Assay Detail
Binding
CHEMBL643182
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Evaluated for the binding affinity towards the Adenosine A2 receptor in corpora striata of rats using [3H]NECA as radioligand.
58
Total Activities
58
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
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 | 58 | 5.93 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL16687 | CGS-15943 | — | 1 | 8.55 |
| CHEMBL464859 | NECA | — | 1 | 7.77 |
| CHEMBL303198 | — | — | 1 | 7.68 |
| CHEMBL312449 | — | — | 1 | 7.64 |
| CHEMBL72051 | — | — | 1 | 7.55 |
| CHEMBL73181 | — | — | 1 | 7.54 |
| CHEMBL73095 | — | — | 1 | 7.48 |
| CHEMBL431376 | — | — | 1 | 7.44 |
| CHEMBL307187 | — | — | 1 | 7.36 |
| CHEMBL72052 | — | — | 1 | 7.21 |
| CHEMBL312744 | — | — | 1 | 7.00 |
| CHEMBL311481 | — | — | 1 | 7.00 |
| CHEMBL71106 | — | — | 1 | 6.77 |
| CHEMBL72367 | — | — | 1 | 6.68 |
| CHEMBL72903 | — | — | 1 | 6.40 |
| CHEMBL72577 | — | — | 1 | 6.28 |
| CHEMBL74403 | — | — | 1 | 6.25 |
| CHEMBL45891 | — | — | 1 | 6.19 |
| CHEMBL73682 | — | — | 1 | 6.16 |
| CHEMBL72517 | — | — | 1 | 6.05 |
| CHEMBL73039 | — | — | 1 | 6.00 |
| CHEMBL72177 | — | — | 1 | 5.77 |
| CHEMBL72669 | — | — | 1 | 5.68 |
| CHEMBL311616 | — | — | 1 | 5.64 |
| CHEMBL420368 | — | — | 1 | 5.51 |
| CHEMBL310177 | — | — | 1 | 5.50 |
| CHEMBL70585 | — | — | 1 | 5.48 |
| CHEMBL70359 | — | — | 1 | 5.46 |
| CHEMBL442176 | — | — | 1 | 5.41 |
| CHEMBL73006 | — | — | 1 | 5.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL16687 | CGS-15943 | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL464859 | NECA | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL303198 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL312449 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL72051 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL73181 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL73095 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL431376 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL307187 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL72052 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL312744 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL311481 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL71106 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL72367 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL72903 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL72577 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL74403 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL45891 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL73682 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL72517 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL73039 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL72177 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL72669 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL311616 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL420368 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL310177 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL70585 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL70359 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL442176 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL73006 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL306850 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL73747 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL74681 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL72953 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL73596 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL6958 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL308834 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL73210 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL72398 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL275084 | ISOBUTYLMETHYLXANTHINE | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL421117 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL269318 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL70422 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL69722 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL7033 | — | IC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL304769 | — | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL306351 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL113 | CAFFEINE | IC50 | = | 63000.0 | nM | 4.20 |
| CHEMBL73163 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL73132 | — | IC50 | = | 110000.0 | nM | - |