Assay Detail
Binding
CHEMBL950993
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Displacement of [3H]DPDPX from human adenosine A1 receptor expressed in CHO cells
19
Total Activities
19
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
Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.38 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL198008 | — | — | 1 | 9.30 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 9.30 |
| CHEMBL464859 | NECA | — | 1 | 7.85 |
| CHEMBL200636 | — | — | 1 | 7.30 |
| CHEMBL429435 | — | — | 1 | 6.31 |
| CHEMBL257256 | — | — | 1 | 6.24 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 6.05 |
| CHEMBL271753 | — | — | 1 | 5.83 |
| CHEMBL271106 | — | — | 1 | 5.74 |
| CHEMBL429131 | — | — | 1 | 5.68 |
| CHEMBL257487 | — | — | 1 | 5.61 |
| CHEMBL402848 | — | — | 1 | 5.61 |
| CHEMBL403521 | — | — | 1 | 5.48 |
| CHEMBL272795 | — | — | 1 | 5.35 |
| CHEMBL272596 | — | — | 1 | 5.26 |
| CHEMBL198779 | — | — | 1 | 5.10 |
| CHEMBL200480 | — | — | 1 | - |
| CHEMBL445664 | — | — | 1 | - |
| CHEMBL260311 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL198008 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL464859 | NECA | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL200636 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL429435 | — | Ki | = | 486.0 | nM | 6.31 |
| CHEMBL257256 | — | Ki | = | 582.0 | nM | 6.24 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 890.0 | nM | 6.05 |
| CHEMBL271753 | — | Ki | = | 1462.0 | nM | 5.83 |
| CHEMBL271106 | — | Ki | = | 1840.0 | nM | 5.74 |
| CHEMBL429131 | — | Ki | = | 2080.0 | nM | 5.68 |
| CHEMBL257487 | — | Ki | = | 2445.0 | nM | 5.61 |
| CHEMBL402848 | — | Ki | = | 2443.0 | nM | 5.61 |
| CHEMBL403521 | — | Ki | = | 3336.0 | nM | 5.48 |
| CHEMBL272795 | — | Ki | = | 4480.0 | nM | 5.35 |
| CHEMBL272596 | — | Ki | = | 5474.0 | nM | 5.26 |
| CHEMBL198779 | — | Ki | = | 8000.0 | nM | 5.10 |
| CHEMBL200480 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL445664 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL260311 | — | Ki | > | 10000.0 | nM | - |