Assay Detail
Binding
CHEMBL641344
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Displacement [3H]-CGS-21,680 from Adenosine A2A receptor in rat striatal membrane.
21
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 21 | 5.47 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL303198 | — | — | 1 | 7.68 |
| CHEMBL130162 | — | — | 1 | 7.22 |
| CHEMBL132118 | — | — | 1 | 6.54 |
| CHEMBL113142 | ZM-241385 | — | 1 | 6.28 |
| CHEMBL87496 | — | — | 2 | 5.87 |
| CHEMBL17127 | SCH-58261 | — | 1 | 5.72 |
| CHEMBL16687 | CGS-15943 | — | 1 | 5.48 |
| CHEMBL335334 | — | — | 1 | 5.44 |
| CHEMBL130975 | — | — | 1 | 5.33 |
| CHEMBL131133 | — | — | 1 | 5.33 |
| CHEMBL337629 | — | — | 1 | 5.25 |
| CHEMBL130787 | — | — | 1 | 5.22 |
| CHEMBL336968 | — | — | 1 | 4.82 |
| CHEMBL130545 | — | — | 1 | 4.81 |
| CHEMBL2112674 | — | — | 1 | 4.62 |
| CHEMBL130707 | — | — | 1 | 4.59 |
| CHEMBL337243 | — | — | 1 | 4.47 |
| CHEMBL337081 | — | — | 1 | 4.44 |
| CHEMBL44 | GENISTEIN | 2.0 | 1 | 4.44 |
| CHEMBL2112673 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL303198 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL130162 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL132118 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL113142 | ZM-241385 | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL87496 | — | Ki | = | 1360.0 | nM | 5.87 |
| CHEMBL87496 | — | Ki | = | 1360.0 | nM | 5.87 |
| CHEMBL17127 | SCH-58261 | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL16687 | CGS-15943 | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL335334 | — | Ki | = | 3660.0 | nM | 5.44 |
| CHEMBL131133 | — | Ki | = | 4630.0 | nM | 5.33 |
| CHEMBL130975 | — | Ki | = | 4690.0 | nM | 5.33 |
| CHEMBL337629 | — | Ki | = | 5640.0 | nM | 5.25 |
| CHEMBL130787 | — | Ki | = | 6040.0 | nM | 5.22 |
| CHEMBL336968 | — | Ki | = | 15200.0 | nM | 4.82 |
| CHEMBL130545 | — | Ki | = | 15600.0 | nM | 4.81 |
| CHEMBL2112674 | — | Ki | = | 23900.0 | nM | 4.62 |
| CHEMBL130707 | — | Ki | = | 25600.0 | nM | 4.59 |
| CHEMBL337243 | — | Ki | = | 33500.0 | nM | 4.47 |
| CHEMBL337081 | — | Ki | = | 36100.0 | nM | 4.44 |
| CHEMBL44 | GENISTEIN | Ki | = | 36000.0 | nM | 4.44 |
| CHEMBL2112673 | — | Ki | = | 106000.0 | nM | - |