Assay Detail
Binding
CHEMBL931047
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Displacement of [3H]ABMECA from human adenosine A3 receptor expressed in CHO cells
22
Total Activities
22
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
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 |
|---|---|---|---|
| Ki | 22 | 7.05 | 9.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL200732 | — | — | 1 | 9.42 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 8.85 |
| CHEMBL271686 | — | — | 1 | 8.03 |
| CHEMBL436485 | — | — | 1 | 7.81 |
| CHEMBL271685 | — | — | 1 | 7.67 |
| CHEMBL373065 | — | — | 1 | 7.54 |
| CHEMBL255975 | — | — | 1 | 7.51 |
| CHEMBL428245 | — | — | 1 | 7.36 |
| CHEMBL256185 | — | — | 1 | 6.96 |
| CHEMBL255809 | — | — | 1 | 6.94 |
| CHEMBL404235 | — | — | 1 | 6.93 |
| CHEMBL272550 | — | — | 1 | 6.92 |
| CHEMBL255596 | — | — | 1 | 6.90 |
| CHEMBL271684 | — | — | 1 | 6.87 |
| CHEMBL272368 | — | — | 1 | 6.40 |
| CHEMBL255976 | — | — | 1 | 6.37 |
| CHEMBL406911 | — | — | 1 | 6.25 |
| CHEMBL272155 | — | — | 1 | 6.18 |
| CHEMBL403584 | — | — | 1 | 6.14 |
| CHEMBL255597 | — | — | 1 | 6.08 |
| CHEMBL271730 | — | — | 1 | 6.06 |
| CHEMBL271732 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL200732 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL271686 | — | Ki | = | 9.32 | nM | 8.03 |
| CHEMBL436485 | — | Ki | = | 15.5 | nM | 7.81 |
| CHEMBL271685 | — | Ki | = | 21.3 | nM | 7.67 |
| CHEMBL373065 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL255975 | — | Ki | = | 30.7 | nM | 7.51 |
| CHEMBL428245 | — | Ki | = | 43.4 | nM | 7.36 |
| CHEMBL256185 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL255809 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL404235 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL272550 | — | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL255596 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL271684 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL272368 | — | Ki | = | 398.0 | nM | 6.40 |
| CHEMBL255976 | — | Ki | = | 425.0 | nM | 6.37 |
| CHEMBL406911 | — | Ki | = | 565.0 | nM | 6.25 |
| CHEMBL272155 | — | Ki | = | 667.0 | nM | 6.18 |
| CHEMBL403584 | — | Ki | = | 727.0 | nM | 6.14 |
| CHEMBL255597 | — | Ki | = | 837.0 | nM | 6.08 |
| CHEMBL271730 | — | Ki | = | 867.0 | nM | 6.06 |
| CHEMBL271732 | — | Ki | = | 1530.0 | nM | 5.82 |