Assay Detail
Binding
CHEMBL657361
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Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Cholecystokinin receptor type A (CHEMBL2871) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Hybrid cholecystokinin-A antagonists based on molecular modeling of lorglumide and L-364,718.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.91 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL9506 | DEVAZEPIDE | 2.0 | 1 | 9.15 |
| CHEMBL9485 | — | — | 1 | 7.31 |
| CHEMBL9308 | — | — | 1 | 7.05 |
| CHEMBL8893 | — | — | 1 | 6.40 |
| CHEMBL8949 | — | — | 1 | 6.35 |
| CHEMBL9312 | — | — | 1 | 6.10 |
| CHEMBL9379 | — | — | 1 | 6.00 |
| CHEMBL268197 | — | — | 1 | - |
| CHEMBL275031 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL9506 | DEVAZEPIDE | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL9485 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL9308 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL8893 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL8949 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL9312 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL9379 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL268197 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL275031 | — | Ki | > | 4000.0 | nM | - |