Assay Detail
Binding
CHEMBL649101
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Displacement of [3H](R)-PIA binding to Adenosine A1 receptor in rat brain membranes
31
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Brain membranes |
| 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 | 5.02 | 6.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL105672 | — | — | 1 | 6.11 |
| CHEMBL103787 | — | — | 1 | 5.56 |
| CHEMBL193 | NIFEDIPINE | 4.0 | 2 | 5.54 |
| CHEMBL1099207 | — | — | 1 | 5.48 |
| CHEMBL101332 | — | — | 1 | 5.44 |
| CHEMBL2112340 | — | — | 1 | 5.27 |
| CHEMBL315984 | — | — | 1 | 5.23 |
| CHEMBL100004 | — | — | 1 | 5.19 |
| CHEMBL100646 | — | — | 1 | 5.19 |
| CHEMBL283013 | — | — | 1 | 5.18 |
| CHEMBL39632 | — | — | 1 | 5.17 |
| CHEMBL103404 | — | — | 2 | 5.16 |
| CHEMBL100071 | — | — | 2 | 5.13 |
| CHEMBL99744 | — | — | 1 | 5.12 |
| CHEMBL100003 | — | — | 1 | 5.09 |
| CHEMBL102138 | — | — | 1 | 5.05 |
| CHEMBL475534 | NITRENDIPINE | 3.0 | 1 | 5.05 |
| CHEMBL101162 | — | — | 1 | 5.04 |
| CHEMBL103950 | — | — | 1 | 4.97 |
| CHEMBL2063640 | — | — | 1 | 4.96 |
| CHEMBL2112411 | — | — | 1 | 4.79 |
| CHEMBL1484 | NICARDIPINE | 4.0 | 1 | 4.71 |
| CHEMBL1428 | NIMODIPINE | 4.0 | 1 | 4.70 |
| CHEMBL2051956 | DEXNIGULDIPINE | 2.0 | 1 | 4.38 |
| CHEMBL102613 | — | — | 1 | 4.35 |
| CHEMBL103643 | — | — | 1 | 4.31 |
| CHEMBL103419 | — | — | 1 | 4.29 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL105672 | — | Ki | = | 785.0 | nM | 6.11 |
| CHEMBL103787 | — | Ki | = | 2750.0 | nM | 5.56 |
| CHEMBL193 | NIFEDIPINE | Ki | = | 2890.0 | nM | 5.54 |
| CHEMBL1099207 | — | Ki | = | 3340.0 | nM | 5.48 |
| CHEMBL101332 | — | Ki | = | 3660.0 | nM | 5.44 |
| CHEMBL2112340 | — | Ki | = | 5390.0 | nM | 5.27 |
| CHEMBL315984 | — | Ki | = | 5930.0 | nM | 5.23 |
| CHEMBL100004 | — | Ki | = | 6500.0 | nM | 5.19 |
| CHEMBL100646 | — | Ki | = | 6450.0 | nM | 5.19 |
| CHEMBL283013 | — | Ki | = | 6660.0 | nM | 5.18 |
| CHEMBL39632 | — | Ki | = | 6680.0 | nM | 5.17 |
| CHEMBL103404 | — | Ki | = | 6950.0 | nM | 5.16 |
| CHEMBL100071 | — | Ki | = | 7410.0 | nM | 5.13 |
| CHEMBL99744 | — | Ki | = | 7520.0 | nM | 5.12 |
| CHEMBL100003 | — | Ki | = | 8170.0 | nM | 5.09 |
| CHEMBL475534 | NITRENDIPINE | Ki | = | 8960.0 | nM | 5.05 |
| CHEMBL102138 | — | Ki | = | 8810.0 | nM | 5.05 |
| CHEMBL101162 | — | Ki | = | 9100.0 | nM | 5.04 |
| CHEMBL103950 | — | Ki | = | 10800.0 | nM | 4.97 |
| CHEMBL2063640 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL2112411 | — | Ki | = | 16100.0 | nM | 4.79 |
| CHEMBL1484 | NICARDIPINE | Ki | = | 19600.0 | nM | 4.71 |
| CHEMBL1428 | NIMODIPINE | Ki | = | 20100.0 | nM | 4.70 |
| CHEMBL100071 | — | Ki | = | 25900.0 | nM | 4.59 |
| CHEMBL103404 | — | Ki | = | 32600.0 | nM | 4.49 |
| CHEMBL2051956 | DEXNIGULDIPINE | Ki | = | 41300.0 | nM | 4.38 |
| CHEMBL102613 | — | Ki | = | 44500.0 | nM | 4.35 |
| CHEMBL103643 | — | Ki | = | 49200.0 | nM | 4.31 |
| CHEMBL103419 | — | Ki | = | 51000.0 | nM | 4.29 |
| CHEMBL405355 | NIGULDIPINE | Ki | < | 10000.0 | nM | - |
| CHEMBL193 | NIFEDIPINE | Ki | < | 10000.0 | nM | - |