Assay Detail
Binding
CHEMBL5099271
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Inhibition of CA200645 binding to NanoLuc-fused human adenosine A1 receptor expressed in HEK293 cells assessed as kinetic dissociation constant by NanoBRET competition binding assay
27
Total Activities
27
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 |
|---|---|---|---|
| Kd | 27 | 6.75 | 7.81 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5205907 | — | — | 1 | 7.81 |
| CHEMBL5174429 | — | — | 1 | 7.75 |
| CHEMBL5195714 | — | — | 1 | 7.66 |
| CHEMBL5171042 | — | — | 1 | 7.63 |
| CHEMBL5174052 | — | — | 1 | 7.47 |
| CHEMBL5197358 | — | — | 1 | 7.34 |
| CHEMBL5187330 | — | — | 1 | 7.23 |
| CHEMBL5186757 | — | — | 1 | 6.97 |
| CHEMBL5208245 | — | — | 1 | 6.94 |
| CHEMBL5203632 | — | — | 1 | 6.91 |
| CHEMBL5201013 | — | — | 1 | 6.90 |
| CHEMBL5187478 | — | — | 1 | 6.77 |
| CHEMBL5199871 | — | — | 1 | 6.74 |
| CHEMBL5191989 | — | — | 1 | 6.71 |
| CHEMBL5184828 | — | — | 1 | 6.67 |
| CHEMBL464859 | NECA | — | 1 | 6.63 |
| CHEMBL477 | ADENOSINE | 4.0 | 1 | 6.53 |
| CHEMBL5209222 | — | — | 1 | 6.48 |
| CHEMBL5171285 | — | — | 1 | 6.44 |
| CHEMBL3771208 | — | — | 1 | 6.30 |
| CHEMBL5188601 | — | — | 1 | 6.23 |
| CHEMBL5186981 | — | — | 1 | 6.22 |
| CHEMBL5206687 | — | — | 1 | 6.13 |
| CHEMBL5170857 | — | — | 1 | 6.04 |
| CHEMBL5182056 | — | — | 1 | 6.02 |
| CHEMBL5172389 | — | — | 1 | 5.94 |
| CHEMBL5179726 | — | — | 1 | 5.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5205907 | — | Kd | = | 15.49 | nM | 7.81 |
| CHEMBL5174429 | — | Kd | = | 17.78 | nM | 7.75 |
| CHEMBL5195714 | — | Kd | = | 21.88 | nM | 7.66 |
| CHEMBL5171042 | — | Kd | = | 23.44 | nM | 7.63 |
| CHEMBL5174052 | — | Kd | = | 33.88 | nM | 7.47 |
| CHEMBL5197358 | — | Kd | = | 45.71 | nM | 7.34 |
| CHEMBL5187330 | — | Kd | = | 58.88 | nM | 7.23 |
| CHEMBL5186757 | — | Kd | = | 107.15 | nM | 6.97 |
| CHEMBL5208245 | — | Kd | = | 114.82 | nM | 6.94 |
| CHEMBL5203632 | — | Kd | = | 123.03 | nM | 6.91 |
| CHEMBL5201013 | — | Kd | = | 125.89 | nM | 6.90 |
| CHEMBL5187478 | — | Kd | = | 169.82 | nM | 6.77 |
| CHEMBL5199871 | — | Kd | = | 181.97 | nM | 6.74 |
| CHEMBL5191989 | — | Kd | = | 194.98 | nM | 6.71 |
| CHEMBL5184828 | — | Kd | = | 213.8 | nM | 6.67 |
| CHEMBL464859 | NECA | Kd | = | 234.42 | nM | 6.63 |
| CHEMBL477 | ADENOSINE | Kd | = | 295.12 | nM | 6.53 |
| CHEMBL5209222 | — | Kd | = | 331.13 | nM | 6.48 |
| CHEMBL5171285 | — | Kd | = | 363.08 | nM | 6.44 |
| CHEMBL3771208 | — | Kd | = | 501.19 | nM | 6.30 |
| CHEMBL5188601 | — | Kd | = | 588.84 | nM | 6.23 |
| CHEMBL5186981 | — | Kd | = | 602.56 | nM | 6.22 |
| CHEMBL5206687 | — | Kd | = | 741.31 | nM | 6.13 |
| CHEMBL5170857 | — | Kd | = | 912.01 | nM | 6.04 |
| CHEMBL5182056 | — | Kd | = | 954.99 | nM | 6.02 |
| CHEMBL5172389 | — | Kd | = | 1148.15 | nM | 5.94 |
| CHEMBL5179726 | — | Kd | = | 1445.44 | nM | 5.84 |