Assay Detail
Binding
CHEMBL1679250
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-ZM241385 from human adenosine A2A receptor expressed in high five cells after 30 mins by scintillation counting
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.22 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL240624 | PRELADENANT | 3.0 | 1 | 8.30 |
| CHEMBL1671936 | — | — | 1 | 8.23 |
| CHEMBL1671935 | — | — | 1 | 8.04 |
| CHEMBL1671938 | — | — | 1 | 7.92 |
| CHEMBL1671932 | — | — | 1 | 7.77 |
| CHEMBL1671933 | — | — | 1 | 7.72 |
| CHEMBL1671934 | — | — | 1 | 7.66 |
| CHEMBL1671923 | — | — | 1 | 7.55 |
| CHEMBL1671937 | — | — | 1 | 7.50 |
| CHEMBL1671922 | — | — | 1 | 7.44 |
| CHEMBL1671929 | — | — | 1 | 7.30 |
| CHEMBL431770 | ISTRADEFYLLINE | 4.0 | 1 | 7.14 |
| CHEMBL1671921 | — | — | 1 | 7.05 |
| CHEMBL1671928 | — | — | 1 | 6.96 |
| CHEMBL1671924 | — | — | 1 | 6.92 |
| CHEMBL1671931 | — | — | 1 | 6.75 |
| CHEMBL1671917 | — | — | 1 | 6.72 |
| CHEMBL1671930 | — | — | 1 | 6.70 |
| CHEMBL1671916 | — | — | 1 | 6.66 |
| CHEMBL1671925 | — | — | 1 | 6.66 |
| CHEMBL1671920 | — | — | 1 | 6.52 |
| CHEMBL1671918 | — | — | 1 | 6.46 |
| CHEMBL1671919 | — | — | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL240624 | PRELADENANT | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL1671936 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL1671935 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL1671938 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1671932 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL1671933 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL1671934 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL1671923 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL1671937 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL1671922 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL1671929 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL431770 | ISTRADEFYLLINE | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL1671921 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL1671928 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL1671924 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL1671931 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL1671917 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL1671930 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL1671916 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL1671925 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL1671920 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL1671918 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL1671919 | — | Ki | = | 890.0 | nM | 6.05 |