Assay Detail
Binding
CHEMBL4682727
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]CCPA from adenosine receptor A1 in rat brain cortex membranes incubated for 90 mins by radioligand competition assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cortex |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Substituted 4-phenylthiazoles: Development of potent and selective A, A and dual A/A adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 7.85 | 9.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1316674 | — | — | 1 | 9.91 |
| CHEMBL52333 | ROLOFYLLINE | 3.0 | 1 | 9.72 |
| CHEMBL4796077 | — | — | 1 | 9.46 |
| CHEMBL4797181 | — | — | 1 | 9.28 |
| CHEMBL4764086 | — | — | 1 | 9.03 |
| CHEMBL4795542 | — | — | 1 | 9.00 |
| CHEMBL4755914 | — | — | 1 | 8.83 |
| CHEMBL4790122 | — | — | 1 | 8.75 |
| CHEMBL4784975 | — | — | 1 | 8.55 |
| CHEMBL4779033 | — | — | 1 | 8.46 |
| CHEMBL4797325 | — | — | 1 | 8.18 |
| CHEMBL1625681 | — | — | 1 | 6.36 |
| CHEMBL1562432 | — | — | 1 | 6.09 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.85 |
| CHEMBL111545 | — | — | 1 | 4.81 |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | 4.39 |
| CHEMBL4745527 | — | — | 1 | - |
| CHEMBL4746936 | — | — | 1 | - |
| CHEMBL4763881 | — | — | 1 | - |
| CHEMBL4757397 | — | — | 1 | - |
| CHEMBL4780555 | — | — | 1 | - |
| CHEMBL4758461 | — | — | 1 | - |
| CHEMBL4752438 | — | — | 1 | - |
| CHEMBL4747947 | — | — | 1 | - |
| CHEMBL1242892 | — | — | 1 | - |
| CHEMBL1242426 | — | — | 1 | - |
| CHEMBL4787673 | — | — | 1 | - |
| CHEMBL1242247 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1316674 | — | Ki | = | 0.124 | nM | 9.91 |
| CHEMBL52333 | ROLOFYLLINE | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL4796077 | — | Ki | = | 0.348 | nM | 9.46 |
| CHEMBL4797181 | — | Ki | = | 0.529 | nM | 9.28 |
| CHEMBL4764086 | — | Ki | = | 0.939 | nM | 9.03 |
| CHEMBL4795542 | — | Ki | = | 1.01 | nM | 9.00 |
| CHEMBL4755914 | — | Ki | = | 1.47 | nM | 8.83 |
| CHEMBL4790122 | — | Ki | = | 1.77 | nM | 8.75 |
| CHEMBL4784975 | — | Ki | = | 2.79 | nM | 8.55 |
| CHEMBL4779033 | — | Ki | = | 3.47 | nM | 8.46 |
| CHEMBL4797325 | — | Ki | = | 6.69 | nM | 8.18 |
| CHEMBL1625681 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL1562432 | — | Ki | = | 805.0 | nM | 6.09 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL111545 | — | Ki | = | 15600.0 | nM | 4.81 |
| CHEMBL113 | CAFFEINE | Ki | = | 41000.0 | nM | 4.39 |
| CHEMBL4745527 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4746936 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4763881 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4757397 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4780555 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4758461 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4752438 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4747947 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1242892 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1242426 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4787673 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1242247 | — | Ki | > | 1000.0 | nM | - |