Assay Detail
Binding
CHEMBL4263212
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Displacement of [3H]NECA from recombinant human adenosine A3 receptor expressed in CHO cell membranes measured after 180 mins
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
Studies on enantioselectivity of chiral 4-acetylamino-6-alkyloxy-2-alkylthiopyrimidines acting as antagonists of the human A<sub>3</sub> adenosine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.47 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 9.70 |
| CHEMBL4282074 | — | — | 1 | 9.30 |
| CHEMBL4277994 | — | — | 1 | 9.22 |
| CHEMBL4285922 | — | — | 1 | 8.77 |
| CHEMBL464859 | NECA | — | 1 | 7.12 |
| CHEMBL4285494 | — | — | 1 | 6.74 |
| CHEMBL4288869 | — | — | 1 | 6.71 |
| CHEMBL4289256 | — | — | 1 | 6.36 |
| CHEMBL4292670 | — | — | 1 | 6.24 |
| CHEMBL4278607 | — | — | 1 | 6.13 |
| CHEMBL4283891 | — | — | 1 | 5.86 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL431733 | NAMODENOSON | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL4282074 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL4277994 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL4285922 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL464859 | NECA | Ki | = | 75.5 | nM | 7.12 |
| CHEMBL4285494 | — | Ki | = | 183.2 | nM | 6.74 |
| CHEMBL4288869 | — | Ki | = | 195.1 | nM | 6.71 |
| CHEMBL4289256 | — | Ki | = | 440.2 | nM | 6.36 |
| CHEMBL4292670 | — | Ki | = | 580.1 | nM | 6.24 |
| CHEMBL4278607 | — | Ki | = | 737.5 | nM | 6.13 |
| CHEMBL4283891 | — | Ki | = | 1390.0 | nM | 5.86 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | > | 1000.0 | nM | - |