Assay Detail
Binding
CHEMBL2394755
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Displacement of [beta-33P]-2MeS-ADP from human P2Y1 receptor expressed in HEK293 cells after 1 hr by scintillation counting analysis
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
New azole antagonists with high affinity for the P2Y(1) receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 7.03 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2393201 | — | — | 1 | 8.15 |
| CHEMBL2393200 | — | — | 1 | 8.00 |
| CHEMBL2393213 | — | — | 1 | 7.96 |
| CHEMBL2390979 | — | — | 1 | 7.82 |
| CHEMBL2393211 | — | — | 1 | 7.82 |
| CHEMBL2393206 | — | — | 1 | 7.75 |
| CHEMBL2393219 | — | — | 1 | 7.72 |
| CHEMBL2393207 | — | — | 1 | 7.68 |
| CHEMBL2393220 | — | — | 1 | 7.64 |
| CHEMBL2393214 | — | — | 1 | 7.60 |
| CHEMBL2393202 | — | — | 1 | 7.57 |
| CHEMBL2393210 | — | — | 1 | 7.39 |
| CHEMBL2393196 | — | — | 1 | 7.35 |
| CHEMBL2393203 | — | — | 1 | 7.26 |
| CHEMBL2393212 | — | — | 1 | 7.23 |
| CHEMBL2393216 | — | — | 1 | 7.16 |
| CHEMBL2393195 | — | — | 1 | 7.05 |
| CHEMBL2393204 | — | — | 1 | 6.60 |
| CHEMBL2393209 | — | — | 1 | 6.56 |
| CHEMBL2393208 | — | — | 1 | 6.47 |
| CHEMBL2393217 | — | — | 1 | 6.39 |
| CHEMBL2393205 | — | — | 1 | 6.17 |
| CHEMBL2393198 | — | — | 1 | 6.06 |
| CHEMBL2393215 | — | — | 1 | 5.82 |
| CHEMBL2393218 | — | — | 1 | 5.60 |
| CHEMBL2393199 | — | — | 1 | 5.56 |
| CHEMBL2393194 | — | — | 1 | 5.54 |
| CHEMBL2393197 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2393201 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL2393200 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2393213 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2390979 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2393211 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2393206 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL2393219 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL2393207 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL2393220 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL2393214 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL2393202 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL2393210 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL2393196 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL2393203 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL2393212 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL2393216 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL2393195 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL2393204 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL2393209 | — | Ki | = | 275.0 | nM | 6.56 |
| CHEMBL2393208 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL2393217 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL2393205 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL2393198 | — | Ki | = | 870.0 | nM | 6.06 |
| CHEMBL2393215 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL2393218 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL2393199 | — | Ki | = | 2730.0 | nM | 5.56 |
| CHEMBL2393194 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL2393197 | — | Ki | > | 36000.0 | nM | - |