Assay Detail
Binding
CHEMBL4152680
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]CCPA from recombinant human adenosine A1 receptor transfected in CHO cell membranes after 3 hrs by microbeta scintillation counting analysis
26
Total Activities
26
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
New potent and selective A1 adenosine receptor antagonists as potential tools for the treatment of gastrointestinal diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 7.70 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4175366 | — | — | 1 | 8.55 |
| CHEMBL4165013 | — | — | 1 | 8.49 |
| CHEMBL4167491 | — | — | 1 | 8.41 |
| CHEMBL4167077 | — | — | 1 | 8.24 |
| CHEMBL4171919 | — | — | 1 | 8.22 |
| CHEMBL4170850 | — | — | 1 | 8.21 |
| CHEMBL4177249 | — | — | 1 | 8.21 |
| CHEMBL4170180 | — | — | 1 | 8.19 |
| CHEMBL4170460 | — | — | 1 | 8.10 |
| CHEMBL4170873 | — | — | 1 | 8.10 |
| CHEMBL4163630 | — | — | 1 | 8.00 |
| CHEMBL4159165 | — | — | 1 | 8.00 |
| CHEMBL4160264 | — | — | 1 | 8.00 |
| CHEMBL4164048 | — | — | 1 | 7.82 |
| CHEMBL4174108 | — | — | 1 | 7.77 |
| CHEMBL4159137 | — | — | 1 | 7.75 |
| CHEMBL424597 | — | — | 1 | 7.64 |
| CHEMBL4174308 | — | — | 1 | 7.60 |
| CHEMBL4163601 | — | — | 1 | 7.57 |
| CHEMBL4173347 | — | — | 1 | 7.51 |
| CHEMBL4161796 | — | — | 1 | 7.43 |
| CHEMBL4160242 | — | — | 1 | 7.26 |
| CHEMBL4169401 | — | — | 1 | 7.12 |
| CHEMBL4175631 | — | — | 1 | 7.00 |
| CHEMBL4176479 | — | — | 1 | 6.62 |
| CHEMBL4167197 | — | — | 1 | 4.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4175366 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL4165013 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL4167491 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL4167077 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL4171919 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4170850 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL4177249 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL4170180 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL4170460 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4170873 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4163630 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4159165 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4160264 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4164048 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL4174108 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4159137 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL424597 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL4174308 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL4163601 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL4173347 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL4161796 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL4160242 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL4169401 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL4175631 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL4176479 | — | Ki | = | 242.0 | nM | 6.62 |
| CHEMBL4167197 | — | Ki | = | 54000.0 | nM | 4.27 |