Assay Detail
Functional
CHEMBL641306
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand.
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Striatum |
| 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 | 35 | 6.42 | 7.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL275605 | — | — | 1 | 7.59 |
| CHEMBL16677 | — | — | 1 | 7.34 |
| CHEMBL444281 | — | — | 1 | 7.20 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | — | 1 | 7.20 |
| CHEMBL16866 | — | — | 1 | 7.15 |
| CHEMBL27043 | — | — | 1 | 7.12 |
| CHEMBL17167 | — | — | 1 | 7.01 |
| CHEMBL432664 | — | — | 1 | 6.90 |
| CHEMBL27081 | — | — | 1 | 6.90 |
| CHEMBL17173 | — | — | 1 | 6.90 |
| CHEMBL17202 | — | — | 1 | 6.84 |
| CHEMBL278039 | — | — | 1 | 6.82 |
| CHEMBL16931 | — | — | 1 | 6.66 |
| CHEMBL17003 | — | — | 1 | 6.66 |
| CHEMBL17294 | — | — | 1 | 6.39 |
| CHEMBL17341 | — | — | 1 | 6.36 |
| CHEMBL275606 | — | — | 1 | 6.30 |
| CHEMBL16741 | — | — | 1 | 6.27 |
| CHEMBL17002 | — | — | 1 | 6.26 |
| CHEMBL273807 | — | — | 1 | 6.21 |
| CHEMBL275360 | — | — | 1 | 6.17 |
| CHEMBL16997 | — | — | 1 | 6.10 |
| CHEMBL17123 | — | — | 1 | 6.06 |
| CHEMBL277386 | — | — | 1 | 6.04 |
| CHEMBL16534 | — | — | 1 | 6.02 |
| CHEMBL16929 | — | — | 1 | 6.00 |
| CHEMBL275427 | — | — | 1 | 6.00 |
| CHEMBL16984 | — | — | 1 | 6.00 |
| CHEMBL16787 | — | — | 1 | 5.93 |
| CHEMBL17141 | — | — | 1 | 5.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL275605 | — | Ki | = | 25.9 | nM | 7.59 |
| CHEMBL16677 | — | Ki | = | 45.6 | nM | 7.34 |
| CHEMBL444281 | — | Ki | = | 63.3 | nM | 7.20 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL16866 | — | Ki | = | 71.1 | nM | 7.15 |
| CHEMBL27043 | — | Ki | = | 76.3 | nM | 7.12 |
| CHEMBL17167 | — | Ki | = | 98.1 | nM | 7.01 |
| CHEMBL432664 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL27081 | — | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL17173 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL17202 | — | Ki | = | 143.0 | nM | 6.84 |
| CHEMBL278039 | — | Ki | = | 152.0 | nM | 6.82 |
| CHEMBL16931 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL17003 | — | Ki | = | 221.0 | nM | 6.66 |
| CHEMBL17294 | — | Ki | = | 406.0 | nM | 6.39 |
| CHEMBL17341 | — | Ki | = | 434.0 | nM | 6.36 |
| CHEMBL275606 | — | Ki | = | 497.0 | nM | 6.30 |
| CHEMBL16741 | — | Ki | = | 541.0 | nM | 6.27 |
| CHEMBL17002 | — | Ki | = | 548.0 | nM | 6.26 |
| CHEMBL273807 | — | Ki | = | 612.0 | nM | 6.21 |
| CHEMBL275360 | — | Ki | = | 683.0 | nM | 6.17 |
| CHEMBL16997 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL17123 | — | Ki | = | 874.0 | nM | 6.06 |
| CHEMBL277386 | — | Ki | = | 917.0 | nM | 6.04 |
| CHEMBL16534 | — | Ki | = | 949.0 | nM | 6.02 |
| CHEMBL275427 | — | Ki | = | 995.0 | nM | 6.00 |
| CHEMBL16984 | — | Ki | = | 999.0 | nM | 6.00 |
| CHEMBL16929 | — | Ki | = | 988.0 | nM | 6.00 |
| CHEMBL16787 | — | Ki | = | 1180.0 | nM | 5.93 |
| CHEMBL17141 | — | Ki | = | 1370.0 | nM | 5.86 |
| CHEMBL27041 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL275149 | — | Ki | = | 2750.0 | nM | 5.56 |
| CHEMBL16724 | — | Ki | = | 4290.0 | nM | 5.37 |
| CHEMBL16908 | — | Ki | = | 4450.0 | nM | 5.35 |
| CHEMBL17103 | — | Ki | < | 10.0 | nM | - |