Assay Detail
Binding
CHEMBL871844
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards human Adenosine A1 receptor expressed in CHO cells using 1 nM [3H]DPCPX
14
Total Activities
14
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
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 7.14 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL194728 | — | — | 1 | 9.40 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 8.19 |
| CHEMBL194290 | — | — | 1 | 7.98 |
| CHEMBL196258 | — | — | 1 | 7.58 |
| CHEMBL197669 | ST1535 | 1.0 | 1 | 7.14 |
| CHEMBL196259 | — | — | 1 | 7.10 |
| CHEMBL198942 | — | — | 1 | 6.58 |
| CHEMBL113142 | ZM-241385 | — | 1 | 6.51 |
| CHEMBL197682 | — | — | 1 | 6.47 |
| CHEMBL198200 | — | — | 1 | 5.98 |
| CHEMBL195001 | — | — | 1 | 5.64 |
| CHEMBL1204225 | — | — | 1 | - |
| CHEMBL68500 | ALLOXAZINE | — | 1 | - |
| CHEMBL431770 | ISTRADEFYLLINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL194728 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL194290 | — | Ki | = | 10.4 | nM | 7.98 |
| CHEMBL196258 | — | Ki | = | 26.2 | nM | 7.58 |
| CHEMBL197669 | ST1535 | Ki | = | 71.8 | nM | 7.14 |
| CHEMBL196259 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL198942 | — | Ki | = | 266.0 | nM | 6.58 |
| CHEMBL113142 | ZM-241385 | Ki | = | 307.9 | nM | 6.51 |
| CHEMBL197682 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL198200 | — | Ki | = | 1056.3 | nM | 5.98 |
| CHEMBL195001 | — | Ki | = | 2270.0 | nM | 5.64 |
| CHEMBL1204225 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL68500 | ALLOXAZINE | Ki | > | 100000.0 | nM | - |
| CHEMBL431770 | ISTRADEFYLLINE | Ki | > | 1000.0 | nM | - |