Assay Detail
Functional
CHEMBL644471
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Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand.
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 6.63 | 7.78 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL16929 | — | — | 1 | 7.78 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | — | 1 | 7.74 |
| CHEMBL275605 | — | — | 1 | 7.62 |
| CHEMBL16677 | — | — | 1 | 7.59 |
| CHEMBL16931 | — | — | 1 | 7.41 |
| CHEMBL275360 | — | — | 1 | 7.41 |
| CHEMBL16534 | — | — | 1 | 7.23 |
| CHEMBL16787 | — | — | 1 | 7.16 |
| CHEMBL17002 | — | — | 1 | 6.95 |
| CHEMBL275427 | — | — | 1 | 6.73 |
| CHEMBL16997 | — | — | 1 | 6.72 |
| CHEMBL17294 | — | — | 1 | 6.65 |
| CHEMBL277386 | — | — | 1 | 6.62 |
| CHEMBL17341 | — | — | 1 | 6.37 |
| CHEMBL273807 | — | — | 1 | 6.30 |
| CHEMBL27041 | — | — | 1 | 6.22 |
| CHEMBL275149 | — | — | 1 | 6.19 |
| CHEMBL17103 | — | — | 1 | 5.82 |
| CHEMBL17003 | — | — | 1 | 5.79 |
| CHEMBL17173 | — | — | 1 | 5.71 |
| CHEMBL16724 | — | — | 1 | 5.62 |
| CHEMBL17123 | — | — | 1 | 5.59 |
| CHEMBL278039 | — | — | 1 | 5.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL16929 | — | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | Ki | = | 18.4 | nM | 7.74 |
| CHEMBL275605 | — | Ki | = | 23.8 | nM | 7.62 |
| CHEMBL16677 | — | Ki | = | 25.8 | nM | 7.59 |
| CHEMBL16931 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL275360 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL16534 | — | Ki | = | 58.9 | nM | 7.23 |
| CHEMBL16787 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL17002 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL275427 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL16997 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL17294 | — | Ki | = | 223.0 | nM | 6.65 |
| CHEMBL277386 | — | Ki | = | 238.0 | nM | 6.62 |
| CHEMBL17341 | — | Ki | = | 431.0 | nM | 6.37 |
| CHEMBL273807 | — | Ki | = | 503.0 | nM | 6.30 |
| CHEMBL27041 | — | Ki | = | 595.0 | nM | 6.22 |
| CHEMBL275149 | — | Ki | = | 642.0 | nM | 6.19 |
| CHEMBL17103 | — | Ki | = | 1518.0 | nM | 5.82 |
| CHEMBL17003 | — | Ki | = | 1640.0 | nM | 5.79 |
| CHEMBL17173 | — | Ki | = | 1970.0 | nM | 5.71 |
| CHEMBL16724 | — | Ki | = | 2370.0 | nM | 5.62 |
| CHEMBL17123 | — | Ki | = | 2540.0 | nM | 5.59 |
| CHEMBL278039 | — | Ki | = | 5140.0 | nM | 5.29 |