Assay Detail
Binding
CHEMBL640700
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Binding affinity towards the adenosine A1 receptor in cerebral cortices of Sprague-Dawley male rats using [3H]CHA as radioligand.
94
Total Activities
93
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
4-Amino[1,2,4]triazolo[4,3-a]quinoxalines. A novel class of potent adenosine receptor antagonists and potential rapid-onset antidepressants.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 94 | 6.04 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL45891 | — | — | 2 | 8.77 |
| CHEMBL72669 | — | — | 1 | 8.26 |
| CHEMBL16687 | CGS-15943 | — | 1 | 8.22 |
| CHEMBL464859 | NECA | — | 1 | 8.00 |
| CHEMBL72517 | — | — | 1 | 7.70 |
| CHEMBL311616 | — | — | 1 | 7.62 |
| CHEMBL420368 | — | — | 1 | 7.62 |
| CHEMBL73478 | — | — | 1 | 7.55 |
| CHEMBL306351 | — | — | 1 | 7.50 |
| CHEMBL73747 | — | — | 1 | 7.36 |
| CHEMBL442176 | — | — | 1 | 7.24 |
| CHEMBL72177 | — | — | 1 | 7.22 |
| CHEMBL307187 | — | — | 1 | 7.19 |
| CHEMBL73181 | — | — | 1 | 7.12 |
| CHEMBL70435 | — | — | 1 | 7.00 |
| CHEMBL310177 | — | — | 1 | 6.96 |
| CHEMBL72051 | — | — | 1 | 6.96 |
| CHEMBL312449 | — | — | 1 | 6.96 |
| CHEMBL431376 | — | — | 1 | 6.85 |
| CHEMBL73596 | — | — | 1 | 6.80 |
| CHEMBL306850 | — | — | 1 | 6.77 |
| CHEMBL73006 | — | — | 1 | 6.75 |
| CHEMBL73595 | — | — | 1 | 6.66 |
| CHEMBL421117 | — | — | 1 | 6.64 |
| CHEMBL303198 | — | — | 1 | 6.57 |
| CHEMBL72953 | — | — | 1 | 6.55 |
| CHEMBL311481 | — | — | 1 | 6.54 |
| CHEMBL70701 | — | — | 1 | 6.46 |
| CHEMBL70585 | — | — | 1 | 6.43 |
| CHEMBL73163 | — | — | 1 | 6.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL45891 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL45891 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL72669 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL16687 | CGS-15943 | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL464859 | NECA | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL72517 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL311616 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL420368 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL73478 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL306351 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL73747 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL442176 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL72177 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL307187 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL73181 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL70435 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL312449 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL72051 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL310177 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL431376 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL73596 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL306850 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL73006 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL73595 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL421117 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL303198 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL72953 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL311481 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL70701 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL70585 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL73163 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL72052 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL304769 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL71106 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL310251 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL6958 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL73056 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL308834 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL306044 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL74681 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL70359 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL73682 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL304621 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL70810 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL72367 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL72235 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL312744 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL72518 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL72271 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL73210 | — | IC50 | = | 1800.0 | nM | 5.75 |