Assay Detail
Binding
CHEMBL644953
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Binding affinity against human recombinant Adenosine A3 receptor stably expressed in HEK293 cells by displacing [125I]AB-MECA radioligand
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 6.35 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1625681 | — | — | 1 | 8.64 |
| CHEMBL1788234 | — | — | 1 | 8.01 |
| CHEMBL117962 | — | — | 1 | 7.33 |
| CHEMBL1788230 | — | — | 1 | 6.19 |
| CHEMBL2112561 | — | — | 1 | 5.77 |
| CHEMBL117899 | — | — | 1 | 5.48 |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | 4.88 |
| CHEMBL2111766 | — | — | 1 | 4.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1625681 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL1788234 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL117962 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL1788230 | — | Ki | = | 640.0 | nM | 6.19 |
| CHEMBL2112561 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL117899 | — | Ki | = | 3330.0 | nM | 5.48 |
| CHEMBL113 | CAFFEINE | Ki | = | 13300.0 | nM | 4.88 |
| CHEMBL2111766 | — | Ki | = | 30600.0 | nM | 4.51 |