Assay Detail
Binding
CHEMBL931045
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Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells
22
Total Activities
22
Compounds Tested
2
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
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-N,N-dialkyluronamides as human A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | - | - |
| Ki | 7 | 6.18 | 6.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL200732 | — | — | 1 | 6.71 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 6.65 |
| CHEMBL255596 | — | — | 1 | 6.62 |
| CHEMBL255809 | — | — | 1 | 6.46 |
| CHEMBL255975 | — | — | 1 | 6.39 |
| CHEMBL373065 | — | — | 1 | 5.23 |
| CHEMBL436485 | — | — | 1 | 5.21 |
| CHEMBL272550 | — | — | 1 | - |
| CHEMBL271730 | — | — | 1 | - |
| CHEMBL271732 | — | — | 1 | - |
| CHEMBL404235 | — | — | 1 | - |
| CHEMBL428245 | — | — | 1 | - |
| CHEMBL272155 | — | — | 1 | - |
| CHEMBL406911 | — | — | 1 | - |
| CHEMBL272368 | — | — | 1 | - |
| CHEMBL403584 | — | — | 1 | - |
| CHEMBL255597 | — | — | 1 | - |
| CHEMBL256185 | — | — | 1 | - |
| CHEMBL255976 | — | — | 1 | - |
| CHEMBL271684 | — | — | 1 | - |
| CHEMBL271686 | — | — | 1 | - |
| CHEMBL271685 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL200732 | — | Ki | = | 193.0 | nM | 6.71 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 222.0 | nM | 6.65 |
| CHEMBL255596 | — | Ki | = | 237.0 | nM | 6.62 |
| CHEMBL255809 | — | Ki | = | 345.0 | nM | 6.46 |
| CHEMBL255975 | — | Ki | = | 404.0 | nM | 6.39 |
| CHEMBL373065 | — | Ki | = | 5870.0 | nM | 5.23 |
| CHEMBL436485 | — | Ki | = | 6220.0 | nM | 5.21 |
| CHEMBL272550 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL271730 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL271732 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL404235 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL428245 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL272155 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL406911 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL272368 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL403584 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL255597 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL256185 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL255976 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL271684 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL271686 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL271685 | — | IC50 | >= | 10000.0 | nM | - |