Assay Detail
Binding
CHEMBL644313
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]- DPCPX binding at human Adenosine A1 receptor expressed in CHO cells
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design, synthesis, and biological evaluation of C9- and C2-substituted pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 7.03 | 8.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281129 | — | — | 1 | 8.08 |
| CHEMBL280888 | — | — | 1 | 8.05 |
| CHEMBL21541 | — | — | 1 | 7.52 |
| CHEMBL544678 | — | — | 1 | 7.39 |
| CHEMBL553587 | — | — | 1 | 7.32 |
| CHEMBL20888 | — | — | 1 | 7.30 |
| CHEMBL22113 | — | — | 1 | 7.16 |
| CHEMBL21572 | — | — | 1 | 7.16 |
| CHEMBL21910 | — | — | 1 | 7.10 |
| CHEMBL554955 | — | — | 1 | 7.00 |
| CHEMBL22085 | — | — | 1 | 6.87 |
| CHEMBL20555 | — | — | 1 | 6.82 |
| CHEMBL20445 | — | — | 1 | 6.76 |
| CHEMBL280411 | — | — | 1 | 6.63 |
| CHEMBL20681 | — | — | 1 | 6.58 |
| CHEMBL283319 | — | — | 1 | 6.50 |
| CHEMBL283572 | — | — | 1 | 6.18 |
| CHEMBL439447 | — | — | 1 | 6.11 |
| CHEMBL21943 | — | — | 1 | - |
| CHEMBL278541 | — | — | 1 | - |
| CHEMBL21654 | — | — | 1 | - |
| CHEMBL21434 | — | — | 1 | - |
| CHEMBL20795 | — | — | 1 | - |
| CHEMBL281372 | — | — | 1 | - |
| CHEMBL278331 | — | — | 1 | - |
| CHEMBL279975 | — | — | 1 | - |
| CHEMBL21550 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281129 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL280888 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL21541 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL544678 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL553587 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL20888 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL22113 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL21572 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL21910 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL554955 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL22085 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL20555 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL20445 | — | Ki | = | 175.0 | nM | 6.76 |
| CHEMBL280411 | — | Ki | = | 235.0 | nM | 6.63 |
| CHEMBL20681 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL283319 | — | Ki | = | 316.0 | nM | 6.50 |
| CHEMBL283572 | — | Ki | = | 666.0 | nM | 6.18 |
| CHEMBL439447 | — | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL21943 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL278541 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL21654 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL21434 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL20795 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL281372 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL278331 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL279975 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL21550 | — | Ki | > | 1000.0 | nM | - |