Assay Detail
Functional
CHEMBL4048596
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Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
17
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A Structure-Activity Relationship Study of Bitopic N6-Substituted Adenosine Derivatives as Biased Adenosine A1 Receptor Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 6.55 | 7.85 |
| pEC50 | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL464859 | NECA | — | 1 | 7.85 |
| CHEMBL4096796 | — | — | 1 | 7.19 |
| CHEMBL4101850 | — | — | 1 | 6.91 |
| CHEMBL4072009 | — | — | 1 | 6.55 |
| CHEMBL4081224 | — | — | 1 | 6.55 |
| CHEMBL4075186 | — | — | 1 | 6.48 |
| CHEMBL4089092 | — | — | 1 | 6.46 |
| CHEMBL4078771 | — | — | 1 | 6.39 |
| CHEMBL4076495 | — | — | 1 | 6.35 |
| CHEMBL4076565 | — | — | 1 | 6.35 |
| CHEMBL4104819 | — | — | 1 | 6.10 |
| CHEMBL4086624 | — | — | 1 | 6.08 |
| CHEMBL4085418 | — | — | 1 | 5.85 |
| CHEMBL4105473 | — | — | 1 | - |
| CHEMBL4063841 | — | — | 1 | - |
| CHEMBL4077152 | — | — | 1 | - |
| CHEMBL4069296 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL464859 | NECA | EC50 | = | 14.13 | nM | 7.85 |
| CHEMBL4096796 | — | EC50 | = | 64.57 | nM | 7.19 |
| CHEMBL4101850 | — | EC50 | = | 123.03 | nM | 6.91 |
| CHEMBL4072009 | — | EC50 | = | 281.84 | nM | 6.55 |
| CHEMBL4081224 | — | EC50 | = | 281.84 | nM | 6.55 |
| CHEMBL4075186 | — | EC50 | = | 331.13 | nM | 6.48 |
| CHEMBL4089092 | — | EC50 | = | 346.74 | nM | 6.46 |
| CHEMBL4078771 | — | EC50 | = | 407.38 | nM | 6.39 |
| CHEMBL4076495 | — | EC50 | = | 446.68 | nM | 6.35 |
| CHEMBL4076565 | — | EC50 | = | 446.68 | nM | 6.35 |
| CHEMBL4104819 | — | EC50 | = | 794.33 | nM | 6.10 |
| CHEMBL4086624 | — | EC50 | = | 831.76 | nM | 6.08 |
| CHEMBL4085418 | — | EC50 | = | 1412.54 | nM | 5.85 |
| CHEMBL4105473 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL4063841 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL4077152 | — | pEC50 | - | — | - | |
| CHEMBL4069296 | — | pEC50 | - | — | - |