Assay Detail
Binding
CHEMBL640326
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Inhibition of binding towards adenosine A1 receptor using [3H]N-cyclohexyladenosine ([3H]CHA) in rat whole brain membranes.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Brain membranes |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Structure-activity profile of a series of novel triazoloquinazoline adenosine antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.82 | 8.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL268550 | — | — | 1 | 8.02 |
| CHEMBL268431 | — | — | 1 | 7.68 |
| CHEMBL268867 | — | — | 1 | 7.68 |
| CHEMBL269785 | — | — | 1 | 7.66 |
| CHEMBL267015 | — | — | 1 | 7.51 |
| CHEMBL267415 | — | — | 1 | 7.42 |
| CHEMBL266267 | — | — | 1 | 7.21 |
| CHEMBL8136 | — | — | 1 | 7.05 |
| CHEMBL7748 | — | — | 1 | 6.84 |
| CHEMBL268615 | — | — | 1 | 6.53 |
| CHEMBL266095 | — | — | 1 | 6.49 |
| CHEMBL7551 | — | — | 1 | 6.21 |
| CHEMBL7511 | — | — | 1 | 6.08 |
| CHEMBL7897 | — | — | 1 | 5.91 |
| CHEMBL7266 | — | — | 1 | 5.80 |
| CHEMBL414023 | — | — | 1 | 5.00 |
| CHEMBL7582 | — | — | 1 | - |
| CHEMBL7759 | — | — | 1 | - |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL268550 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL268431 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL268867 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL269785 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL267015 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL267415 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL266267 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL8136 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL7748 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL268615 | — | IC50 | = | 295.0 | nM | 6.53 |
| CHEMBL266095 | — | IC50 | = | 324.0 | nM | 6.49 |
| CHEMBL7551 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL7511 | — | IC50 | = | 827.0 | nM | 6.08 |
| CHEMBL7897 | — | IC50 | = | 1219.0 | nM | 5.91 |
| CHEMBL7266 | — | IC50 | = | 1570.0 | nM | 5.80 |
| CHEMBL414023 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL7582 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL7759 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1355736 | THEOPHYLLINE | IC50 | > | 10000.0 | nM | - |