Assay Detail
Functional
CHEMBL1015330
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Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
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
N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine receptor with antinociceptive effects in mice.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 5.42 | 5.56 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL449575 | — | — | 1 | 5.56 |
| CHEMBL477444 | — | — | 1 | 5.49 |
| CHEMBL477445 | — | — | 1 | 5.32 |
| CHEMBL489640 | — | — | 1 | 5.31 |
| CHEMBL514541 | — | — | 1 | - |
| CHEMBL515330 | — | — | 1 | - |
| CHEMBL478071 | — | — | 1 | - |
| CHEMBL477665 | — | — | 1 | - |
| CHEMBL514701 | — | — | 1 | - |
| CHEMBL477666 | — | — | 1 | - |
| CHEMBL477667 | — | — | 1 | - |
| CHEMBL523934 | — | — | 1 | - |
| CHEMBL489226 | — | — | 1 | - |
| CHEMBL489428 | — | — | 1 | - |
| CHEMBL489628 | — | — | 1 | - |
| CHEMBL489638 | — | — | 1 | - |
| CHEMBL522095 | — | — | 1 | - |
| CHEMBL489639 | — | — | 1 | - |
| CHEMBL490250 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL449575 | — | Ki | = | 2740.0 | nM | 5.56 |
| CHEMBL477444 | — | Ki | = | 3210.0 | nM | 5.49 |
| CHEMBL477445 | — | Ki | = | 4830.0 | nM | 5.32 |
| CHEMBL489640 | — | Ki | = | 4930.0 | nM | 5.31 |
| CHEMBL514541 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL515330 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL478071 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL477665 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL514701 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL477666 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL477667 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL523934 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL489226 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL489428 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL489628 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL489638 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL522095 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL489639 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL490250 | — | Ki | > | 10000.0 | nM | - |