Assay Detail
Binding
CHEMBL5099261
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Inhibition of CA200645 binding to NanoLuc-fused human adenosine A1 receptor expressed in HEK293 cells measured for 10 mins by NanoBRET competition binding assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and Structure-Activity Relationship Studies of Novel Adenosine A<sub>1</sub> Receptor-Selective Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 31 | 6.56 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5174052 | — | — | 1 | 7.55 |
| CHEMBL5174429 | — | — | 1 | 7.43 |
| CHEMBL5195714 | — | — | 1 | 7.39 |
| CHEMBL5171042 | — | — | 1 | 7.30 |
| CHEMBL5187330 | — | — | 1 | 7.26 |
| CHEMBL5205907 | — | — | 1 | 7.19 |
| CHEMBL5197358 | — | — | 1 | 7.17 |
| CHEMBL5203632 | — | — | 1 | 7.05 |
| CHEMBL5191989 | — | — | 1 | 6.86 |
| CHEMBL5186757 | — | — | 1 | 6.84 |
| CHEMBL5187478 | — | — | 1 | 6.67 |
| CHEMBL5208245 | — | — | 1 | 6.63 |
| CHEMBL5201013 | — | — | 1 | 6.61 |
| CHEMBL464859 | NECA | — | 1 | 6.61 |
| CHEMBL5199871 | — | — | 1 | 6.56 |
| CHEMBL5172389 | — | — | 1 | 6.54 |
| CHEMBL5184828 | — | — | 1 | 6.49 |
| CHEMBL5170857 | — | — | 1 | 6.39 |
| CHEMBL5171285 | — | — | 1 | 6.35 |
| CHEMBL5188601 | — | — | 1 | 6.35 |
| CHEMBL5186981 | — | — | 1 | 6.23 |
| CHEMBL3771208 | — | — | 1 | 6.18 |
| CHEMBL5179726 | — | — | 1 | 6.16 |
| CHEMBL5206687 | — | — | 1 | 6.15 |
| CHEMBL5209222 | — | — | 1 | 6.15 |
| CHEMBL477 | ADENOSINE | 4.0 | 1 | 6.09 |
| CHEMBL5182056 | — | — | 1 | 5.94 |
| CHEMBL5183907 | — | — | 1 | 5.90 |
| CHEMBL5196040 | — | — | 1 | 5.85 |
| CHEMBL5171835 | — | — | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5174052 | — | Ki | = | 28.18 | nM | 7.55 |
| CHEMBL5174429 | — | Ki | = | 37.15 | nM | 7.43 |
| CHEMBL5195714 | — | Ki | = | 40.74 | nM | 7.39 |
| CHEMBL5171042 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL5187330 | — | Ki | = | 54.95 | nM | 7.26 |
| CHEMBL5205907 | — | Ki | = | 64.57 | nM | 7.19 |
| CHEMBL5197358 | — | Ki | = | 67.61 | nM | 7.17 |
| CHEMBL5203632 | — | Ki | = | 89.13 | nM | 7.05 |
| CHEMBL5191989 | — | Ki | = | 138.04 | nM | 6.86 |
| CHEMBL5186757 | — | Ki | = | 144.54 | nM | 6.84 |
| CHEMBL5187478 | — | Ki | = | 213.8 | nM | 6.67 |
| CHEMBL5208245 | — | Ki | = | 234.42 | nM | 6.63 |
| CHEMBL5201013 | — | Ki | = | 245.47 | nM | 6.61 |
| CHEMBL464859 | NECA | Ki | = | 245.47 | nM | 6.61 |
| CHEMBL5199871 | — | Ki | = | 275.42 | nM | 6.56 |
| CHEMBL5172389 | — | Ki | = | 288.4 | nM | 6.54 |
| CHEMBL5184828 | — | Ki | = | 323.59 | nM | 6.49 |
| CHEMBL5170857 | — | Ki | = | 407.38 | nM | 6.39 |
| CHEMBL5171285 | — | Ki | = | 446.68 | nM | 6.35 |
| CHEMBL5188601 | — | Ki | = | 446.68 | nM | 6.35 |
| CHEMBL5186981 | — | Ki | = | 588.84 | nM | 6.23 |
| CHEMBL3771208 | — | Ki | = | 660.69 | nM | 6.18 |
| CHEMBL5179726 | — | Ki | = | 691.83 | nM | 6.16 |
| CHEMBL5206687 | — | Ki | = | 707.95 | nM | 6.15 |
| CHEMBL5209222 | — | Ki | = | 707.95 | nM | 6.15 |
| CHEMBL477 | ADENOSINE | Ki | = | 812.83 | nM | 6.09 |
| CHEMBL5182056 | — | Ki | = | 1148.15 | nM | 5.94 |
| CHEMBL5183907 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL5196040 | — | Ki | = | 1412.54 | nM | 5.85 |
| CHEMBL5171835 | — | Ki | = | 1698.24 | nM | 5.77 |
| CHEMBL5184329 | — | Ki | = | 2630.27 | nM | 5.58 |