Assay Detail
Binding
CHEMBL641522
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In vitro binding affinity at human Adenosine A3 receptor from HEK293 cells by [125I]AB-MECA displacement.
18
Total Activities
18
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
Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.65 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL340868 | — | — | 1 | 9.96 |
| CHEMBL89093 | — | — | 1 | 9.25 |
| CHEMBL88147 | — | — | 1 | 9.19 |
| CHEMBL317382 | — | — | 1 | 8.52 |
| CHEMBL329722 | — | — | 1 | 8.12 |
| CHEMBL16687 | CGS-15943 | — | 1 | 7.86 |
| CHEMBL318251 | — | — | 1 | 7.86 |
| CHEMBL319971 | — | — | 1 | 7.84 |
| CHEMBL313422 | — | — | 1 | 7.67 |
| CHEMBL93932 | — | — | 1 | 7.62 |
| CHEMBL100195 | — | — | 1 | 7.48 |
| CHEMBL7266 | — | — | 1 | 7.19 |
| CHEMBL95811 | — | — | 1 | 7.09 |
| CHEMBL96041 | — | — | 1 | 7.08 |
| CHEMBL317310 | — | — | 1 | 6.61 |
| CHEMBL414023 | — | — | 1 | 6.58 |
| CHEMBL317157 | — | — | 1 | 6.07 |
| CHEMBL97383 | — | — | 1 | 5.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL340868 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL89093 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL88147 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL317382 | — | Ki | = | 3.03 | nM | 8.52 |
| CHEMBL329722 | — | Ki | = | 7.66 | nM | 8.12 |
| CHEMBL16687 | CGS-15943 | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL318251 | — | Ki | = | 13.9 | nM | 7.86 |
| CHEMBL319971 | — | Ki | = | 14.6 | nM | 7.84 |
| CHEMBL313422 | — | Ki | = | 21.5 | nM | 7.67 |
| CHEMBL93932 | — | Ki | = | 23.8 | nM | 7.62 |
| CHEMBL100195 | — | Ki | = | 32.9 | nM | 7.48 |
| CHEMBL7266 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL95811 | — | Ki | = | 80.8 | nM | 7.09 |
| CHEMBL96041 | — | Ki | = | 82.5 | nM | 7.08 |
| CHEMBL317310 | — | Ki | = | 244.0 | nM | 6.61 |
| CHEMBL414023 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL317157 | — | Ki | = | 856.0 | nM | 6.07 |
| CHEMBL97383 | — | Ki | = | 1813.0 | nM | 5.74 |