Assay Detail
Binding
CHEMBL2422901
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ZM241385 from human A2A receptor expressed in HEK293 cell membranes after 60 mins by scintillation counting
14
Total Activities
14
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
Design and synthesis of (4E)-4-(4-substitutedbenzylideneamino)-3-substituted-2,3-dihydro-2-thioxothiazole-5-carbonitrile as novel A2A receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 9.14 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2419139 | — | — | 1 | 11.00 |
| CHEMBL2419146 | — | — | 1 | 10.57 |
| CHEMBL2419147 | — | — | 1 | 10.52 |
| CHEMBL2419150 | — | — | 1 | 10.17 |
| CHEMBL2419140 | — | — | 1 | 9.85 |
| CHEMBL2419143 | — | — | 1 | 8.84 |
| CHEMBL2419138 | — | — | 1 | 8.74 |
| CHEMBL2419145 | — | — | 1 | 8.58 |
| CHEMBL2419137 | — | — | 1 | 8.12 |
| CHEMBL2419141 | — | — | 1 | 8.02 |
| CHEMBL2419148 | — | — | 1 | 7.96 |
| CHEMBL2419142 | — | — | 1 | 7.26 |
| CHEMBL2419149 | — | — | 1 | - |
| CHEMBL2419144 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2419139 | — | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL2419146 | — | Ki | = | 0.027 | nM | 10.57 |
| CHEMBL2419147 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL2419150 | — | Ki | = | 0.067 | nM | 10.17 |
| CHEMBL2419140 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL2419143 | — | Ki | = | 1.44 | nM | 8.84 |
| CHEMBL2419138 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL2419145 | — | Ki | = | 2.64 | nM | 8.58 |
| CHEMBL2419137 | — | Ki | = | 7.61 | nM | 8.12 |
| CHEMBL2419141 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL2419148 | — | Ki | = | 10.98 | nM | 7.96 |
| CHEMBL2419142 | — | Ki | = | 54.8 | nM | 7.26 |
| CHEMBL2419149 | — | Ki | = | 0.0042 | nM | - |
| CHEMBL2419144 | — | Ki | = | 0.0047 | nM | - |