Assay Detail
Functional
CHEMBL2401083
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA addition
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| IC50 | 7 | 6.14 | 6.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2398483 | — | — | 1 | 6.58 |
| CHEMBL2398484 | — | — | 1 | 6.38 |
| CHEMBL197669 | ST1535 | 1.0 | 1 | 6.37 |
| CHEMBL2398482 | — | — | 1 | 6.35 |
| CHEMBL2398486 | — | — | 1 | 6.00 |
| CHEMBL2398485 | — | — | 1 | 5.68 |
| CHEMBL2398480 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2398483 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL2398484 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL197669 | ST1535 | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL2398482 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL2398486 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL2398485 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL2398480 | — | IC50 | = | 2300.0 | nM | 5.64 |