Assay Detail
Functional
CHEMBL1769841
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Antagonist activity at human cloned adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation after 15 mins
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| IC50 | 5 | 8.02 | 8.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1766359 | — | — | 1 | 8.94 |
| CHEMBL1766358 | — | — | 1 | 8.08 |
| CHEMBL1766354 | — | — | 1 | 7.77 |
| CHEMBL1766353 | — | — | 1 | 7.75 |
| CHEMBL1766352 | — | — | 1 | 7.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1766359 | — | IC50 | = | 1.15 | nM | 8.94 |
| CHEMBL1766358 | — | IC50 | = | 8.25 | nM | 8.08 |
| CHEMBL1766354 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1766353 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1766352 | — | IC50 | = | 28.0 | nM | 7.55 |