Assay Detail
Binding
CHEMBL647261
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Displacement of [3H]-CGS- 21680 binding to Adenosine A2A receptor in rat striatal membranes
31
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 31 | 4.69 | 5.56 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2063640 | — | — | 1 | 5.56 |
| CHEMBL315984 | — | — | 1 | 5.32 |
| CHEMBL101332 | — | — | 1 | 5.28 |
| CHEMBL102138 | — | — | 1 | 5.17 |
| CHEMBL100004 | — | — | 1 | 5.15 |
| CHEMBL103404 | — | — | 2 | 5.05 |
| CHEMBL99744 | — | — | 1 | 5.02 |
| CHEMBL100646 | — | — | 1 | 5.01 |
| CHEMBL100003 | — | — | 1 | 4.94 |
| CHEMBL103787 | — | — | 1 | 4.90 |
| CHEMBL1099207 | — | — | 1 | 4.74 |
| CHEMBL193 | NIFEDIPINE | 4.0 | 2 | 4.74 |
| CHEMBL39632 | — | — | 1 | 4.68 |
| CHEMBL101162 | — | — | 1 | 4.64 |
| CHEMBL475534 | NITRENDIPINE | 3.0 | 1 | 4.64 |
| CHEMBL100071 | — | — | 2 | 4.55 |
| CHEMBL105672 | — | — | 1 | 4.46 |
| CHEMBL418426 | — | — | 1 | 4.45 |
| CHEMBL103950 | — | — | 1 | 4.42 |
| CHEMBL2112340 | — | — | 1 | 4.42 |
| CHEMBL1428 | NIMODIPINE | 4.0 | 1 | 4.35 |
| CHEMBL2112411 | — | — | 1 | 4.31 |
| CHEMBL103419 | — | — | 1 | 4.25 |
| CHEMBL1484 | NICARDIPINE | 4.0 | 1 | 4.20 |
| CHEMBL102613 | — | — | 1 | 4.15 |
| CHEMBL283013 | — | — | 1 | 4.06 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | - |
| CHEMBL2051956 | DEXNIGULDIPINE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2063640 | — | Ki | = | 2740.0 | nM | 5.56 |
| CHEMBL315984 | — | Ki | = | 4770.0 | nM | 5.32 |
| CHEMBL101332 | — | Ki | = | 5270.0 | nM | 5.28 |
| CHEMBL102138 | — | Ki | = | 6710.0 | nM | 5.17 |
| CHEMBL100004 | — | Ki | = | 7100.0 | nM | 5.15 |
| CHEMBL103404 | — | Ki | = | 8960.0 | nM | 5.05 |
| CHEMBL99744 | — | Ki | = | 9560.0 | nM | 5.02 |
| CHEMBL100646 | — | Ki | = | 9720.0 | nM | 5.01 |
| CHEMBL100003 | — | Ki | = | 11500.0 | nM | 4.94 |
| CHEMBL103787 | — | Ki | = | 12700.0 | nM | 4.90 |
| CHEMBL193 | NIFEDIPINE | Ki | = | 18200.0 | nM | 4.74 |
| CHEMBL1099207 | — | Ki | = | 18200.0 | nM | 4.74 |
| CHEMBL39632 | — | Ki | = | 20700.0 | nM | 4.68 |
| CHEMBL475534 | NITRENDIPINE | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL101162 | — | Ki | = | 23100.0 | nM | 4.64 |
| CHEMBL100071 | — | Ki | = | 28400.0 | nM | 4.55 |
| CHEMBL105672 | — | Ki | = | 35100.0 | nM | 4.46 |
| CHEMBL100071 | — | Ki | = | 35900.0 | nM | 4.45 |
| CHEMBL418426 | — | Ki | = | 35600.0 | nM | 4.45 |
| CHEMBL103950 | — | Ki | = | 38000.0 | nM | 4.42 |
| CHEMBL2112340 | — | Ki | = | 38300.0 | nM | 4.42 |
| CHEMBL1428 | NIMODIPINE | Ki | = | 44300.0 | nM | 4.35 |
| CHEMBL103404 | — | Ki | = | 46100.0 | nM | 4.34 |
| CHEMBL2112411 | — | Ki | = | 49300.0 | nM | 4.31 |
| CHEMBL103419 | — | Ki | = | 56800.0 | nM | 4.25 |
| CHEMBL1484 | NICARDIPINE | Ki | = | 63800.0 | nM | 4.20 |
| CHEMBL102613 | — | Ki | = | 71000.0 | nM | 4.15 |
| CHEMBL283013 | — | Ki | = | 86300.0 | nM | 4.06 |
| CHEMBL2051956 | DEXNIGULDIPINE | Ki | - | nM | - | |
| CHEMBL193 | NIFEDIPINE | Ki | < | 10000.0 | nM | - |
| CHEMBL405355 | NIGULDIPINE | Ki | < | 10000.0 | nM | - |