Assay Detail
Functional
CHEMBL3878910
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, Synthesis, and Pharmacological Characterization of 2-(2-Furanyl)thiazolo[5,4-d]pyrimidine-5,7-diamine Derivatives: New Highly Potent A2A Adenosine Receptor Inverse Agonists with Antinociceptive Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.31 | 10.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3958838 | — | — | 1 | 10.29 |
| CHEMBL3904408 | — | — | 1 | 10.02 |
| CHEMBL113142 | ZM-241385 | — | 1 | 9.17 |
| CHEMBL3935610 | — | — | 1 | 7.80 |
| CHEMBL3950142 | — | — | 1 | 7.75 |
| CHEMBL3908770 | — | — | 1 | 7.68 |
| CHEMBL3932413 | — | — | 1 | 7.66 |
| CHEMBL3934626 | — | — | 1 | 7.51 |
| CHEMBL3931329 | — | — | 1 | 6.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3958838 | — | IC50 | = | 0.051 | nM | 10.29 |
| CHEMBL3904408 | — | IC50 | = | 0.095 | nM | 10.02 |
| CHEMBL113142 | ZM-241385 | IC50 | = | 0.678 | nM | 9.17 |
| CHEMBL3935610 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3950142 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3908770 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3932413 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3934626 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3931329 | — | IC50 | = | 123.0 | nM | 6.91 |