Assay Detail
Binding
CHEMBL2175134
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [33P]2-MeS-ADP from human recombinant P2Y12 receptor expressed in CHO cell membranes by scintillation counting method
63
Total Activities
63
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
Identification of high-affinity P2Y₁₂ antagonists based on a phenylpyrazole glutamic acid piperazine backbone.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 63 | 7.22 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2172149 | — | — | 1 | 9.10 |
| CHEMBL2172129 | — | — | 1 | 8.82 |
| CHEMBL2172148 | — | — | 1 | 8.51 |
| CHEMBL2172150 | — | — | 1 | 8.30 |
| CHEMBL2172128 | — | — | 1 | 8.30 |
| CHEMBL2172146 | — | — | 1 | 8.24 |
| CHEMBL2172133 | — | — | 1 | 8.19 |
| CHEMBL2172272 | — | — | 1 | 8.14 |
| CHEMBL2172151 | — | — | 1 | 8.11 |
| CHEMBL2172140 | — | — | 1 | 8.11 |
| CHEMBL398435 | TICAGRELOR | 4.0 | 1 | 7.85 |
| CHEMBL2172156 | — | — | 1 | 7.72 |
| CHEMBL2172273 | — | — | 1 | 7.70 |
| CHEMBL2172165 | — | — | 1 | 7.66 |
| CHEMBL2172127 | — | — | 1 | 7.64 |
| CHEMBL2103828 | ELINOGREL | 2.0 | 1 | 7.64 |
| CHEMBL2172132 | — | — | 1 | 7.64 |
| CHEMBL2172274 | — | — | 1 | 7.57 |
| CHEMBL2172143 | — | — | 1 | 7.52 |
| CHEMBL2172163 | — | — | 1 | 7.48 |
| CHEMBL2172144 | — | — | 1 | 7.40 |
| CHEMBL2172269 | — | — | 1 | 7.39 |
| CHEMBL2172157 | — | — | 1 | 7.38 |
| CHEMBL2172131 | — | — | 1 | 7.38 |
| CHEMBL2172155 | — | — | 1 | 7.32 |
| CHEMBL2172154 | — | — | 1 | 7.29 |
| CHEMBL2172152 | — | — | 1 | 7.27 |
| CHEMBL2172161 | — | — | 1 | 7.25 |
| CHEMBL2172268 | — | — | 1 | 7.25 |
| CHEMBL2172162 | — | — | 1 | 7.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2172149 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL2172129 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL2172148 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL2172150 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2172128 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2172146 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL2172133 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL2172272 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL2172151 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL2172140 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL398435 | TICAGRELOR | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL2172156 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL2172273 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL2172165 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL2172132 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL2103828 | ELINOGREL | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL2172127 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL2172274 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL2172143 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL2172163 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL2172144 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL2172269 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL2172157 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL2172131 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL2172155 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL2172154 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL2172152 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL2172161 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL2172268 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL2172162 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL2172267 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL2172147 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL2172153 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL2172141 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL2172275 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL2172270 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL2172139 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL2172138 | — | Ki | = | 111.0 | nM | 6.96 |
| CHEMBL2172145 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL2172277 | — | Ki | = | 139.0 | nM | 6.86 |
| CHEMBL2172166 | — | Ki | = | 173.0 | nM | 6.76 |
| CHEMBL2172135 | — | Ki | = | 172.0 | nM | 6.76 |
| CHEMBL2172130 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL2172137 | — | Ki | = | 183.0 | nM | 6.74 |
| CHEMBL2172142 | — | Ki | = | 193.0 | nM | 6.71 |
| CHEMBL2172134 | — | Ki | = | 202.0 | nM | 6.70 |
| CHEMBL2172136 | — | Ki | = | 207.0 | nM | 6.68 |
| CHEMBL2172160 | — | Ki | = | 219.0 | nM | 6.66 |
| CHEMBL2172158 | — | Ki | = | 238.0 | nM | 6.62 |
| CHEMBL2172279 | — | Ki | = | 242.0 | nM | 6.62 |