Assay Detail
Binding
CHEMBL640535
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Receptor binding affinity for the adenosine A2A receptor were determined using [3H]ZM-241385 as a radioligand in pig
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| 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 | 5.91 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL98659 | — | — | 1 | 6.92 |
| CHEMBL99169 | — | — | 1 | 6.42 |
| CHEMBL329712 | — | — | 1 | 6.42 |
| CHEMBL415118 | — | — | 1 | 6.36 |
| CHEMBL98597 | — | — | 1 | 6.31 |
| CHEMBL318928 | — | — | 1 | 6.25 |
| CHEMBL97937 | — | — | 1 | 6.15 |
| CHEMBL99983 | — | — | 1 | 6.06 |
| CHEMBL318732 | — | — | 1 | 6.01 |
| CHEMBL317052 | REGADENOSON ANHYDROUS | 4.0 | 1 | 5.95 |
| CHEMBL318483 | — | — | 1 | 5.95 |
| CHEMBL101218 | — | — | 1 | 5.89 |
| CHEMBL101383 | — | — | 1 | 5.87 |
| CHEMBL98278 | — | — | 1 | 5.80 |
| CHEMBL100348 | — | — | 1 | 5.78 |
| CHEMBL319608 | — | — | 1 | 5.77 |
| CHEMBL102035 | — | — | 1 | 5.67 |
| CHEMBL98802 | — | — | 1 | 5.62 |
| CHEMBL99052 | — | — | 1 | 5.46 |
| CHEMBL101663 | — | — | 1 | 5.23 |
| CHEMBL100876 | — | — | 1 | 5.17 |
| CHEMBL98221 | — | — | 1 | 5.00 |
| CHEMBL98958 | — | — | 1 | - |
| CHEMBL316729 | — | — | 1 | - |
| CHEMBL328642 | — | — | 1 | - |
| CHEMBL100992 | — | — | 1 | - |
| CHEMBL98849 | — | — | 1 | - |
| CHEMBL99554 | — | — | 1 | - |
| CHEMBL319949 | — | — | 1 | - |
| CHEMBL443495 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL98659 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL99169 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL329712 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL415118 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL98597 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL318928 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL97937 | — | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL99983 | — | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL318732 | — | Ki | = | 980.0 | nM | 6.01 |
| CHEMBL317052 | REGADENOSON ANHYDROUS | Ki | = | 1120.0 | nM | 5.95 |
| CHEMBL318483 | — | Ki | = | 1120.0 | nM | 5.95 |
| CHEMBL101218 | — | Ki | = | 1280.0 | nM | 5.89 |
| CHEMBL101383 | — | Ki | = | 1350.0 | nM | 5.87 |
| CHEMBL98278 | — | Ki | = | 1580.0 | nM | 5.80 |
| CHEMBL100348 | — | Ki | = | 1660.0 | nM | 5.78 |
| CHEMBL319608 | — | Ki | = | 1710.0 | nM | 5.77 |
| CHEMBL102035 | — | Ki | = | 2140.0 | nM | 5.67 |
| CHEMBL98802 | — | Ki | = | 2420.0 | nM | 5.62 |
| CHEMBL99052 | — | Ki | = | 3430.0 | nM | 5.46 |
| CHEMBL101663 | — | Ki | = | 5900.0 | nM | 5.23 |
| CHEMBL100876 | — | Ki | = | 6680.0 | nM | 5.17 |
| CHEMBL98221 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL317053 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL98023 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL98973 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL318264 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL100513 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL443495 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL319949 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL99554 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL98849 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL100992 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL328642 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL316729 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL98958 | — | Ki | > | 100000.0 | nM | - |