Assay Detail
Functional
CHEMBL4156076
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
26
Total Activities
13
Compounds Tested
2
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
Structure-activity relationship studies and pharmacological characterization of N5-heteroarylalkyl-substituted-2-(2-furanyl)thiazolo[5,4-d]pyrimidine-5,7-diamine-based derivatives as inverse agonists at human A2A adenosine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Emax | 13 | - | - |
| IC50 | 13 | 9.11 | 10.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4161758 | — | — | 2 | 10.44 |
| CHEMBL4172399 | — | — | 2 | 10.40 |
| CHEMBL4172264 | — | — | 2 | 10.35 |
| CHEMBL4167125 | — | — | 2 | 10.23 |
| CHEMBL4162638 | — | — | 2 | 9.46 |
| CHEMBL4159215 | — | — | 2 | 9.39 |
| CHEMBL113142 | ZM-241385 | — | 2 | 9.08 |
| CHEMBL4167813 | — | — | 2 | 8.89 |
| CHEMBL4167557 | — | — | 2 | 8.37 |
| CHEMBL4162037 | — | — | 2 | 8.36 |
| CHEMBL4172818 | — | — | 2 | 7.95 |
| CHEMBL4168016 | — | — | 2 | 7.75 |
| CHEMBL4175676 | — | — | 2 | 7.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4161758 | — | IC50 | = | 0.036 | nM | 10.44 |
| CHEMBL4172399 | — | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL4172264 | — | IC50 | = | 0.045 | nM | 10.35 |
| CHEMBL4167125 | — | IC50 | = | 0.059 | nM | 10.23 |
| CHEMBL4162638 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL4159215 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL113142 | ZM-241385 | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL4167813 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4167557 | — | IC50 | = | 4.26 | nM | 8.37 |
| CHEMBL4162037 | — | IC50 | = | 4.41 | nM | 8.36 |
| CHEMBL4172818 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL4168016 | — | IC50 | = | 17.6 | nM | 7.75 |
| CHEMBL4175676 | — | IC50 | = | 18.7 | nM | 7.73 |
| CHEMBL113142 | ZM-241385 | Emax | = | 121.0 | % | - |
| CHEMBL4161758 | — | Emax | = | 132.0 | % | - |
| CHEMBL4172399 | — | Emax | = | 133.0 | % | - |
| CHEMBL4167125 | — | Emax | = | 126.0 | % | - |
| CHEMBL4159215 | — | Emax | = | 137.0 | % | - |
| CHEMBL4167813 | — | Emax | = | 128.0 | % | - |
| CHEMBL4175676 | — | Emax | = | 122.0 | % | - |
| CHEMBL4172818 | — | Emax | = | 117.0 | % | - |
| CHEMBL4172264 | — | Emax | = | 138.0 | % | - |
| CHEMBL4167557 | — | Emax | = | 121.0 | % | - |
| CHEMBL4162638 | — | Emax | = | 141.0 | % | - |
| CHEMBL4162037 | — | Emax | = | 129.0 | % | - |
| CHEMBL4168016 | — | Emax | = | 115.0 | % | - |