Assay Detail
Functional
CHEMBL903246
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human adenosine A2A receptor
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
3H-[1,2,4]-Triazolo[5,1-i]purin-5-amine derivatives as adenosine A2A antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 8.68 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL245848 | — | — | 1 | 10.00 |
| CHEMBL246055 | — | — | 1 | 9.52 |
| CHEMBL391953 | — | — | 1 | 9.40 |
| CHEMBL246261 | — | — | 1 | 9.40 |
| CHEMBL246053 | — | — | 1 | 9.15 |
| CHEMBL246054 | — | — | 1 | 9.15 |
| CHEMBL245849 | — | — | 1 | 9.10 |
| CHEMBL395472 | — | — | 1 | 9.05 |
| CHEMBL246467 | — | — | 1 | 9.05 |
| CHEMBL392168 | — | — | 1 | 9.05 |
| CHEMBL392169 | — | — | 1 | 9.00 |
| CHEMBL246262 | — | — | 1 | 8.85 |
| CHEMBL245645 | — | — | 1 | 8.82 |
| CHEMBL246263 | — | — | 1 | 8.77 |
| CHEMBL248300 | — | — | 1 | 8.77 |
| CHEMBL245847 | — | — | 1 | 8.77 |
| CHEMBL246469 | — | — | 1 | 8.70 |
| CHEMBL246468 | — | — | 1 | 8.43 |
| CHEMBL398046 | — | — | 1 | 8.39 |
| CHEMBL245646 | — | — | 1 | 8.34 |
| CHEMBL398083 | — | — | 1 | 8.34 |
| CHEMBL248298 | — | — | 1 | 8.23 |
| CHEMBL248299 | — | — | 1 | 8.20 |
| CHEMBL246673 | — | — | 1 | 8.03 |
| CHEMBL247900 | — | — | 1 | 8.00 |
| CHEMBL246675 | — | — | 1 | 7.90 |
| CHEMBL246674 | — | — | 1 | 7.69 |
| CHEMBL392386 | — | — | 1 | 7.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL245848 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL246055 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL391953 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL246261 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL246053 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL246054 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL245849 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL395472 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL246467 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL392168 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL392169 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL246262 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL245645 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL246263 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL248300 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL245847 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL246469 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL246468 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL398046 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL245646 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL398083 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL248298 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL248299 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL246673 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL247900 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL246675 | — | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL246674 | — | Ki | = | 20.5 | nM | 7.69 |
| CHEMBL392386 | — | Ki | = | 89.7 | nM | 7.05 |