Assay Detail
Binding
CHEMBL643209
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Displacement of [3H]ZM-241385 from human adenosine A2A receptors expressed in HEK293 cells
12
Total Activities
12
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
Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as adenosine receptor antagonists. Influence of the N5 substituent on the affinity at the human A 3 and A 2B adenosine receptor subtypes: a molecular modeling investigation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.24 | 9.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL16867 | — | — | 1 | 9.51 |
| CHEMBL435022 | — | — | 1 | 7.42 |
| CHEMBL341777 | — | — | 1 | 7.40 |
| CHEMBL336217 | — | — | 1 | 7.38 |
| CHEMBL138593 | — | — | 1 | 7.35 |
| CHEMBL135719 | — | — | 1 | 7.26 |
| CHEMBL132806 | — | — | 1 | 7.24 |
| CHEMBL134566 | — | — | 1 | 7.22 |
| CHEMBL541455 | — | — | 1 | 7.22 |
| CHEMBL324735 | — | — | 1 | 6.42 |
| CHEMBL341376 | — | — | 1 | 6.37 |
| CHEMBL335950 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL16867 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL435022 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL341777 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL336217 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL138593 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL135719 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL132806 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL134566 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL541455 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL324735 | — | Ki | = | 381.0 | nM | 6.42 |
| CHEMBL341376 | — | Ki | = | 423.0 | nM | 6.37 |
| CHEMBL335950 | — | Ki | = | 800.0 | nM | 6.10 |