Assay Detail
Binding
CHEMBL2401084
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ZM241385 from human recombinant adenosine A2A receptor expressed in HEK293 cells after 1 hr by competitive binding assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of metabolites of 2-n-butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535), a potent antagonist of the A2A adenosine receptor for the treatment of Parkinson's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.74 | 8.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2398484 | — | — | 1 | 8.12 |
| CHEMBL2398482 | — | — | 1 | 8.08 |
| CHEMBL197669 | ST1535 | 1.0 | 1 | 7.97 |
| CHEMBL2398486 | — | — | 1 | 7.92 |
| CHEMBL2398483 | — | — | 1 | 7.72 |
| CHEMBL2398480 | — | — | 1 | 7.66 |
| CHEMBL2398485 | — | — | 1 | 7.28 |
| CHEMBL2398481 | — | — | 1 | 7.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2398484 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL2398482 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL197669 | ST1535 | Ki | = | 10.7 | nM | 7.97 |
| CHEMBL2398486 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL2398483 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL2398480 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL2398485 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL2398481 | — | Ki | = | 64.0 | nM | 7.19 |