Assay Detail
ADMET
CHEMBL4048587
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Agonist activity at human A1AR expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4 dye-based fluorescence assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| 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 | 7.03 | 9.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL464859 | NECA | — | 1 | 9.36 |
| CHEMBL4076495 | — | — | 1 | 7.53 |
| CHEMBL4096796 | — | — | 1 | 7.46 |
| CHEMBL4086624 | — | — | 1 | 7.45 |
| CHEMBL4085418 | — | — | 1 | 7.25 |
| CHEMBL4063841 | — | — | 1 | 7.13 |
| CHEMBL4089092 | — | — | 1 | 7.11 |
| CHEMBL4078771 | — | — | 1 | 7.06 |
| CHEMBL4101850 | — | — | 1 | 7.03 |
| CHEMBL4081224 | — | — | 1 | 6.96 |
| CHEMBL4104819 | — | — | 1 | 6.91 |
| CHEMBL4077152 | — | — | 1 | 6.87 |
| CHEMBL4075186 | — | — | 1 | 6.70 |
| CHEMBL4069296 | — | — | 1 | 6.59 |
| CHEMBL4105473 | — | — | 1 | 6.25 |
| CHEMBL4076565 | — | — | 1 | 6.05 |
| CHEMBL4072009 | — | — | 1 | 5.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL464859 | NECA | EC50 | = | 0.4365 | nM | 9.36 |
| CHEMBL4076495 | — | EC50 | = | 29.51 | nM | 7.53 |
| CHEMBL4096796 | — | EC50 | = | 34.67 | nM | 7.46 |
| CHEMBL4086624 | — | EC50 | = | 35.48 | nM | 7.45 |
| CHEMBL4085418 | — | EC50 | = | 56.23 | nM | 7.25 |
| CHEMBL4063841 | — | EC50 | = | 74.13 | nM | 7.13 |
| CHEMBL4089092 | — | EC50 | = | 77.62 | nM | 7.11 |
| CHEMBL4078771 | — | EC50 | = | 87.1 | nM | 7.06 |
| CHEMBL4101850 | — | EC50 | = | 93.33 | nM | 7.03 |
| CHEMBL4081224 | — | EC50 | = | 109.65 | nM | 6.96 |
| CHEMBL4104819 | — | EC50 | = | 123.03 | nM | 6.91 |
| CHEMBL4077152 | — | EC50 | = | 134.9 | nM | 6.87 |
| CHEMBL4075186 | — | EC50 | = | 199.53 | nM | 6.70 |
| CHEMBL4069296 | — | EC50 | = | 257.04 | nM | 6.59 |
| CHEMBL4105473 | — | EC50 | = | 562.34 | nM | 6.25 |
| CHEMBL4076565 | — | EC50 | = | 891.25 | nM | 6.05 |
| CHEMBL4072009 | — | EC50 | = | 1348.96 | nM | 5.87 |