Assay Detail
Functional
CHEMBL3135340
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and evaluation of N6-substituted 2-aminoadenosine-5-N-methylcarboxamides as A3 adenosine receptor agonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 19 | 6.37 | 7.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL464859 | NECA | — | 1 | 7.90 |
| CHEMBL331372 | CGS-21680 | — | 1 | 7.90 |
| CHEMBL3133079 | — | — | 1 | 7.10 |
| CHEMBL119709 | IB-MECA | — | 1 | 7.10 |
| CHEMBL3133078 | — | — | 1 | 6.60 |
| CHEMBL3133161 | — | — | 1 | 6.40 |
| CHEMBL3133151 | — | — | 1 | 6.30 |
| CHEMBL3133080 | — | — | 1 | 6.10 |
| CHEMBL3133159 | — | — | 1 | 6.10 |
| CHEMBL3133158 | — | — | 1 | 5.90 |
| CHEMBL3133157 | — | — | 1 | 5.60 |
| CHEMBL3133160 | — | — | 1 | 5.50 |
| CHEMBL3133081 | — | — | 1 | 5.40 |
| CHEMBL3133082 | — | — | 1 | 5.30 |
| CHEMBL3133153 | — | — | 1 | - |
| CHEMBL3133154 | — | — | 1 | - |
| CHEMBL3133155 | — | — | 1 | - |
| CHEMBL3133156 | — | — | 1 | - |
| CHEMBL3133152 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL464859 | NECA | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL331372 | CGS-21680 | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL3133079 | — | EC50 | = | 79.43 | nM | 7.10 |
| CHEMBL119709 | IB-MECA | EC50 | = | 79.43 | nM | 7.10 |
| CHEMBL3133078 | — | EC50 | = | 251.19 | nM | 6.60 |
| CHEMBL3133161 | — | EC50 | = | 398.11 | nM | 6.40 |
| CHEMBL3133151 | — | EC50 | = | 501.19 | nM | 6.30 |
| CHEMBL3133080 | — | EC50 | = | 794.33 | nM | 6.10 |
| CHEMBL3133159 | — | EC50 | = | 794.33 | nM | 6.10 |
| CHEMBL3133158 | — | EC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL3133157 | — | EC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL3133160 | — | EC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL3133081 | — | EC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL3133082 | — | EC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL3133153 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3133154 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3133155 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3133156 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3133152 | — | EC50 | > | 10000.0 | nM | - |