Assay Detail
Binding
CHEMBL976198
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Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 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 | HEK293 |
| 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 | 7.95 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL513681 | — | — | 1 | 9.10 |
| CHEMBL466035 | — | — | 1 | 8.77 |
| CHEMBL512276 | — | — | 1 | 8.70 |
| CHEMBL469136 | — | — | 1 | 8.68 |
| CHEMBL512290 | — | — | 1 | 8.55 |
| CHEMBL468506 | — | — | 1 | 8.49 |
| CHEMBL466453 | — | — | 1 | 8.23 |
| CHEMBL466021 | — | — | 1 | 8.15 |
| CHEMBL467271 | — | — | 1 | 8.11 |
| CHEMBL469119 | — | — | 1 | 8.02 |
| CHEMBL468295 | — | — | 1 | 8.00 |
| CHEMBL513135 | — | — | 1 | 7.94 |
| CHEMBL468920 | — | — | 1 | 7.86 |
| CHEMBL511714 | — | — | 1 | 7.79 |
| CHEMBL452454 | — | — | 1 | 7.62 |
| CHEMBL466828 | — | — | 1 | 7.37 |
| CHEMBL468296 | — | — | 1 | 7.09 |
| CHEMBL468306 | — | — | 1 | 6.30 |
| CHEMBL467270 | — | — | 1 | 6.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL513681 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL466035 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL512276 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL469136 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL512290 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL468506 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL466453 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL466021 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL467271 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL469119 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL468295 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL513135 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL468920 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL511714 | — | Ki | = | 16.2 | nM | 7.79 |
| CHEMBL452454 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL466828 | — | Ki | = | 42.7 | nM | 7.37 |
| CHEMBL468296 | — | Ki | = | 81.3 | nM | 7.09 |
| CHEMBL468306 | — | Ki | = | 501.0 | nM | 6.30 |
| CHEMBL467270 | — | Ki | = | 602.0 | nM | 6.22 |