Assay Detail
Binding
CHEMBL644556
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Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
28
Total Activities
28
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 | 28 | 8.96 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL122819 | — | — | 1 | 9.68 |
| CHEMBL123172 | — | — | 1 | 9.66 |
| CHEMBL123465 | — | — | 1 | 9.64 |
| CHEMBL122512 | — | — | 1 | 9.60 |
| CHEMBL333415 | — | — | 1 | 9.60 |
| CHEMBL122685 | — | — | 1 | 9.57 |
| CHEMBL124788 | — | — | 1 | 9.54 |
| CHEMBL122511 | — | — | 1 | 9.52 |
| CHEMBL333860 | — | — | 1 | 9.52 |
| CHEMBL332742 | — | — | 1 | 9.48 |
| CHEMBL121339 | — | — | 1 | 9.39 |
| CHEMBL330982 | — | — | 1 | 9.39 |
| CHEMBL330873 | — | — | 1 | 9.35 |
| CHEMBL123203 | — | — | 1 | 9.21 |
| CHEMBL123462 | — | — | 1 | 9.17 |
| CHEMBL339655 | — | — | 1 | 9.00 |
| CHEMBL122667 | — | — | 1 | 8.96 |
| CHEMBL333535 | — | — | 1 | 8.96 |
| CHEMBL123195 | — | — | 1 | 8.92 |
| CHEMBL122632 | — | — | 1 | 8.92 |
| CHEMBL123450 | — | — | 1 | 8.74 |
| CHEMBL123144 | — | — | 1 | 8.72 |
| CHEMBL122987 | — | — | 1 | 8.48 |
| CHEMBL123346 | — | — | 1 | 8.30 |
| CHEMBL125647 | — | — | 1 | 8.23 |
| CHEMBL123310 | — | — | 1 | 6.21 |
| CHEMBL122928 | — | — | 1 | 6.17 |
| CHEMBL331111 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL122819 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL123172 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL123465 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL122512 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL333415 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL122685 | — | IC50 | = | 0.27 | nM | 9.57 |
| CHEMBL124788 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL122511 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL333860 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL332742 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL121339 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL330982 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL330873 | — | IC50 | = | 0.45 | nM | 9.35 |
| CHEMBL123203 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL123462 | — | IC50 | = | 0.67 | nM | 9.17 |
| CHEMBL339655 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL122667 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL333535 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL123195 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL122632 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL123450 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL123144 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL122987 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL123346 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL125647 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL123310 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL122928 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL331111 | — | IC50 | < | 0.1 | nM | - |