Assay Detail
Binding
CHEMBL3756023
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Displacement of [3H]DPCPX at human A1 receptor expressed in CHO cell membrane after 120 mins by scintillation counting method
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 | Autocuration |
Publication
Structural refinement of pyrazolo[4,3-d]pyrimidine derivatives to obtain highly potent and selective antagonists for the human A3 adenosine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 6.63 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3754656 | — | — | 1 | 7.28 |
| CHEMBL2322916 | — | — | 1 | 7.16 |
| CHEMBL2322917 | — | — | 1 | 7.12 |
| CHEMBL2322918 | — | — | 1 | 6.82 |
| CHEMBL3753083 | — | — | 1 | 6.67 |
| CHEMBL3753937 | — | — | 1 | 6.60 |
| CHEMBL3753291 | — | — | 1 | 6.40 |
| CHEMBL3752862 | — | — | 1 | 6.33 |
| CHEMBL3751978 | — | — | 1 | 6.26 |
| CHEMBL3753976 | — | — | 1 | 6.16 |
| CHEMBL3753642 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3754656 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL2322916 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL2322917 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL2322918 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL3753083 | — | Ki | = | 213.0 | nM | 6.67 |
| CHEMBL3753937 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL3753291 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL3752862 | — | Ki | = | 466.0 | nM | 6.33 |
| CHEMBL3751978 | — | Ki | = | 552.0 | nM | 6.26 |
| CHEMBL3753976 | — | Ki | = | 687.0 | nM | 6.16 |
| CHEMBL3753642 | — | Ki | = | 764.0 | nM | 6.12 |