Assay Detail
Binding
CHEMBL642117
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Ability to displace the specific binding of [3H]-CGS- to adenosine A2A receptor form bovine brain striatal membranes
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
A novel class of highly potent and selective A1 adenosine antagonists: structure-affinity profile of a series of 1,8-naphthyridine derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 6.27 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL464859 | NECA | — | 1 | 7.80 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | — | 1 | 7.20 |
| CHEMBL97687 | — | — | 1 | 7.18 |
| CHEMBL97760 | — | — | 1 | 7.00 |
| CHEMBL97757 | — | — | 1 | 6.77 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 6.41 |
| CHEMBL97337 | — | — | 1 | 6.38 |
| CHEMBL97549 | — | — | 1 | 6.34 |
| CHEMBL316630 | — | — | 1 | 6.34 |
| CHEMBL95384 | — | — | 1 | 6.33 |
| CHEMBL313864 | — | — | 1 | 6.20 |
| CHEMBL45891 | — | — | 1 | 6.12 |
| CHEMBL139000 | (R)-PIA | — | 1 | 6.12 |
| CHEMBL97624 | — | — | 1 | 6.08 |
| CHEMBL329293 | — | — | 1 | 5.90 |
| CHEMBL329294 | — | — | 1 | 5.85 |
| CHEMBL420705 | (S)-PIA | — | 1 | 5.75 |
| CHEMBL94538 | — | — | 1 | 5.75 |
| CHEMBL97896 | — | — | 1 | 5.72 |
| CHEMBL102430 | — | — | 1 | 5.23 |
| CHEMBL97665 | — | — | 1 | 5.16 |
| CHEMBL97663 | — | — | 1 | - |
| CHEMBL97778 | — | — | 1 | - |
| CHEMBL97037 | — | — | 1 | - |
| CHEMBL98227 | — | — | 1 | - |
| CHEMBL96576 | — | — | 1 | - |
| CHEMBL97904 | — | — | 1 | - |
| CHEMBL415697 | — | — | 1 | - |
| CHEMBL97344 | — | — | 1 | - |
| CHEMBL319580 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL464859 | NECA | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL97687 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL97760 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL97757 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL97337 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL97549 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL316630 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL95384 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL313864 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL45891 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL139000 | (R)-PIA | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL97624 | — | Ki | = | 830.0 | nM | 6.08 |
| CHEMBL329293 | — | Ki | = | 1250.0 | nM | 5.90 |
| CHEMBL329294 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL94538 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL420705 | (S)-PIA | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL97896 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL102430 | — | Ki | = | 5900.0 | nM | 5.23 |
| CHEMBL97665 | — | Ki | = | 7000.0 | nM | 5.16 |
| CHEMBL96617 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL328214 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL328334 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL97895 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL319580 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL97344 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL415697 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL97904 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL96576 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL98227 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL97037 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL97778 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL97663 | — | Ki | > | 10000.0 | nM | - |