 1 | 8.41 |
| CHEMBL464859 | NECA | — | 1 | 7.80 |
| CHEMBL66393 | — | — | 1 | 7.69 |
| CHEMBL119709 | IB-MECA | — | 1 | 6.94 |
| CHEMBL285819 | — | — | 1 | 6.92 |
| CHEMBL2113418 | — | — | 1 | 6.66 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 6.42 |
| CHEMBL284969 | — | — | 1 | 6.24 |
| CHEMBL139000 | (R)-PIA | — | 1 | 6.12 |
| CHEMBL444550 | — | — | 1 | 6.03 |
| CHEMBL606495 | — | — | 1 | 5.88 |
| CHEMBL605034 | — | — | 1 | 5.81 |
| CHEMBL420705 | (S)-PIA | — | 1 | 5.75 |
| CHEMBL73809 | — | — | 1 | 5.47 |
| CHEMBL400189 | — | — | 1 | 5.14 |
| CHEMBL2113388 | — | — | 1 | 5.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL251997 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL464859 | NECA | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL66393 | — | Ki | = | 20.4 | nM | 7.69 |
| CHEMBL119709 | IB-MECA | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL285819 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL2113418 | — | Ki | = | 218.0 | nM | 6.66 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 385.0 | nM | 6.42 |
| CHEMBL284969 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL139000 | (R)-PIA | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL444550 | — | Ki | = | 935.0 | nM | 6.03 |
| CHEMBL606495 | — | Ki | = | 1330.0 | nM | 5.88 |
| CHEMBL605034 | — | Ki | = | 1533.0 | nM | 5.81 |
| CHEMBL420705 | (S)-PIA | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL73809 | — | Ki | = | 3420.0 | nM | 5.47 |
| CHEMBL400189 | — | Ki | = | 7220.0 | nM | 5.14 |
| CHEMBL2113388 | — | Ki | = | 7440.0 | nM | 5.13 |