Assay Detail
Binding
CHEMBL4156072
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in CHO cell membranes measured after 60 mins by scintillation counting method
21
Total Activities
17
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 13 | 8.37 | 9.62 |
| KiL | 4 | - | - |
| KiH | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4162638 | — | — | 1 | 9.62 |
| CHEMBL4159215 | — | — | 1 | 9.60 |
| CHEMBL4167813 | — | — | 1 | 9.38 |
| CHEMBL113142 | ZM-241385 | — | 1 | 9.06 |
| CHEMBL4167557 | — | — | 1 | 8.67 |
| CHEMBL4162037 | — | — | 1 | 8.65 |
| CHEMBL4172818 | — | — | 1 | 8.29 |
| CHEMBL4168016 | — | — | 1 | 8.00 |
| CHEMBL4175676 | — | — | 1 | 7.92 |
| CHEMBL4168980 | — | — | 1 | 7.70 |
| CHEMBL4175878 | — | — | 1 | 7.66 |
| CHEMBL4172715 | — | — | 1 | 7.47 |
| CHEMBL4165484 | — | — | 1 | 6.84 |
| CHEMBL4172264 | — | — | 2 | - |
| CHEMBL4167125 | — | — | 2 | - |
| CHEMBL4172399 | — | — | 2 | - |
| CHEMBL4161758 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4162638 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL4159215 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL4167813 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL113142 | ZM-241385 | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL4167557 | — | Ki | = | 2.15 | nM | 8.67 |
| CHEMBL4162037 | — | Ki | = | 2.24 | nM | 8.65 |
| CHEMBL4172818 | — | Ki | = | 5.14 | nM | 8.29 |
| CHEMBL4168016 | — | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL4175676 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4168980 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4175878 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL4172715 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL4165484 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL4167125 | — | KiH | = | 217.0 | fM | - |
| CHEMBL4172399 | — | KiL | = | 1.73 | nM | - |
| CHEMBL4172399 | — | KiH | = | 39.0 | fM | - |
| CHEMBL4161758 | — | KiL | = | 3.82 | nM | - |
| CHEMBL4161758 | — | KiH | = | 10.7 | fM | - |
| CHEMBL4167125 | — | KiL | = | 0.68 | nM | - |
| CHEMBL4172264 | — | KiL | = | 18.0 | nM | - |
| CHEMBL4172264 | — | KiH | = | 10.6 | fM | - |