Assay Detail
Functional
CHEMBL750159
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Antagonistic activity against P2Y purinoceptor 1
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| 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 |
|---|---|---|---|
| IC50 | 13 | 6.74 | 8.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL444278 | — | — | 1 | 8.08 |
| CHEMBL146342 | — | — | 1 | 7.43 |
| CHEMBL2112867 | — | — | 1 | 7.31 |
| CHEMBL2112864 | — | — | 1 | 7.28 |
| CHEMBL343651 | — | — | 1 | 7.06 |
| CHEMBL2112863 | — | — | 1 | 6.80 |
| CHEMBL2112865 | — | — | 1 | 6.66 |
| CHEMBL2112868 | — | — | 1 | 6.45 |
| CHEMBL2112861 | — | — | 1 | 6.43 |
| CHEMBL356041 | — | — | 1 | 6.42 |
| CHEMBL2112869 | — | — | 1 | 6.34 |
| CHEMBL2112866 | — | — | 1 | 5.73 |
| CHEMBL2112007 | — | — | 1 | 5.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL444278 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL146342 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL2112867 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL2112864 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL343651 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL2112863 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL2112865 | — | IC50 | = | 221.0 | nM | 6.66 |
| CHEMBL2112868 | — | IC50 | = | 356.0 | nM | 6.45 |
| CHEMBL2112861 | — | IC50 | = | 367.0 | nM | 6.43 |
| CHEMBL356041 | — | IC50 | = | 377.0 | nM | 6.42 |
| CHEMBL2112869 | — | IC50 | = | 452.0 | nM | 6.34 |
| CHEMBL2112866 | — | IC50 | = | 1870.0 | nM | 5.73 |
| CHEMBL2112007 | — | IC50 | = | 2400.0 | nM | 5.62 |