Assay Detail
Binding
CHEMBL643183
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Inhibition of binding to Adenosine-2 receptor using [3H]NECA in rat striatum
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Structure-activity profile of a series of novel triazoloquinazoline adenosine antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.88 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL268431 | — | — | 1 | 8.48 |
| CHEMBL268550 | — | — | 1 | 8.26 |
| CHEMBL267015 | — | — | 1 | 7.72 |
| CHEMBL267415 | — | — | 1 | 7.57 |
| CHEMBL268867 | — | — | 1 | 7.25 |
| CHEMBL8136 | — | — | 1 | 7.21 |
| CHEMBL266095 | — | — | 1 | 6.94 |
| CHEMBL268615 | — | — | 1 | 6.84 |
| CHEMBL266267 | — | — | 1 | 6.80 |
| CHEMBL269785 | — | — | 1 | 6.75 |
| CHEMBL7266 | — | — | 1 | 6.28 |
| CHEMBL7551 | — | — | 1 | 5.92 |
| CHEMBL7748 | — | — | 1 | 5.89 |
| CHEMBL7511 | — | — | 1 | 5.80 |
| CHEMBL7897 | — | — | 1 | 5.54 |
| CHEMBL414023 | — | — | 1 | - |
| CHEMBL7759 | — | — | 1 | - |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | - |
| CHEMBL7582 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL268431 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL268550 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL267015 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL267415 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL268867 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL8136 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL266095 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL268615 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL266267 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL269785 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL7266 | — | IC50 | = | 531.0 | nM | 6.28 |
| CHEMBL7551 | — | IC50 | = | 1205.0 | nM | 5.92 |
| CHEMBL7748 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL7511 | — | IC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL7897 | — | IC50 | = | 2914.0 | nM | 5.54 |
| CHEMBL414023 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL7759 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1355736 | THEOPHYLLINE | IC50 | > | 10000.0 | nM | - |
| CHEMBL7582 | — | IC50 | > | 10000.0 | nM | - |