Assay Detail
Binding
CHEMBL644311
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DPCPX from human Adenosine A1 receptor expressed in CHO cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.13 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL16867 | — | — | 1 | 9.00 |
| CHEMBL423542 | — | — | 1 | 8.52 |
| CHEMBL137879 | — | — | 1 | 8.30 |
| CHEMBL344706 | — | — | 1 | 8.00 |
| CHEMBL138332 | — | — | 1 | 7.52 |
| CHEMBL422820 | — | — | 1 | 6.70 |
| CHEMBL137950 | — | — | 1 | 6.60 |
| CHEMBL141154 | — | — | 1 | 6.60 |
| CHEMBL139182 | — | — | 1 | 6.60 |
| CHEMBL65271 | — | — | 1 | 5.99 |
| CHEMBL302765 | — | — | 1 | 5.92 |
| CHEMBL342906 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL16867 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL423542 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL137879 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL344706 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL138332 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL422820 | — | Ki | = | 201.0 | nM | 6.70 |
| CHEMBL137950 | — | Ki | = | 251.0 | nM | 6.60 |
| CHEMBL141154 | — | Ki | = | 249.0 | nM | 6.60 |
| CHEMBL139182 | — | Ki | = | 251.0 | nM | 6.60 |
| CHEMBL65271 | — | Ki | = | 1026.0 | nM | 5.99 |
| CHEMBL302765 | — | Ki | = | 1197.0 | nM | 5.92 |
| CHEMBL342906 | — | Ki | = | 1500.0 | nM | 5.82 |