Assay Detail
Binding
CHEMBL750161
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Inhibition of [3H]5 binding to P2Y purinoceptor 1 expressed in Sf9 cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
2-Substitution of adenine nucleotide analogues containing a bicyclo[3.1.0]hexane ring system locked in a northern conformation: enhanced potency as P2Y1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.53 | 9.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL444278 | — | — | 1 | 9.11 |
| CHEMBL2112864 | — | — | 1 | 8.60 |
| CHEMBL2112867 | — | — | 1 | 8.44 |
| CHEMBL146342 | — | — | 1 | 8.29 |
| CHEMBL343651 | — | — | 1 | 7.90 |
| CHEMBL2112863 | — | — | 1 | 7.75 |
| CHEMBL356041 | — | — | 1 | 7.46 |
| CHEMBL2112868 | — | — | 1 | 7.35 |
| CHEMBL2112869 | — | — | 1 | 7.10 |
| CHEMBL2112865 | — | — | 1 | 7.04 |
| CHEMBL2112866 | — | — | 1 | 6.48 |
| CHEMBL2112007 | — | — | 1 | 6.37 |
| CHEMBL2112861 | — | — | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL444278 | — | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL2112864 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL2112867 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL146342 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL343651 | — | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL2112863 | — | Ki | = | 17.6 | nM | 7.75 |
| CHEMBL356041 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL2112868 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL2112869 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL2112865 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL2112866 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL2112007 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL2112861 | — | Ki | = | 863.0 | nM | 6.06 |