Assay Detail
Binding
CHEMBL640305
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Displacement of [3H]CGS-21680 binding to human Adenosine A2A receptor expressed in HEK293 cells
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
1,2,4-Triazolo[5,1-i]purine derivatives as highly potent and selective human adenosine A(3) receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.55 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL124788 | — | — | 1 | 7.75 |
| CHEMBL330982 | — | — | 1 | 7.64 |
| CHEMBL123310 | — | — | 1 | 7.34 |
| CHEMBL122928 | — | — | 1 | 7.33 |
| CHEMBL122667 | — | — | 1 | 7.25 |
| CHEMBL123450 | — | — | 1 | 7.24 |
| CHEMBL123172 | — | — | 1 | 7.17 |
| CHEMBL122512 | — | — | 1 | 7.15 |
| CHEMBL123465 | — | — | 1 | 6.92 |
| CHEMBL332742 | — | — | 1 | 6.75 |
| CHEMBL122685 | — | — | 1 | 6.73 |
| CHEMBL122511 | — | — | 1 | 6.70 |
| CHEMBL125647 | — | — | 1 | 6.68 |
| CHEMBL330873 | — | — | 1 | 6.44 |
| CHEMBL333415 | — | — | 1 | 6.29 |
| CHEMBL339655 | — | — | 1 | 6.26 |
| CHEMBL123195 | — | — | 1 | 6.05 |
| CHEMBL331111 | — | — | 1 | 5.80 |
| CHEMBL333535 | — | — | 1 | 5.60 |
| CHEMBL121339 | — | — | 1 | 5.58 |
| CHEMBL123144 | — | — | 1 | 5.48 |
| CHEMBL122819 | — | — | 1 | 5.42 |
| CHEMBL123203 | — | — | 1 | 5.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL124788 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL330982 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL123310 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL122928 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL122667 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL123450 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL123172 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL122512 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL123465 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL332742 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL122685 | — | IC50 | = | 188.0 | nM | 6.73 |
| CHEMBL122511 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL125647 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL330873 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL333415 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL339655 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL123195 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL331111 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL333535 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL121339 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL123144 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL122819 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL123203 | — | IC50 | = | 7800.0 | nM | 5.11 |