Assay Detail
Functional
CHEMBL5111994
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at wild type A3R (unknown origin) expressed in Flp-In-CHO 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 | Flp-In-CHO |
| 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 | 8.31 | 10.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL88147 | — | — | 1 | 10.01 |
| CHEMBL464859 | NECA | — | 1 | 9.03 |
| CHEMBL5187501 | — | — | 1 | 8.71 |
| CHEMBL5189274 | — | — | 1 | 8.56 |
| CHEMBL3927012 | — | — | 1 | 8.55 |
| CHEMBL5201810 | — | — | 1 | 8.52 |
| CHEMBL5173159 | — | — | 1 | 8.42 |
| CHEMBL5174600 | — | — | 1 | 8.37 |
| CHEMBL5196781 | — | — | 1 | 8.31 |
| CHEMBL3929143 | — | — | 1 | 8.29 |
| CHEMBL5186062 | — | — | 1 | 8.17 |
| CHEMBL5185003 | — | — | 1 | 8.14 |
| CHEMBL5189470 | — | — | 1 | 8.05 |
| CHEMBL5180010 | — | — | 1 | 7.91 |
| CHEMBL3929812 | — | — | 1 | 7.91 |
| CHEMBL5180268 | — | — | 1 | 7.22 |
| CHEMBL5181728 | — | — | 1 | 7.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL88147 | — | IC50 | = | 0.09772 | nM | 10.01 |
| CHEMBL464859 | NECA | IC50 | = | 0.9333 | nM | 9.03 |
| CHEMBL5187501 | — | IC50 | = | 1.95 | nM | 8.71 |
| CHEMBL5189274 | — | IC50 | = | 2.754 | nM | 8.56 |
| CHEMBL3927012 | — | IC50 | = | 2.818 | nM | 8.55 |
| CHEMBL5201810 | — | IC50 | = | 3.02 | nM | 8.52 |
| CHEMBL5173159 | — | IC50 | = | 3.802 | nM | 8.42 |
| CHEMBL5174600 | — | IC50 | = | 4.266 | nM | 8.37 |
| CHEMBL5196781 | — | IC50 | = | 4.898 | nM | 8.31 |
| CHEMBL3929143 | — | IC50 | = | 5.129 | nM | 8.29 |
| CHEMBL5186062 | — | IC50 | = | 6.761 | nM | 8.17 |
| CHEMBL5185003 | — | IC50 | = | 7.244 | nM | 8.14 |
| CHEMBL5189470 | — | IC50 | = | 8.913 | nM | 8.05 |
| CHEMBL5180010 | — | IC50 | = | 12.3 | nM | 7.91 |
| CHEMBL3929812 | — | IC50 | = | 12.3 | nM | 7.91 |
| CHEMBL5180268 | — | IC50 | = | 60.26 | nM | 7.22 |
| CHEMBL5181728 | — | IC50 | = | 75.86 | nM | 7.12 |