Assay Detail
Binding
CHEMBL645034
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity for adenosine A1 receptor determined using hamster DDT1 cell membranes with [3H]CCPA as radioligand
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cricetulus griseus |
| Cell Type | DDT1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Affinity and intrinsic efficacy (IE) of 5'-carbamoyl adenosine analogues for the A1 adenosine receptor--efforts towards the discovery of a chronic ventricular rate control agent for the treatment of atrial fibrillation (AF).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 6.86 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL392149 | TECADENOSON | 2.0 | 1 | 8.52 |
| CHEMBL347519 | — | — | 1 | 7.92 |
| CHEMBL358613 | — | — | 1 | 7.48 |
| CHEMBL150200 | — | — | 1 | 7.46 |
| CHEMBL150676 | — | — | 1 | 7.44 |
| CHEMBL150348 | — | — | 1 | 7.35 |
| CHEMBL149520 | — | — | 1 | 7.30 |
| CHEMBL151050 | — | — | 1 | 7.26 |
| CHEMBL358227 | — | — | 1 | 7.15 |
| CHEMBL356610 | — | — | 1 | 7.14 |
| CHEMBL151169 | — | — | 1 | 7.11 |
| CHEMBL149790 | — | — | 1 | 7.02 |
| CHEMBL150950 | — | — | 1 | 6.85 |
| CHEMBL150944 | — | — | 1 | 6.83 |
| CHEMBL347342 | — | — | 1 | 6.80 |
| CHEMBL151074 | — | — | 1 | 6.80 |
| CHEMBL150240 | — | — | 1 | 6.78 |
| CHEMBL150490 | — | — | 1 | 6.69 |
| CHEMBL150604 | — | — | 1 | 6.68 |
| CHEMBL358218 | — | — | 1 | 6.65 |
| CHEMBL151046 | — | — | 1 | 6.63 |
| CHEMBL150517 | — | — | 1 | 6.62 |
| CHEMBL357055 | — | — | 1 | 6.60 |
| CHEMBL149735 | — | — | 1 | 6.51 |
| CHEMBL356776 | — | — | 1 | 6.49 |
| CHEMBL356860 | — | — | 1 | 6.28 |
| CHEMBL345494 | — | — | 1 | 6.23 |
| CHEMBL151968 | — | — | 1 | 5.85 |
| CHEMBL150983 | — | — | 1 | 5.74 |
| CHEMBL151282 | — | — | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL392149 | TECADENOSON | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL347519 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL358613 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL150200 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL150676 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL150348 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL149520 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL151050 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL358227 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL356610 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL151169 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL149790 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL150950 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL150944 | — | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL347342 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL151074 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL150240 | — | Ki | = | 167.0 | nM | 6.78 |
| CHEMBL150490 | — | Ki | = | 205.0 | nM | 6.69 |
| CHEMBL150604 | — | Ki | = | 209.0 | nM | 6.68 |
| CHEMBL358218 | — | Ki | = | 226.0 | nM | 6.65 |
| CHEMBL151046 | — | Ki | = | 235.0 | nM | 6.63 |
| CHEMBL150517 | — | Ki | = | 238.0 | nM | 6.62 |
| CHEMBL357055 | — | Ki | = | 253.0 | nM | 6.60 |
| CHEMBL149735 | — | Ki | = | 306.0 | nM | 6.51 |
| CHEMBL356776 | — | Ki | = | 321.0 | nM | 6.49 |
| CHEMBL356860 | — | Ki | = | 524.0 | nM | 6.28 |
| CHEMBL345494 | — | Ki | = | 584.0 | nM | 6.23 |
| CHEMBL151968 | — | Ki | = | 1409.0 | nM | 5.85 |
| CHEMBL150983 | — | Ki | = | 1826.0 | nM | 5.74 |
| CHEMBL151282 | — | Ki | = | 1913.0 | nM | 5.72 |