Assay Detail
Functional
CHEMBL4048593
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Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
17
Total Activities
17
Compounds Tested
1
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 | 17 | 7.00 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL464859 | NECA | — | 1 | 7.80 |
| CHEMBL4086624 | — | — | 1 | 7.75 |
| CHEMBL4077152 | — | — | 1 | 7.73 |
| CHEMBL4101850 | — | — | 1 | 7.45 |
| CHEMBL4096796 | — | — | 1 | 7.22 |
| CHEMBL4063841 | — | — | 1 | 7.20 |
| CHEMBL4085418 | — | — | 1 | 7.12 |
| CHEMBL4089092 | — | — | 1 | 7.04 |
| CHEMBL4104819 | — | — | 1 | 7.02 |
| CHEMBL4069296 | — | — | 1 | 7.01 |
| CHEMBL4105473 | — | — | 1 | 6.83 |
| CHEMBL4078771 | — | — | 1 | 6.80 |
| CHEMBL4076495 | — | — | 1 | 6.65 |
| CHEMBL4072009 | — | — | 1 | 6.54 |
| CHEMBL4081224 | — | — | 1 | 6.35 |
| CHEMBL4075186 | — | — | 1 | 6.33 |
| CHEMBL4076565 | — | — | 1 | 6.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL464859 | NECA | EC50 | = | 15.85 | nM | 7.80 |
| CHEMBL4086624 | — | EC50 | = | 17.78 | nM | 7.75 |
| CHEMBL4077152 | — | EC50 | = | 18.62 | nM | 7.73 |
| CHEMBL4101850 | — | EC50 | = | 35.48 | nM | 7.45 |
| CHEMBL4096796 | — | EC50 | = | 60.26 | nM | 7.22 |
| CHEMBL4063841 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4085418 | — | EC50 | = | 75.86 | nM | 7.12 |
| CHEMBL4089092 | — | EC50 | = | 91.2 | nM | 7.04 |
| CHEMBL4104819 | — | EC50 | = | 95.5 | nM | 7.02 |
| CHEMBL4069296 | — | EC50 | = | 97.72 | nM | 7.01 |
| CHEMBL4105473 | — | EC50 | = | 147.91 | nM | 6.83 |
| CHEMBL4078771 | — | EC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4076495 | — | EC50 | = | 223.87 | nM | 6.65 |
| CHEMBL4072009 | — | EC50 | = | 288.4 | nM | 6.54 |
| CHEMBL4081224 | — | EC50 | = | 446.68 | nM | 6.35 |
| CHEMBL4075186 | — | EC50 | = | 467.74 | nM | 6.33 |
| CHEMBL4076565 | — | EC50 | = | 616.6 | nM | 6.21 |