Assay Detail
Binding
CHEMBL639427
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Binding affinity against adenosine A1 receptor in rat cerebral cortex membrane by radioligand binding assay using [3H](R)-PIA.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
6-phenyl-1,4-dihydropyridine derivatives as potent and selective A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 4.95 | 5.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL143384 | — | — | 1 | 5.92 |
| CHEMBL108753 | — | — | 1 | 5.60 |
| CHEMBL193 | NIFEDIPINE | 4.0 | 1 | 5.54 |
| CHEMBL142868 | — | — | 1 | 5.33 |
| CHEMBL143019 | — | — | 1 | 5.26 |
| CHEMBL315984 | — | — | 1 | 5.23 |
| CHEMBL139931 | — | — | 1 | 5.22 |
| CHEMBL100646 | — | — | 1 | 5.19 |
| CHEMBL325983 | — | — | 1 | 5.13 |
| CHEMBL341839 | — | — | 1 | 5.12 |
| CHEMBL99744 | — | — | 1 | 5.12 |
| CHEMBL142262 | — | — | 1 | 5.02 |
| CHEMBL315458 | — | — | 1 | 4.96 |
| CHEMBL108797 | — | — | 1 | 4.94 |
| CHEMBL140693 | — | — | 1 | 4.88 |
| CHEMBL2112831 | — | — | 1 | 4.86 |
| CHEMBL140513 | — | — | 1 | 4.83 |
| CHEMBL2112411 | — | — | 1 | 4.79 |
| CHEMBL142226 | — | — | 1 | 4.71 |
| CHEMBL105764 | — | — | 1 | 4.67 |
| CHEMBL315168 | — | — | 1 | 4.64 |
| CHEMBL141291 | — | — | 1 | 4.60 |
| CHEMBL100071 | — | — | 1 | 4.59 |
| CHEMBL337552 | — | — | 1 | 4.58 |
| CHEMBL419306 | — | — | 1 | 4.51 |
| CHEMBL103404 | — | — | 1 | 4.49 |
| CHEMBL344284 | — | — | 1 | 4.48 |
| CHEMBL89852 | — | — | 1 | 4.40 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL143384 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL108753 | — | Ki | = | 2490.0 | nM | 5.60 |
| CHEMBL193 | NIFEDIPINE | Ki | = | 2890.0 | nM | 5.54 |
| CHEMBL142868 | — | Ki | = | 4650.0 | nM | 5.33 |
| CHEMBL143019 | — | Ki | = | 5490.0 | nM | 5.26 |
| CHEMBL315984 | — | Ki | = | 5930.0 | nM | 5.23 |
| CHEMBL139931 | — | Ki | = | 6030.0 | nM | 5.22 |
| CHEMBL100646 | — | Ki | = | 6450.0 | nM | 5.19 |
| CHEMBL325983 | — | Ki | = | 7410.0 | nM | 5.13 |
| CHEMBL341839 | — | Ki | = | 7520.0 | nM | 5.12 |
| CHEMBL99744 | — | Ki | = | 7520.0 | nM | 5.12 |
| CHEMBL142262 | — | Ki | = | 9490.0 | nM | 5.02 |
| CHEMBL315458 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL108797 | — | Ki | = | 11600.0 | nM | 4.94 |
| CHEMBL140693 | — | Ki | = | 13100.0 | nM | 4.88 |
| CHEMBL2112831 | — | Ki | = | 13700.0 | nM | 4.86 |
| CHEMBL140513 | — | Ki | = | 14900.0 | nM | 4.83 |
| CHEMBL2112411 | — | Ki | = | 16100.0 | nM | 4.79 |
| CHEMBL142226 | — | Ki | = | 19600.0 | nM | 4.71 |
| CHEMBL105764 | — | Ki | = | 21500.0 | nM | 4.67 |
| CHEMBL315168 | — | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL141291 | — | Ki | = | 25300.0 | nM | 4.60 |
| CHEMBL100071 | — | Ki | = | 25900.0 | nM | 4.59 |
| CHEMBL337552 | — | Ki | = | 26000.0 | nM | 4.58 |
| CHEMBL419306 | — | Ki | = | 31000.0 | nM | 4.51 |
| CHEMBL103404 | — | Ki | = | 32600.0 | nM | 4.49 |
| CHEMBL344284 | — | Ki | = | 33000.0 | nM | 4.48 |
| CHEMBL89852 | — | Ki | = | 40100.0 | nM | 4.40 |
| CHEMBL405355 | NIGULDIPINE | Ki | > | 100000.0 | nM | - |