Assay Detail
Binding
CHEMBL838860
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Percent inhibition of [3H]ZM241,385 binding to human adenosine A2a receptor expressed in CHO cells at 10 uM
11
Total Activities
11
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 | Expert |
Publication
"Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 5.13 | 5.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL188967 | — | — | 1 | 5.92 |
| CHEMBL188592 | — | — | 1 | 5.77 |
| CHEMBL188958 | — | — | 1 | 5.53 |
| CHEMBL187458 | — | — | 1 | 5.38 |
| CHEMBL366216 | — | — | 1 | 5.21 |
| CHEMBL2113046 | — | — | 1 | 5.11 |
| CHEMBL191270 | — | — | 1 | 4.85 |
| CHEMBL363419 | — | — | 1 | 4.80 |
| CHEMBL446698 | — | — | 1 | 4.41 |
| CHEMBL365026 | — | — | 1 | 4.34 |
| CHEMBL188343 | REVERSINE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL188967 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL188592 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL188958 | — | Ki | = | 2950.0 | nM | 5.53 |
| CHEMBL187458 | — | Ki | = | 4120.0 | nM | 5.38 |
| CHEMBL366216 | — | Ki | = | 6100.0 | nM | 5.21 |
| CHEMBL2113046 | — | Ki | = | 7730.0 | nM | 5.11 |
| CHEMBL191270 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL363419 | — | Ki | = | 16000.0 | nM | 4.80 |
| CHEMBL446698 | — | Ki | = | 39000.0 | nM | 4.41 |
| CHEMBL365026 | — | Ki | = | 46000.0 | nM | 4.34 |
| CHEMBL188343 | REVERSINE | Ki | > | 10000.0 | nM | - |