Assay Detail
Functional
CHEMBL951866
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Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as reversal of NECA-mediated inhibition of forskolin-induced cAMP accumulation
4
Total Activities
4
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
Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.56 | 8.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429131 | — | — | 1 | 8.90 |
| CHEMBL272795 | — | — | 1 | 8.73 |
| CHEMBL402848 | — | — | 1 | 8.57 |
| CHEMBL270676 | — | — | 1 | 8.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429131 | — | IC50 | = | 1.25 | nM | 8.90 |
| CHEMBL272795 | — | IC50 | = | 1.84 | nM | 8.73 |
| CHEMBL402848 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL270676 | — | IC50 | = | 9.2 | nM | 8.04 |