Assay Detail
Binding
CHEMBL1769839
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Displacement of [125I]AB-MECA from human cloned adenosine A3 receptor expressed in CHO cells
10
Total Activities
10
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
The identification of the 2-phenylphthalazin-1(2H)-one scaffold as a new decorable core skeleton for the design of potent and selective human A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.21 | 9.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1766358 | — | — | 1 | 9.11 |
| CHEMBL1766354 | — | — | 1 | 8.05 |
| CHEMBL1766353 | — | — | 1 | 8.01 |
| CHEMBL1766359 | — | — | 1 | 7.53 |
| CHEMBL1766352 | — | — | 1 | 7.22 |
| CHEMBL1766271 | — | — | 1 | 6.75 |
| CHEMBL1766360 | — | — | 1 | 6.56 |
| CHEMBL16254 | — | — | 1 | 6.56 |
| CHEMBL278197 | — | — | 1 | 6.31 |
| CHEMBL1766267 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1766358 | — | Ki | = | 0.776 | nM | 9.11 |
| CHEMBL1766354 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL1766353 | — | Ki | = | 9.75 | nM | 8.01 |
| CHEMBL1766359 | — | Ki | = | 29.6 | nM | 7.53 |
| CHEMBL1766352 | — | Ki | = | 60.6 | nM | 7.22 |
| CHEMBL1766271 | — | Ki | = | 178.4 | nM | 6.75 |
| CHEMBL1766360 | — | Ki | = | 274.2 | nM | 6.56 |
| CHEMBL16254 | — | Ki | = | 276.0 | nM | 6.56 |
| CHEMBL278197 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL1766267 | — | Ki | = | 1100.0 | nM | 5.96 |