Assay Detail
Binding
CHEMBL976199
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Displacement of [3H]ZM241385 from human recombinant adenosine A2A receptor expressed in HeLa cells by beta scintillation counter
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
1,3-dialkyl-8-N-substituted benzyloxycarbonylamino-9-deazaxanthines as potent adenosine receptor ligands: Design, synthesis, structure-affinity and structure-selectivity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.08 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL466453 | — | — | 1 | 8.00 |
| CHEMBL513681 | — | — | 1 | 7.98 |
| CHEMBL468295 | — | — | 1 | 7.82 |
| CHEMBL468506 | — | — | 1 | 7.74 |
| CHEMBL466035 | — | — | 1 | 7.66 |
| CHEMBL452454 | — | — | 1 | 7.55 |
| CHEMBL466021 | — | — | 1 | 7.54 |
| CHEMBL512290 | — | — | 1 | 7.46 |
| CHEMBL467271 | — | — | 1 | 7.45 |
| CHEMBL469136 | — | — | 1 | 7.36 |
| CHEMBL466828 | — | — | 1 | 7.30 |
| CHEMBL469119 | — | — | 1 | 7.14 |
| CHEMBL512276 | — | — | 1 | 6.93 |
| CHEMBL513135 | — | — | 1 | 6.88 |
| CHEMBL466652 | — | — | 1 | 6.35 |
| CHEMBL468296 | — | — | 1 | 6.31 |
| CHEMBL511714 | — | — | 1 | 6.00 |
| CHEMBL467270 | — | — | 1 | 5.65 |
| CHEMBL468306 | — | — | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL466453 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL513681 | — | Ki | = | 10.5 | nM | 7.98 |
| CHEMBL468295 | — | Ki | = | 15.1 | nM | 7.82 |
| CHEMBL468506 | — | Ki | = | 18.2 | nM | 7.74 |
| CHEMBL466035 | — | Ki | = | 21.9 | nM | 7.66 |
| CHEMBL452454 | — | Ki | = | 28.2 | nM | 7.55 |
| CHEMBL466021 | — | Ki | = | 28.8 | nM | 7.54 |
| CHEMBL512290 | — | Ki | = | 34.7 | nM | 7.46 |
| CHEMBL467271 | — | Ki | = | 35.5 | nM | 7.45 |
| CHEMBL469136 | — | Ki | = | 43.7 | nM | 7.36 |
| CHEMBL466828 | — | Ki | = | 50.1 | nM | 7.30 |
| CHEMBL469119 | — | Ki | = | 72.4 | nM | 7.14 |
| CHEMBL512276 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL513135 | — | Ki | = | 132.0 | nM | 6.88 |
| CHEMBL466652 | — | Ki | = | 447.0 | nM | 6.35 |
| CHEMBL468296 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL511714 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL467270 | — | Ki | = | 2240.0 | nM | 5.65 |
| CHEMBL468306 | — | Ki | = | 3311.0 | nM | 5.48 |