Assay Detail
Binding
CHEMBL640587
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Receptor binding affinity for the adenosine A2A receptor was determined using [3H]ZM-241385 as a radioligand in rat
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Structure-affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A2A receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 35 | 6.43 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL319387 | — | — | 1 | 8.66 |
| CHEMBL98603 | — | — | 1 | 7.85 |
| CHEMBL98659 | — | — | 1 | 7.30 |
| CHEMBL101218 | — | — | 1 | 7.22 |
| CHEMBL329712 | — | — | 1 | 7.22 |
| CHEMBL99169 | — | — | 1 | 7.22 |
| CHEMBL102116 | — | — | 1 | 7.18 |
| CHEMBL415118 | — | — | 1 | 6.85 |
| CHEMBL318928 | — | — | 1 | 6.72 |
| CHEMBL98597 | — | — | 1 | 6.72 |
| CHEMBL97937 | — | — | 1 | 6.68 |
| CHEMBL99983 | — | — | 1 | 6.66 |
| CHEMBL317052 | REGADENOSON ANHYDROUS | 4.0 | 1 | 6.54 |
| CHEMBL318732 | — | — | 1 | 6.54 |
| CHEMBL101383 | — | — | 1 | 6.46 |
| CHEMBL318483 | — | — | 1 | 6.41 |
| CHEMBL319608 | — | — | 1 | 6.33 |
| CHEMBL99052 | — | — | 1 | 5.96 |
| CHEMBL100348 | — | — | 1 | 5.89 |
| CHEMBL98278 | — | — | 1 | 5.79 |
| CHEMBL101663 | — | — | 1 | 5.65 |
| CHEMBL102035 | — | — | 1 | 5.59 |
| CHEMBL100876 | — | — | 1 | 5.58 |
| CHEMBL98221 | — | — | 1 | 5.41 |
| CHEMBL98802 | — | — | 1 | 5.28 |
| CHEMBL98958 | — | — | 1 | 5.21 |
| CHEMBL100513 | — | — | 1 | 4.68 |
| CHEMBL99554 | — | — | 1 | - |
| CHEMBL98849 | — | — | 1 | - |
| CHEMBL319949 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL319387 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL98603 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL98659 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL101218 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL329712 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL99169 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL102116 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL415118 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL318928 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL98597 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL97937 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL99983 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL317052 | REGADENOSON ANHYDROUS | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL318732 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL101383 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL318483 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL319608 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL99052 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL100348 | — | Ki | = | 1280.0 | nM | 5.89 |
| CHEMBL98278 | — | Ki | = | 1610.0 | nM | 5.79 |
| CHEMBL101663 | — | Ki | = | 2260.0 | nM | 5.65 |
| CHEMBL102035 | — | Ki | = | 2590.0 | nM | 5.59 |
| CHEMBL100876 | — | Ki | = | 2620.0 | nM | 5.58 |
| CHEMBL98221 | — | Ki | = | 3880.0 | nM | 5.41 |
| CHEMBL98802 | — | Ki | = | 5290.0 | nM | 5.28 |
| CHEMBL98958 | — | Ki | = | 6110.0 | nM | 5.21 |
| CHEMBL100513 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL99554 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL98849 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL319949 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL328642 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL318264 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL316729 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL98023 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL100992 | — | Ki | > | 100000.0 | nM | - |