Assay Detail
Binding
CHEMBL4156071
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes measured after 90 mins by scintillation counting method
17
Total Activities
17
Compounds Tested
1
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 | 17 | 7.66 | 8.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4162638 | — | — | 1 | 8.58 |
| CHEMBL4172264 | — | — | 1 | 8.31 |
| CHEMBL4167557 | — | — | 1 | 8.28 |
| CHEMBL4167125 | — | — | 1 | 8.15 |
| CHEMBL4159215 | — | — | 1 | 8.09 |
| CHEMBL4161758 | — | — | 1 | 7.90 |
| CHEMBL4162037 | — | — | 1 | 7.76 |
| CHEMBL4172818 | — | — | 1 | 7.60 |
| CHEMBL4167813 | — | — | 1 | 7.55 |
| CHEMBL4168980 | — | — | 1 | 7.54 |
| CHEMBL4175878 | — | — | 1 | 7.43 |
| CHEMBL4172399 | — | — | 1 | 7.42 |
| CHEMBL4175676 | — | — | 1 | 7.33 |
| CHEMBL4165484 | — | — | 1 | 7.16 |
| CHEMBL4172715 | — | — | 1 | 7.15 |
| CHEMBL4168016 | — | — | 1 | 7.14 |
| CHEMBL113142 | ZM-241385 | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4162638 | — | Ki | = | 2.61 | nM | 8.58 |
| CHEMBL4172264 | — | Ki | = | 4.92 | nM | 8.31 |
| CHEMBL4167557 | — | Ki | = | 5.24 | nM | 8.28 |
| CHEMBL4167125 | — | Ki | = | 7.12 | nM | 8.15 |
| CHEMBL4159215 | — | Ki | = | 8.12 | nM | 8.09 |
| CHEMBL4161758 | — | Ki | = | 12.5 | nM | 7.90 |
| CHEMBL4162037 | — | Ki | = | 17.3 | nM | 7.76 |
| CHEMBL4172818 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL4167813 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL4168980 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL4175878 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL4172399 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL4175676 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL4165484 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL4172715 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL4168016 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL113142 | ZM-241385 | Ki | = | 178.0 | nM | 6.75 |