Assay Detail
Binding
CHEMBL1286671
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Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO-A1 cells after 60 mins
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-A1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as selective human A(1) adenosine receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 6.65 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 8.49 |
| CHEMBL1277025 | — | — | 1 | 7.99 |
| CHEMBL1277116 | — | — | 1 | 7.94 |
| CHEMBL1277925 | — | — | 1 | 7.55 |
| CHEMBL1277845 | — | — | 1 | 7.36 |
| CHEMBL1278010 | — | — | 1 | 7.32 |
| CHEMBL1277846 | — | — | 1 | 7.14 |
| CHEMBL1278102 | — | — | 1 | 7.07 |
| CHEMBL1276939 | — | — | 1 | 7.03 |
| CHEMBL213425 | — | — | 1 | 6.98 |
| CHEMBL1276938 | — | — | 1 | 6.91 |
| CHEMBL1278011 | — | — | 1 | 6.74 |
| CHEMBL1277926 | — | — | 1 | 6.72 |
| CHEMBL1277024 | — | — | 1 | 6.72 |
| CHEMBL1276852 | — | — | 1 | 6.60 |
| CHEMBL1278104 | — | — | 1 | 6.57 |
| CHEMBL1278194 | — | — | 1 | 6.32 |
| CHEMBL1277480 | — | — | 1 | 6.25 |
| CHEMBL1276851 | — | — | 1 | 5.84 |
| CHEMBL1277302 | — | — | 1 | 5.80 |
| CHEMBL1276853 | — | — | 1 | 5.79 |
| CHEMBL1277301 | — | — | 1 | 5.62 |
| CHEMBL1277390 | — | — | 1 | 5.61 |
| CHEMBL1277207 | — | — | 1 | 5.51 |
| CHEMBL1277667 | — | — | 1 | 5.49 |
| CHEMBL382494 | — | — | 1 | 5.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL1277025 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL1277116 | — | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL1277925 | — | Ki | = | 28.3 | nM | 7.55 |
| CHEMBL1277845 | — | Ki | = | 43.6 | nM | 7.36 |
| CHEMBL1278010 | — | Ki | = | 47.4 | nM | 7.32 |
| CHEMBL1277846 | — | Ki | = | 71.8 | nM | 7.14 |
| CHEMBL1278102 | — | Ki | = | 85.3 | nM | 7.07 |
| CHEMBL1276939 | — | Ki | = | 92.7 | nM | 7.03 |
| CHEMBL213425 | — | Ki | = | 104.3 | nM | 6.98 |
| CHEMBL1276938 | — | Ki | = | 122.9 | nM | 6.91 |
| CHEMBL1278011 | — | Ki | = | 180.2 | nM | 6.74 |
| CHEMBL1277926 | — | Ki | = | 192.3 | nM | 6.72 |
| CHEMBL1277024 | — | Ki | = | 188.5 | nM | 6.72 |
| CHEMBL1276852 | — | Ki | = | 252.3 | nM | 6.60 |
| CHEMBL1278104 | — | Ki | = | 267.4 | nM | 6.57 |
| CHEMBL1278194 | — | Ki | = | 475.2 | nM | 6.32 |
| CHEMBL1277480 | — | Ki | = | 563.5 | nM | 6.25 |
| CHEMBL1276851 | — | Ki | = | 1432.0 | nM | 5.84 |
| CHEMBL1277302 | — | Ki | = | 1595.0 | nM | 5.80 |
| CHEMBL1276853 | — | Ki | = | 1616.0 | nM | 5.79 |
| CHEMBL1277301 | — | Ki | = | 2385.0 | nM | 5.62 |
| CHEMBL1277390 | — | Ki | = | 2445.0 | nM | 5.61 |
| CHEMBL1277207 | — | Ki | = | 3080.0 | nM | 5.51 |
| CHEMBL1277667 | — | Ki | = | 3245.0 | nM | 5.49 |
| CHEMBL382494 | — | Ki | = | 3250.0 | nM | 5.49 |