Assay Detail
Binding
CHEMBL657362
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Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Cholecystokinin receptor type A (CHEMBL2871) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecystokinin-A receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.37 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL419764 | — | — | 1 | 9.52 |
| CHEMBL1121 | SINCALIDE | 4.0 | 1 | 9.28 |
| CHEMBL332261 | — | — | 1 | 9.21 |
| CHEMBL431858 | — | — | 1 | 7.97 |
| CHEMBL116001 | — | — | 1 | 6.53 |
| CHEMBL116127 | — | — | 1 | 6.24 |
| CHEMBL326064 | — | — | 1 | 6.09 |
| CHEMBL113699 | — | — | 1 | 5.99 |
| CHEMBL113718 | IQM-95333 | — | 1 | 5.54 |
| CHEMBL324294 | — | — | 1 | - |
| CHEMBL325070 | — | — | 1 | - |
| CHEMBL114517 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL419764 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL1121 | SINCALIDE | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL332261 | — | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL431858 | — | Ki | = | 10.6 | nM | 7.97 |
| CHEMBL116001 | — | Ki | = | 298.0 | nM | 6.53 |
| CHEMBL116127 | — | Ki | = | 572.0 | nM | 6.24 |
| CHEMBL326064 | — | Ki | = | 813.0 | nM | 6.09 |
| CHEMBL113699 | — | Ki | = | 1030.0 | nM | 5.99 |
| CHEMBL113718 | IQM-95333 | Ki | = | 2890.0 | nM | 5.54 |
| CHEMBL324294 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL325070 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL114517 | — | Ki | > | 5000.0 | nM | - |