Assay Detail
Binding
CHEMBL4041943
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Displacement of [3H]DPCPX from adenosine receptor A1 in rat brain membrane
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Selected C8 two-chain linkers enhance the adenosine A1/A2A receptor affinity and selectivity of caffeine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 4.95 | 5.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL602259 | — | — | 1 | 5.82 |
| CHEMBL1927666 | — | — | 1 | 5.37 |
| CHEMBL2088309 | — | — | 1 | 5.31 |
| CHEMBL2088306 | — | — | 1 | 5.12 |
| CHEMBL1451750 | — | — | 1 | 5.10 |
| CHEMBL1806759 | — | — | 1 | 4.76 |
| CHEMBL2088316 | — | — | 1 | 4.68 |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | 4.36 |
| CHEMBL1927669 | — | — | 1 | 4.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL602259 | — | Ki | = | 1520.0 | nM | 5.82 |
| CHEMBL1927666 | — | Ki | = | 4320.0 | nM | 5.37 |
| CHEMBL2088309 | — | Ki | = | 4850.0 | nM | 5.31 |
| CHEMBL2088306 | — | Ki | = | 7600.0 | nM | 5.12 |
| CHEMBL1451750 | — | Ki | = | 7950.0 | nM | 5.10 |
| CHEMBL1806759 | — | Ki | = | 17380.0 | nM | 4.76 |
| CHEMBL2088316 | — | Ki | = | 20840.0 | nM | 4.68 |
| CHEMBL113 | CAFFEINE | Ki | = | 43900.0 | nM | 4.36 |
| CHEMBL1927669 | — | Ki | = | 90000.0 | nM | 4.05 |