Assay Detail
Binding
CHEMBL1803433
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ZM241385 from stabilized human adenosine receptor A2a expressed in HEK293 cells followed by receptor capturing on Biocore chips by SPR method
16
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Biophysical mapping of the adenosine A2A receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.71 | 9.00 |
| Kd | 8 | 7.05 | 9.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL240624 | PRELADENANT | 3.0 | 2 | 9.50 |
| CHEMBL113142 | ZM-241385 | — | 2 | 9.30 |
| CHEMBL1800358 | — | — | 2 | 9.00 |
| CHEMBL1800357 | — | — | 2 | 7.90 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | — | 2 | 7.70 |
| CHEMBL431770 | ISTRADEFYLLINE | 4.0 | 2 | 6.70 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 2 | 5.50 |
| CHEMBL113 | CAFFEINE | 4.0 | 2 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL240624 | PRELADENANT | Kd | = | 0.3162 | nM | 9.50 |
| CHEMBL113142 | ZM-241385 | Kd | = | 0.5012 | nM | 9.30 |
| CHEMBL1800358 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL240624 | PRELADENANT | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL113142 | ZM-241385 | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL1800357 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL1800358 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL431770 | ISTRADEFYLLINE | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL1800357 | — | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL431770 | ISTRADEFYLLINE | Kd | = | 1258.93 | nM | 5.90 |
| CHEMBL1355736 | THEOPHYLLINE | Kd | = | 3162.28 | nM | 5.50 |
| CHEMBL113 | CAFFEINE | Ki | = | 5011.87 | nM | 5.30 |
| CHEMBL113 | CAFFEINE | Kd | = | 25118.86 | nM | 4.60 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | > | 10000.0 | nM | - |