Assay Detail
Binding
CHEMBL3413619
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Displacement of [125I]I-AB-MECA from mouse A3 adenosine receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
In vivo phenotypic screening for treating chronic neuropathic pain: modification of C2-arylethynyl group of conformationally constrained A3 adenosine receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 7.33 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2064657 | — | — | 1 | 8.51 |
| CHEMBL3407784 | — | — | 1 | 7.44 |
| CHEMBL2064640 | — | — | 1 | 7.43 |
| CHEMBL2064639 | — | — | 1 | 7.42 |
| CHEMBL3407788 | — | — | 1 | 7.39 |
| CHEMBL3407783 | — | — | 1 | 7.37 |
| CHEMBL3407776 | — | — | 1 | 7.30 |
| CHEMBL3407778 | — | — | 1 | 7.27 |
| CHEMBL2064636 | — | — | 1 | 7.24 |
| CHEMBL3407773 | — | — | 1 | 7.19 |
| CHEMBL3407774 | — | — | 1 | 7.17 |
| CHEMBL2064645 | — | — | 1 | 7.07 |
| CHEMBL3407775 | — | — | 1 | 6.95 |
| CHEMBL3407777 | — | — | 1 | 6.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2064657 | — | Ki | = | 3.08 | nM | 8.51 |
| CHEMBL3407784 | — | Ki | = | 36.1 | nM | 7.44 |
| CHEMBL2064640 | — | Ki | = | 37.2 | nM | 7.43 |
| CHEMBL2064639 | — | Ki | = | 37.7 | nM | 7.42 |
| CHEMBL3407788 | — | Ki | = | 40.9 | nM | 7.39 |
| CHEMBL3407783 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL3407776 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL3407778 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL2064636 | — | Ki | = | 58.2 | nM | 7.24 |
| CHEMBL3407773 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL3407774 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL2064645 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL3407775 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL3407777 | — | Ki | = | 126.0 | nM | 6.90 |