Assay Detail
Binding
CHEMBL662391
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Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Cholecystokinin receptor type A (CHEMBL2871) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Rationally designed "dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.90 | 6.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL341460 | — | — | 1 | 6.10 |
| CHEMBL2112693 | — | — | 1 | 6.06 |
| CHEMBL335914 | — | — | 1 | 6.02 |
| CHEMBL341281 | — | — | 1 | 5.96 |
| CHEMBL2112694 | — | — | 1 | 5.89 |
| CHEMBL2062154 | CI-988 | 1.0 | 1 | 5.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL341460 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL2112693 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL335914 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL341281 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2112694 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2062154 | CI-988 | IC50 | = | 4300.0 | nM | 5.37 |