Assay Detail
Functional
CHEMBL2384074
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Antagonist activity at human adenosine A1 receptor assessed as cAMP level by cell based assay
5
Total Activities
5
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
Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 6.35 | 8.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273094 | XANTHINE AMINE CONGENER | — | 1 | 8.08 |
| CHEMBL197669 | ST1535 | 1.0 | 1 | 7.14 |
| CHEMBL113142 | ZM-241385 | — | 1 | 6.11 |
| CHEMBL431770 | ISTRADEFYLLINE | 4.0 | 1 | 6.08 |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | 4.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273094 | XANTHINE AMINE CONGENER | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL197669 | ST1535 | Ki | = | 71.8 | nM | 7.14 |
| CHEMBL113142 | ZM-241385 | Ki | = | 774.0 | nM | 6.11 |
| CHEMBL431770 | ISTRADEFYLLINE | Ki | = | 841.0 | nM | 6.08 |
| CHEMBL113 | CAFFEINE | Ki | = | 44000.0 | nM | 4.36 |