Assay Detail
Functional
CHEMBL642193
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against adenosine A1 receptor in rat brain membrane in presence of [3H]R-PIA radioligand.
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Brain |
| Subcellular | Membrane |
| 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 | 36 | 7.45 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273094 | XANTHINE AMINE CONGENER | — | 1 | 8.92 |
| CHEMBL17294 | — | — | 1 | 8.40 |
| CHEMBL16677 | — | — | 1 | 8.38 |
| CHEMBL275605 | — | — | 1 | 8.30 |
| CHEMBL444281 | — | — | 1 | 8.23 |
| CHEMBL275427 | — | — | 1 | 8.20 |
| CHEMBL17003 | — | — | 1 | 8.13 |
| CHEMBL17202 | — | — | 1 | 8.12 |
| CHEMBL275360 | — | — | 1 | 7.99 |
| CHEMBL17173 | — | — | 1 | 7.96 |
| CHEMBL16787 | — | — | 1 | 7.88 |
| CHEMBL16997 | — | — | 1 | 7.82 |
| CHEMBL278039 | — | — | 1 | 7.80 |
| CHEMBL273807 | — | — | 1 | 7.78 |
| CHEMBL432664 | — | — | 1 | 7.76 |
| CHEMBL27043 | — | — | 1 | 7.70 |
| CHEMBL17167 | — | — | 1 | 7.61 |
| CHEMBL16984 | — | — | 1 | 7.57 |
| CHEMBL17341 | — | — | 1 | 7.55 |
| CHEMBL17002 | — | — | 1 | 7.42 |
| CHEMBL16741 | — | — | 1 | 7.42 |
| CHEMBL17123 | — | — | 1 | 7.37 |
| CHEMBL277386 | — | — | 1 | 7.35 |
| CHEMBL27041 | — | — | 1 | 7.24 |
| CHEMBL17141 | — | — | 1 | 7.19 |
| CHEMBL17299 | — | — | 1 | 6.92 |
| CHEMBL16931 | — | — | 1 | 6.84 |
| CHEMBL27081 | — | — | 1 | 6.82 |
| CHEMBL275149 | — | — | 1 | 6.78 |
| CHEMBL16908 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273094 | XANTHINE AMINE CONGENER | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL17294 | — | Ki | = | 3.94 | nM | 8.40 |
| CHEMBL16677 | — | Ki | = | 4.22 | nM | 8.38 |
| CHEMBL275605 | — | Ki | = | 5.02 | nM | 8.30 |
| CHEMBL444281 | — | Ki | = | 5.88 | nM | 8.23 |
| CHEMBL275427 | — | Ki | = | 6.35 | nM | 8.20 |
| CHEMBL17003 | — | Ki | = | 7.46 | nM | 8.13 |
| CHEMBL17202 | — | Ki | = | 7.67 | nM | 8.12 |
| CHEMBL275360 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL17173 | — | Ki | = | 11.1 | nM | 7.96 |
| CHEMBL16787 | — | Ki | = | 13.1 | nM | 7.88 |
| CHEMBL16997 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL278039 | — | Ki | = | 15.7 | nM | 7.80 |
| CHEMBL273807 | — | Ki | = | 16.8 | nM | 7.78 |
| CHEMBL432664 | — | Ki | = | 17.5 | nM | 7.76 |
| CHEMBL27043 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL17167 | — | Ki | = | 24.8 | nM | 7.61 |
| CHEMBL16984 | — | Ki | = | 26.8 | nM | 7.57 |
| CHEMBL17341 | — | Ki | = | 27.9 | nM | 7.55 |
| CHEMBL16741 | — | Ki | = | 38.4 | nM | 7.42 |
| CHEMBL17002 | — | Ki | = | 37.6 | nM | 7.42 |
| CHEMBL17123 | — | Ki | = | 43.1 | nM | 7.37 |
| CHEMBL277386 | — | Ki | = | 44.6 | nM | 7.35 |
| CHEMBL27041 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL17141 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL17299 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL16931 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL27081 | — | Ki | = | 153.0 | nM | 6.82 |
| CHEMBL275149 | — | Ki | = | 167.0 | nM | 6.78 |
| CHEMBL16908 | — | Ki | = | 201.0 | nM | 6.70 |
| CHEMBL275606 | — | Ki | = | 218.0 | nM | 6.66 |
| CHEMBL16929 | — | Ki | = | 272.0 | nM | 6.57 |
| CHEMBL16534 | — | Ki | = | 439.0 | nM | 6.36 |
| CHEMBL17103 | — | Ki | = | 602.0 | nM | 6.22 |
| CHEMBL417812 | — | Ki | = | 679.0 | nM | 6.17 |
| CHEMBL16724 | — | Ki | = | 756.0 | nM | 6.12 |