Assay Detail
Binding
CHEMBL876372
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Displacement of [3H]CGS-21680 from recombinant human adenosine A2a receptor expressed in HEK cells
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
2-Pyrazolyl-N(6)-substituted adenosine derivatives as high affinity and selective adenosine A(3) receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 6.12 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL98278 | — | — | 1 | 8.82 |
| CHEMBL363458 | — | — | 1 | 7.28 |
| CHEMBL119709 | IB-MECA | — | 1 | 7.25 |
| CHEMBL318928 | — | — | 1 | 6.72 |
| CHEMBL317052 | REGADENOSON ANHYDROUS | 4.0 | 1 | 6.53 |
| CHEMBL375190 | — | — | 1 | 6.44 |
| CHEMBL231891 | — | — | 1 | 5.75 |
| CHEMBL361072 | — | — | 1 | 5.60 |
| CHEMBL188482 | — | — | 1 | 5.48 |
| CHEMBL184557 | — | — | 1 | 5.40 |
| CHEMBL361075 | — | — | 1 | 5.40 |
| CHEMBL400414 | — | — | 1 | 5.40 |
| CHEMBL186443 | — | — | 1 | 5.39 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 5.27 |
| CHEMBL574597 | — | — | 1 | 5.07 |
| CHEMBL365642 | — | — | 1 | - |
| CHEMBL361938 | — | — | 1 | - |
| CHEMBL398587 | — | — | 1 | - |
| CHEMBL231677 | — | — | 1 | - |
| CHEMBL362117 | — | — | 1 | - |
| CHEMBL183940 | — | — | 1 | - |
| CHEMBL189069 | — | — | 1 | - |
| CHEMBL234790 | — | — | 1 | - |
| CHEMBL359991 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL98278 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL363458 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL119709 | IB-MECA | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL318928 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL317052 | REGADENOSON ANHYDROUS | Ki | = | 297.0 | nM | 6.53 |
| CHEMBL375190 | — | Ki | = | 363.0 | nM | 6.44 |
| CHEMBL231891 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL361072 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL188482 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL184557 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL361075 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL400414 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL186443 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 5360.0 | nM | 5.27 |
| CHEMBL574597 | — | Ki | = | 8530.0 | nM | 5.07 |
| CHEMBL365642 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL361938 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL398587 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL231677 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL362117 | — | Ki | > | 3900.0 | nM | - |
| CHEMBL183940 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL189069 | — | Ki | > | 4000.0 | nM | - |
| CHEMBL234790 | — | Ki | > | 6000.0 | nM | - |
| CHEMBL359991 | — | Ki | > | 5000.0 | nM | - |