Assay Detail
Binding
CHEMBL663482
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Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
14
Total Activities
14
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
Cholecystokinin antagonists. Synthesis and biological evaluation of 4-substituted 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.48 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL53907 | — | — | 1 | 9.70 |
| CHEMBL50986 | — | — | 1 | 9.05 |
| CHEMBL298948 | — | — | 1 | 8.36 |
| CHEMBL298705 | — | — | 1 | 7.09 |
| CHEMBL416483 | — | — | 1 | 7.00 |
| CHEMBL53234 | — | — | 1 | 6.92 |
| CHEMBL299538 | — | — | 1 | 6.70 |
| CHEMBL301172 | — | — | 1 | 6.66 |
| CHEMBL51569 | — | — | 1 | 6.52 |
| CHEMBL300926 | — | — | 1 | 4.85 |
| CHEMBL301331 | — | — | 1 | 4.66 |
| CHEMBL51280 | — | — | 1 | 4.60 |
| CHEMBL646 | TRIAZOLAM | 4.0 | 1 | 4.41 |
| CHEMBL661 | ALPRAZOLAM | 4.0 | 1 | 4.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL53907 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL50986 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL298948 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL298705 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL416483 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL53234 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL299538 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL301172 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL51569 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL300926 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL301331 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL51280 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL646 | TRIAZOLAM | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL661 | ALPRAZOLAM | IC50 | = | 64000.0 | nM | 4.19 |