Assay Detail
Binding
CHEMBL642199
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Displacement of specific [3H](R)-PIA binding at adenosine A1 receptor from rat brain membranes.
29
Total Activities
29
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
Structure-activity relationships of 4-(phenylethynyl)-6-phenyl-1,4-dihydropyridines as highly selective A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 4.86 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL88147 | — | — | 1 | 6.52 |
| CHEMBL90160 | — | — | 1 | 5.44 |
| CHEMBL311542 | — | — | 1 | 5.35 |
| CHEMBL2112340 | — | — | 1 | 5.27 |
| CHEMBL315984 | — | — | 1 | 5.23 |
| CHEMBL328932 | — | — | 1 | 5.09 |
| CHEMBL314071 | — | — | 1 | 5.09 |
| CHEMBL315720 | — | — | 1 | 5.07 |
| CHEMBL86692 | — | — | 1 | 5.07 |
| CHEMBL315458 | — | — | 1 | 4.96 |
| CHEMBL2063640 | — | — | 1 | 4.96 |
| CHEMBL89343 | — | — | 1 | 4.90 |
| CHEMBL86829 | — | — | 1 | 4.90 |
| CHEMBL276854 | — | — | 1 | 4.83 |
| CHEMBL89797 | — | — | 1 | 4.81 |
| CHEMBL315897 | — | — | 1 | 4.79 |
| CHEMBL89874 | — | — | 1 | 4.76 |
| CHEMBL89264 | — | — | 1 | 4.73 |
| CHEMBL85130 | — | — | 1 | 4.73 |
| CHEMBL90733 | — | — | 1 | 4.72 |
| CHEMBL89494 | — | — | 1 | 4.64 |
| CHEMBL86968 | — | — | 1 | 4.63 |
| CHEMBL89575 | — | — | 1 | 4.58 |
| CHEMBL328895 | — | — | 1 | 4.50 |
| CHEMBL88688 | — | — | 1 | 4.46 |
| CHEMBL89852 | — | — | 1 | 4.40 |
| CHEMBL84583 | — | — | 1 | 4.28 |
| CHEMBL89358 | — | — | 1 | 4.18 |
| CHEMBL89093 | — | — | 1 | 4.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL88147 | — | Ki | = | 305.0 | nM | 6.52 |
| CHEMBL90160 | — | Ki | = | 3650.0 | nM | 5.44 |
| CHEMBL311542 | — | Ki | = | 4480.0 | nM | 5.35 |
| CHEMBL2112340 | — | Ki | = | 5390.0 | nM | 5.27 |
| CHEMBL315984 | — | Ki | = | 5930.0 | nM | 5.23 |
| CHEMBL328932 | — | Ki | = | 8200.0 | nM | 5.09 |
| CHEMBL314071 | — | Ki | = | 8030.0 | nM | 5.09 |
| CHEMBL315720 | — | Ki | = | 8590.0 | nM | 5.07 |
| CHEMBL86692 | — | Ki | = | 8580.0 | nM | 5.07 |
| CHEMBL315458 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL2063640 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL89343 | — | Ki | = | 12600.0 | nM | 4.90 |
| CHEMBL86829 | — | Ki | = | 12500.0 | nM | 4.90 |
| CHEMBL276854 | — | Ki | = | 14900.0 | nM | 4.83 |
| CHEMBL89797 | — | Ki | = | 15400.0 | nM | 4.81 |
| CHEMBL315897 | — | Ki | = | 16200.0 | nM | 4.79 |
| CHEMBL89874 | — | Ki | = | 17400.0 | nM | 4.76 |
| CHEMBL89264 | — | Ki | = | 18800.0 | nM | 4.73 |
| CHEMBL85130 | — | Ki | = | 18500.0 | nM | 4.73 |
| CHEMBL90733 | — | Ki | = | 19100.0 | nM | 4.72 |
| CHEMBL89494 | — | Ki | = | 23100.0 | nM | 4.64 |
| CHEMBL86968 | — | Ki | = | 23600.0 | nM | 4.63 |
| CHEMBL89575 | — | Ki | = | 26600.0 | nM | 4.58 |
| CHEMBL328895 | — | Ki | = | 31500.0 | nM | 4.50 |
| CHEMBL88688 | — | Ki | = | 34500.0 | nM | 4.46 |
| CHEMBL89852 | — | Ki | = | 40100.0 | nM | 4.40 |
| CHEMBL84583 | — | Ki | = | 53000.0 | nM | 4.28 |
| CHEMBL89358 | — | Ki | = | 65600.0 | nM | 4.18 |
| CHEMBL89093 | — | Ki | = | 100000.0 | nM | 4.00 |