Assay Detail
Functional
CHEMBL646441
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Antagonist activity against human adenosine A3 receptor expressed in HEK cells in presence of [125]IAB-MECA or [125I]IABA radioligand.
25
Total Activities
25
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 | 25 | 6.55 | 7.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273094 | XANTHINE AMINE CONGENER | — | 1 | 7.59 |
| CHEMBL16997 | — | — | 1 | 7.52 |
| CHEMBL17294 | — | — | 1 | 7.51 |
| CHEMBL17341 | — | — | 1 | 7.21 |
| CHEMBL275605 | — | — | 1 | 7.10 |
| CHEMBL17202 | — | — | 1 | 6.92 |
| CHEMBL16677 | — | — | 1 | 6.86 |
| CHEMBL16787 | — | — | 1 | 6.86 |
| CHEMBL277386 | — | — | 1 | 6.67 |
| CHEMBL27081 | — | — | 1 | 6.64 |
| CHEMBL17002 | — | — | 1 | 6.64 |
| CHEMBL275149 | — | — | 1 | 6.55 |
| CHEMBL16534 | — | — | 1 | 6.45 |
| CHEMBL16741 | — | — | 1 | 6.44 |
| CHEMBL16929 | — | — | 1 | 6.41 |
| CHEMBL273807 | — | — | 1 | 6.24 |
| CHEMBL17173 | — | — | 1 | 6.17 |
| CHEMBL16724 | — | — | 1 | 6.09 |
| CHEMBL17103 | — | — | 1 | 6.04 |
| CHEMBL278039 | — | — | 1 | 5.90 |
| CHEMBL275427 | — | — | 1 | 5.73 |
| CHEMBL17003 | — | — | 1 | 5.64 |
| CHEMBL27041 | — | — | 1 | 5.41 |
| CHEMBL275360 | — | — | 1 | - |
| CHEMBL16931 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273094 | XANTHINE AMINE CONGENER | Ki | = | 25.6 | nM | 7.59 |
| CHEMBL16997 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL17294 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL17341 | — | Ki | = | 61.9 | nM | 7.21 |
| CHEMBL275605 | — | Ki | = | 79.2 | nM | 7.10 |
| CHEMBL17202 | — | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL16677 | — | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL16787 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL277386 | — | Ki | = | 213.0 | nM | 6.67 |
| CHEMBL27081 | — | Ki | = | 227.0 | nM | 6.64 |
| CHEMBL17002 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL275149 | — | Ki | = | 284.0 | nM | 6.55 |
| CHEMBL16534 | — | Ki | = | 352.0 | nM | 6.45 |
| CHEMBL16741 | — | Ki | = | 363.0 | nM | 6.44 |
| CHEMBL16929 | — | Ki | = | 391.0 | nM | 6.41 |
| CHEMBL273807 | — | Ki | = | 570.0 | nM | 6.24 |
| CHEMBL17173 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL16724 | — | Ki | = | 816.0 | nM | 6.09 |
| CHEMBL17103 | — | Ki | = | 922.0 | nM | 6.04 |
| CHEMBL278039 | — | Ki | = | 1270.0 | nM | 5.90 |
| CHEMBL275427 | — | Ki | = | 1870.0 | nM | 5.73 |
| CHEMBL17003 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL27041 | — | Ki | = | 3910.0 | nM | 5.41 |
| CHEMBL275360 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL16931 | — | Ki | > | 5000.0 | nM | - |