Assay Detail
Binding
CHEMBL830246
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Displacement of [125I]-AB MECA from recombinant human adenosine A3 receptor expressed in HEK cells
26
Total Activities
26
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 | 26 | 7.71 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL119709 | IB-MECA | — | 1 | 8.96 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 8.85 |
| CHEMBL361072 | — | — | 1 | 8.70 |
| CHEMBL186443 | — | — | 1 | 8.70 |
| CHEMBL398587 | — | — | 1 | 8.70 |
| CHEMBL183940 | — | — | 1 | 8.52 |
| CHEMBL574597 | — | — | 1 | 8.47 |
| CHEMBL361938 | — | — | 1 | 8.22 |
| CHEMBL365642 | — | — | 1 | 8.00 |
| CHEMBL231677 | — | — | 1 | 7.82 |
| CHEMBL375190 | — | — | 1 | 7.80 |
| CHEMBL189069 | — | — | 1 | 7.72 |
| CHEMBL400414 | — | — | 1 | 7.39 |
| CHEMBL188454 | — | — | 1 | 7.31 |
| CHEMBL188482 | — | — | 1 | 7.22 |
| CHEMBL234790 | — | — | 1 | 7.14 |
| CHEMBL359991 | — | — | 1 | 7.01 |
| CHEMBL231891 | — | — | 1 | 6.97 |
| CHEMBL363458 | — | — | 1 | 6.96 |
| CHEMBL187300 | — | — | 1 | 6.83 |
| CHEMBL184557 | — | — | 1 | 6.80 |
| CHEMBL362117 | — | — | 1 | 6.77 |
| CHEMBL361075 | — | — | 1 | 6.50 |
| CHEMBL98278 | — | — | 1 | - |
| CHEMBL318928 | — | — | 1 | - |
| CHEMBL317052 | REGADENOSON ANHYDROUS | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL119709 | IB-MECA | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL361072 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL186443 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL398587 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL183940 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL574597 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL361938 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL365642 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL231677 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL375190 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL189069 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL400414 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL188454 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL188482 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL234790 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL359991 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL231891 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL363458 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL187300 | — | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL184557 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL362117 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL361075 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL98278 | — | Ki | > | 10.0 | nM | - |
| CHEMBL318928 | — | Ki | > | 6.0 | nM | - |
| CHEMBL317052 | REGADENOSON ANHYDROUS | Ki | > | 10.0 | nM | - |