Assay Detail
Functional
CHEMBL5111998
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Antagonist activity at wild type A1R (unknown origin) expressed in CHO-K1 cells assessed as inhibition of NECA reduced forskolin stimulated cAMP accumulation incubated for 30 mins
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Dual A1/A3 Adenosine Receptor Antagonists: Binding Kinetics and Structure-Activity Relationship Studies Using Mutagenesis and Alchemical Binding Free Energy Calculations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 8.18 | 8.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL464859 | NECA | — | 1 | 8.95 |
| CHEMBL5174600 | — | — | 1 | 8.85 |
| CHEMBL3929143 | — | — | 1 | 8.72 |
| CHEMBL5180010 | — | — | 1 | 8.58 |
| CHEMBL3929812 | — | — | 1 | 8.54 |
| CHEMBL5173159 | — | — | 1 | 8.49 |
| CHEMBL5185003 | — | — | 1 | 8.41 |
| CHEMBL5189274 | — | — | 1 | 8.33 |
| CHEMBL5186062 | — | — | 1 | 8.30 |
| CHEMBL3927012 | — | — | 1 | 8.30 |
| CHEMBL5201810 | — | — | 1 | 8.16 |
| CHEMBL5187501 | — | — | 1 | 7.99 |
| CHEMBL5189470 | — | — | 1 | 7.92 |
| CHEMBL5180268 | — | — | 1 | 7.87 |
| CHEMBL5196781 | — | — | 1 | 7.64 |
| CHEMBL88147 | — | — | 1 | 7.32 |
| CHEMBL5181728 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL464859 | NECA | IC50 | = | 1.122 | nM | 8.95 |
| CHEMBL5174600 | — | IC50 | = | 1.413 | nM | 8.85 |
| CHEMBL3929143 | — | IC50 | = | 1.905 | nM | 8.72 |
| CHEMBL5180010 | — | IC50 | = | 2.63 | nM | 8.58 |
| CHEMBL3929812 | — | IC50 | = | 2.884 | nM | 8.54 |
| CHEMBL5173159 | — | IC50 | = | 3.236 | nM | 8.49 |
| CHEMBL5185003 | — | IC50 | = | 3.89 | nM | 8.41 |
| CHEMBL5189274 | — | IC50 | = | 4.677 | nM | 8.33 |
| CHEMBL5186062 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL3927012 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL5201810 | — | IC50 | = | 6.918 | nM | 8.16 |
| CHEMBL5187501 | — | IC50 | = | 10.23 | nM | 7.99 |
| CHEMBL5189470 | — | IC50 | = | 12.02 | nM | 7.92 |
| CHEMBL5180268 | — | IC50 | = | 13.49 | nM | 7.87 |
| CHEMBL5196781 | — | IC50 | = | 22.91 | nM | 7.64 |
| CHEMBL88147 | — | IC50 | = | 47.86 | nM | 7.32 |
| CHEMBL5181728 | — | IC50 | = | 199.53 | nM | 6.70 |