Assay Detail
Binding
CHEMBL950995
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Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells
27
Total Activities
27
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 | 27 | 7.54 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 9.66 |
| CHEMBL429131 | — | — | 1 | 8.85 |
| CHEMBL402848 | — | — | 1 | 8.74 |
| CHEMBL272795 | — | — | 1 | 8.70 |
| CHEMBL270676 | — | — | 1 | 8.46 |
| CHEMBL271106 | — | — | 1 | 8.20 |
| CHEMBL257256 | — | — | 1 | 8.15 |
| CHEMBL257487 | — | — | 1 | 8.12 |
| CHEMBL272582 | — | — | 1 | 8.07 |
| CHEMBL256643 | — | — | 1 | 7.66 |
| CHEMBL272596 | — | — | 1 | 7.58 |
| CHEMBL198779 | — | — | 1 | 7.58 |
| CHEMBL406567 | — | — | 1 | 7.52 |
| CHEMBL272174 | — | — | 1 | 7.51 |
| CHEMBL271753 | — | — | 1 | 7.42 |
| CHEMBL406727 | — | — | 1 | 7.35 |
| CHEMBL464859 | NECA | — | 1 | 7.14 |
| CHEMBL403521 | — | — | 1 | 6.90 |
| CHEMBL200480 | — | — | 1 | 6.89 |
| CHEMBL405824 | — | — | 1 | 6.78 |
| CHEMBL429435 | — | — | 1 | 6.56 |
| CHEMBL445664 | — | — | 1 | 6.36 |
| CHEMBL257298 | — | — | 1 | 6.28 |
| CHEMBL200636 | — | — | 1 | 6.12 |
| CHEMBL198008 | — | — | 1 | 6.02 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | - |
| CHEMBL260311 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL431733 | NAMODENOSON | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL429131 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL402848 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL272795 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL270676 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL271106 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL257256 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL257487 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL272582 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL256643 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL272596 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL198779 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL406567 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL272174 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL271753 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL406727 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL464859 | NECA | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL403521 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL200480 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL405824 | — | Ki | = | 166.0 | nM | 6.78 |
| CHEMBL429435 | — | Ki | = | 276.0 | nM | 6.56 |
| CHEMBL445664 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL257298 | — | Ki | = | 525.0 | nM | 6.28 |
| CHEMBL200636 | — | Ki | = | 763.0 | nM | 6.12 |
| CHEMBL198008 | — | Ki | = | 955.0 | nM | 6.02 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | > | 1000.0 | nM | - |
| CHEMBL260311 | — | Ki | > | 1000.0 | nM | - |