Assay Detail
Binding
CHEMBL640470
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Tested for the displacement [3H]PIA from Adenosine A1 receptor in rat brain membrane
26
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Tetrahydrobenzothiophenone derivatives as a novel class of adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 5.53 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL130162 | — | — | 1 | 8.92 |
| CHEMBL132118 | — | — | 1 | 7.47 |
| CHEMBL303198 | — | — | 1 | 6.57 |
| CHEMBL1717143 | — | — | 1 | 6.25 |
| CHEMBL87496 | — | — | 2 | 6.15 |
| CHEMBL130787 | — | — | 1 | 5.97 |
| CHEMBL130975 | — | — | 1 | 5.90 |
| CHEMBL130545 | — | — | 1 | 5.85 |
| CHEMBL131133 | — | — | 1 | 5.75 |
| CHEMBL335334 | — | — | 1 | 5.71 |
| CHEMBL130707 | — | — | 1 | 5.65 |
| CHEMBL2112674 | — | — | 1 | 5.57 |
| CHEMBL337629 | — | — | 1 | 5.48 |
| CHEMBL2112673 | — | — | 1 | 5.44 |
| CHEMBL44 | GENISTEIN | 2.0 | 1 | 5.30 |
| CHEMBL42639 | — | — | 1 | 4.77 |
| CHEMBL337081 | — | — | 1 | 4.76 |
| CHEMBL337243 | — | — | 1 | 4.74 |
| CHEMBL2112672 | — | — | 1 | 4.49 |
| CHEMBL132222 | — | — | 1 | 4.41 |
| CHEMBL336968 | — | — | 1 | 4.30 |
| CHEMBL75126 | — | — | 1 | 4.29 |
| CHEMBL130596 | — | — | 1 | 4.16 |
| CHEMBL130595 | — | — | 1 | 4.15 |
| CHEMBL16687 | CGS-15943 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL130162 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL132118 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL303198 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL1717143 | — | Ki | = | 567.0 | nM | 6.25 |
| CHEMBL87496 | — | Ki | = | 715.0 | nM | 6.15 |
| CHEMBL87496 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL130787 | — | Ki | = | 1060.0 | nM | 5.97 |
| CHEMBL130975 | — | Ki | = | 1260.0 | nM | 5.90 |
| CHEMBL130545 | — | Ki | = | 1420.0 | nM | 5.85 |
| CHEMBL131133 | — | Ki | = | 1790.0 | nM | 5.75 |
| CHEMBL335334 | — | Ki | = | 1930.0 | nM | 5.71 |
| CHEMBL130707 | — | Ki | = | 2220.0 | nM | 5.65 |
| CHEMBL2112674 | — | Ki | = | 2690.0 | nM | 5.57 |
| CHEMBL337629 | — | Ki | = | 3340.0 | nM | 5.48 |
| CHEMBL2112673 | — | Ki | = | 3640.0 | nM | 5.44 |
| CHEMBL44 | GENISTEIN | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL42639 | — | Ki | = | 17000.0 | nM | 4.77 |
| CHEMBL337081 | — | Ki | = | 17500.0 | nM | 4.76 |
| CHEMBL337243 | — | Ki | = | 18300.0 | nM | 4.74 |
| CHEMBL2112672 | — | Ki | = | 32700.0 | nM | 4.49 |
| CHEMBL132222 | — | Ki | = | 39400.0 | nM | 4.41 |
| CHEMBL336968 | — | Ki | = | 50000.0 | nM | 4.30 |
| CHEMBL75126 | — | Ki | = | 51600.0 | nM | 4.29 |
| CHEMBL130596 | — | Ki | = | 69800.0 | nM | 4.16 |
| CHEMBL130595 | — | Ki | = | 71200.0 | nM | 4.15 |
| CHEMBL16687 | CGS-15943 | Ki | = | 21000.0 | nM | - |