Assay Detail
Binding
CHEMBL828973
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Binding affinity against Adenosine A2a receptor from rat brain tissue was determined using [3H]ZM-241385 as radioligand
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Studies on adenosine A2a receptor antagonists: comparison of three core heterocycles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 7.26 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL174628 | — | — | 1 | 8.40 |
| CHEMBL360840 | — | — | 1 | 8.22 |
| CHEMBL183531 | — | — | 1 | 8.00 |
| CHEMBL360166 | — | — | 1 | 7.96 |
| CHEMBL353323 | — | — | 1 | 7.92 |
| CHEMBL435099 | — | — | 1 | 7.75 |
| CHEMBL184411 | — | — | 1 | 7.72 |
| CHEMBL177459 | — | — | 1 | 7.60 |
| CHEMBL17127 | SCH-58261 | — | 1 | 7.43 |
| CHEMBL426782 | — | — | 1 | 7.43 |
| CHEMBL359641 | — | — | 1 | 7.41 |
| CHEMBL186562 | — | — | 1 | 7.36 |
| CHEMBL184002 | — | — | 1 | 7.24 |
| CHEMBL177386 | — | — | 1 | 7.22 |
| CHEMBL362310 | — | — | 1 | 7.10 |
| CHEMBL182505 | — | — | 1 | 7.00 |
| CHEMBL184233 | — | — | 1 | 6.95 |
| CHEMBL185497 | — | — | 1 | 6.90 |
| CHEMBL363235 | — | — | 1 | 6.83 |
| CHEMBL187058 | — | — | 1 | 6.73 |
| CHEMBL184602 | — | — | 1 | 6.72 |
| CHEMBL182754 | — | — | 1 | 6.51 |
| CHEMBL186960 | — | — | 1 | 6.44 |
| CHEMBL186594 | — | — | 1 | 6.40 |
| CHEMBL362743 | — | — | 1 | 6.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL174628 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL360840 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL183531 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL360166 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL353323 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL435099 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL184411 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL177459 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL17127 | SCH-58261 | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL426782 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL359641 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL186562 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL184002 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL177386 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL362310 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL182505 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL184233 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL185497 | — | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL363235 | — | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL187058 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL184602 | — | Ki | = | 192.0 | nM | 6.72 |
| CHEMBL182754 | — | Ki | = | 312.0 | nM | 6.51 |
| CHEMBL186960 | — | Ki | = | 366.0 | nM | 6.44 |
| CHEMBL186594 | — | Ki | = | 397.0 | nM | 6.40 |
| CHEMBL362743 | — | Ki | = | 659.0 | nM | 6.18 |