Assay Detail
Binding
CHEMBL2024728
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Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting
12
Total Activities
12
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
Discovery of 1,2,4-triazine derivatives as adenosine A(2A) antagonists using structure based drug design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.26 | 9.79 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2024114 | — | — | 1 | 9.79 |
| CHEMBL2021950 | — | — | 1 | 7.78 |
| CHEMBL2024119 | — | — | 1 | 7.50 |
| CHEMBL2024112 | — | — | 1 | 7.36 |
| CHEMBL2024111 | — | — | 1 | 7.25 |
| CHEMBL2024115 | — | — | 1 | 7.07 |
| CHEMBL2024118 | — | — | 1 | 6.96 |
| CHEMBL2024120 | — | — | 1 | 6.93 |
| CHEMBL2024117 | — | — | 1 | 6.77 |
| CHEMBL2024113 | — | — | 1 | 6.71 |
| CHEMBL1370747 | — | — | 1 | 6.56 |
| CHEMBL2024116 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2024114 | — | Ki | = | 0.1622 | nM | 9.79 |
| CHEMBL2021950 | — | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL2024119 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL2024112 | — | Ki | = | 43.65 | nM | 7.36 |
| CHEMBL2024111 | — | Ki | = | 56.23 | nM | 7.25 |
| CHEMBL2024115 | — | Ki | = | 85.11 | nM | 7.07 |
| CHEMBL2024118 | — | Ki | = | 109.65 | nM | 6.96 |
| CHEMBL2024120 | — | Ki | = | 117.49 | nM | 6.93 |
| CHEMBL2024117 | — | Ki | = | 169.82 | nM | 6.77 |
| CHEMBL2024113 | — | Ki | = | 194.98 | nM | 6.71 |
| CHEMBL1370747 | — | Ki | = | 275.42 | nM | 6.56 |
| CHEMBL2024116 | — | Ki | = | 398.11 | nM | 6.40 |