Assay Detail
Binding
CHEMBL1064501
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Inhibition of human P2Y12 receptor expressed in CHO cells
84
Total Activities
84
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Part II: piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 84 | 8.27 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL601696 | — | — | 1 | 9.24 |
| CHEMBL601489 | — | — | 1 | 9.19 |
| CHEMBL570295 | — | — | 1 | 9.17 |
| CHEMBL601695 | — | — | 1 | 9.10 |
| CHEMBL601698 | — | — | 1 | 9.01 |
| CHEMBL601903 | — | — | 1 | 8.96 |
| CHEMBL601692 | — | — | 1 | 8.96 |
| CHEMBL601905 | — | — | 1 | 8.92 |
| CHEMBL601485 | — | — | 1 | 8.85 |
| CHEMBL601478 | — | — | 1 | 8.82 |
| CHEMBL589804 | — | — | 1 | 8.82 |
| CHEMBL589519 | — | — | 1 | 8.82 |
| CHEMBL590260 | — | — | 1 | 8.77 |
| CHEMBL601483 | — | — | 1 | 8.77 |
| CHEMBL590008 | — | — | 1 | 8.77 |
| CHEMBL590146 | — | — | 1 | 8.77 |
| CHEMBL589335 | — | — | 1 | 8.72 |
| CHEMBL601486 | — | — | 1 | 8.70 |
| CHEMBL589901 | — | — | 1 | 8.70 |
| CHEMBL601906 | — | — | 1 | 8.68 |
| CHEMBL590194 | — | — | 1 | 8.60 |
| CHEMBL601484 | — | — | 1 | 8.59 |
| CHEMBL590004 | — | — | 1 | 8.59 |
| CHEMBL602111 | — | — | 1 | 8.55 |
| CHEMBL601907 | — | — | 1 | 8.55 |
| CHEMBL589824 | — | — | 1 | 8.55 |
| CHEMBL589584 | — | — | 1 | 8.49 |
| CHEMBL601487 | — | — | 1 | 8.48 |
| CHEMBL590069 | — | — | 1 | 8.46 |
| CHEMBL589520 | — | — | 1 | 8.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL601696 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL601489 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL570295 | — | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL601695 | — | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL601698 | — | Ki | = | 0.98 | nM | 9.01 |
| CHEMBL601903 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL601692 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL601905 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL601485 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL601478 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL589804 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL589519 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL590008 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL590260 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL601483 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL590146 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL589335 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL601486 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL589901 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL601906 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL590194 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL601484 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL590004 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL589824 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL602111 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL601907 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL589584 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL601487 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL590069 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL589520 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL589518 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL589889 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL589971 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL601697 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL590007 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL601904 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL601910 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL590114 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL602109 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL590261 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL601271 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL602112 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL602108 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL589828 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL590009 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL589697 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL589897 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL590005 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL601488 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL601273 | — | Ki | = | 7.3 | nM | 8.14 |