Assay Detail
Binding
CHEMBL883651
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards human Adenosine A2a receptor expressed in HEK293 cells using 6 nM [3H]CGS-21680
14
Total Activities
14
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
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 | 7.59 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL113142 | ZM-241385 | — | 1 | 10.00 |
| CHEMBL431770 | ISTRADEFYLLINE | 4.0 | 1 | 8.66 |
| CHEMBL196258 | — | — | 1 | 8.48 |
| CHEMBL196259 | — | — | 1 | 8.33 |
| CHEMBL197669 | ST1535 | 1.0 | 1 | 8.18 |
| CHEMBL194728 | — | — | 1 | 7.33 |
| CHEMBL198200 | — | — | 1 | 7.29 |
| CHEMBL1204225 | — | — | 1 | 7.29 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 7.25 |
| CHEMBL194290 | — | — | 1 | 7.15 |
| CHEMBL198942 | — | — | 1 | 7.08 |
| CHEMBL197682 | — | — | 1 | 6.92 |
| CHEMBL195001 | — | — | 1 | 6.32 |
| CHEMBL68500 | ALLOXAZINE | — | 1 | 6.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL113142 | ZM-241385 | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL431770 | ISTRADEFYLLINE | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL196258 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL196259 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL197669 | ST1535 | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL194728 | — | Ki | = | 46.3 | nM | 7.33 |
| CHEMBL198200 | — | Ki | = | 51.6 | nM | 7.29 |
| CHEMBL1204225 | — | Ki | = | 51.3 | nM | 7.29 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL194290 | — | Ki | = | 70.4 | nM | 7.15 |
| CHEMBL198942 | — | Ki | = | 83.7 | nM | 7.08 |
| CHEMBL197682 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL195001 | — | Ki | = | 481.3 | nM | 6.32 |
| CHEMBL68500 | ALLOXAZINE | Ki | = | 935.0 | nM | 6.03 |