Assay Detail
Binding
CHEMBL644658
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Binding affinity for HA-tagged mutant human Adenosine A2A receptor (H250N) using [3H]-CGS-21,680 as radioligand expressed in COS-7 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 6.58 | 9.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL16687 | CGS-15943 | — | 1 | 9.34 |
| CHEMBL464859 | NECA | — | 1 | 8.28 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | — | 1 | 7.81 |
| CHEMBL119709 | IB-MECA | — | 1 | 7.50 |
| CHEMBL2094089 | — | — | 1 | 7.45 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.54 |
| CHEMBL945 | AMILORIDE | 4.0 | 1 | 5.48 |
| CHEMBL193 | NIFEDIPINE | 4.0 | 1 | 4.65 |
| CHEMBL309490 | GALANGIN | — | 1 | 4.48 |
| CHEMBL87496 | — | — | 1 | 4.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL16687 | CGS-15943 | Ki | = | 0.457 | nM | 9.34 |
| CHEMBL464859 | NECA | Ki | = | 5.24 | nM | 8.28 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | Ki | = | 15.6 | nM | 7.81 |
| CHEMBL119709 | IB-MECA | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL2094089 | — | Ki | = | 35.9 | nM | 7.45 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 291.0 | nM | 6.54 |
| CHEMBL945 | AMILORIDE | Ki | = | 3280.0 | nM | 5.48 |
| CHEMBL193 | NIFEDIPINE | Ki | = | 22200.0 | nM | 4.65 |
| CHEMBL309490 | GALANGIN | Ki | = | 33000.0 | nM | 4.48 |
| CHEMBL87496 | — | Ki | = | 54300.0 | nM | 4.26 |