Assay Detail
Functional
CHEMBL4018970
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Antagonist activity at human adenosine A3 receptor expressed in CHO cell membranes assessed as inhibition of 2-Cl-IB-MECA-induced [35S]GTPgammaS binding measured after 30 mins
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-Affinity Relationships and Structure-Kinetics Relationships of Pyrido[2,1-f]purine-2,4-dione Derivatives as Human Adenosine A3 Receptor Antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 2 | 8.05 | 8.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4062581 | — | — | 1 | 8.90 |
| CHEMBL322968 | — | — | 1 | 7.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4062581 | — | Kd | = | 1.259 | nM | 8.90 |
| CHEMBL322968 | — | Kd | = | 63.1 | nM | 7.20 |