Assay Detail
Binding
CHEMBL950994
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Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.33 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL464859 | NECA | — | 1 | 7.80 |
| CHEMBL271753 | — | — | 1 | 7.15 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.47 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 6.40 |
| CHEMBL406727 | — | — | 1 | 6.40 |
| CHEMBL200636 | — | — | 1 | 6.25 |
| CHEMBL198779 | — | — | 1 | 6.08 |
| CHEMBL272174 | — | — | 1 | 5.95 |
| CHEMBL198008 | — | — | 1 | 5.46 |
| CHEMBL271106 | — | — | 1 | 5.38 |
| CHEMBL260311 | — | — | 1 | - |
| CHEMBL445664 | — | — | 1 | - |
| CHEMBL200480 | — | — | 1 | - |
| CHEMBL403521 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL464859 | NECA | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL271753 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 337.0 | nM | 6.47 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 401.0 | nM | 6.40 |
| CHEMBL406727 | — | Ki | = | 398.0 | nM | 6.40 |
| CHEMBL200636 | — | Ki | = | 561.0 | nM | 6.25 |
| CHEMBL198779 | — | Ki | = | 833.0 | nM | 6.08 |
| CHEMBL272174 | — | Ki | = | 1121.0 | nM | 5.95 |
| CHEMBL198008 | — | Ki | = | 3440.0 | nM | 5.46 |
| CHEMBL271106 | — | Ki | = | 4149.0 | nM | 5.38 |
| CHEMBL260311 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL445664 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL200480 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL403521 | — | Ki | > | 10000.0 | nM | - |