Assay Detail
Binding
CHEMBL651448
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Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
16
Total Activities
16
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
SAR study of the indole moiety of CI-988, a potent and selective CCK-B antagonist
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.72 | 7.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL302194 | — | — | 1 | 7.19 |
| CHEMBL64155 | — | — | 1 | 6.23 |
| CHEMBL60386 | — | — | 1 | 6.21 |
| CHEMBL62205 | — | — | 1 | 6.19 |
| CHEMBL62832 | — | — | 1 | 6.17 |
| CHEMBL434020 | — | — | 1 | 5.87 |
| CHEMBL303020 | — | — | 1 | 5.72 |
| CHEMBL262456 | — | — | 1 | 5.66 |
| CHEMBL417412 | — | — | 1 | 5.58 |
| CHEMBL292194 | — | — | 1 | 5.54 |
| CHEMBL294735 | — | — | 1 | 5.44 |
| CHEMBL2062154 | CI-988 | 1.0 | 1 | 5.37 |
| CHEMBL292422 | — | — | 1 | 5.27 |
| CHEMBL64623 | — | — | 1 | 5.16 |
| CHEMBL292956 | — | — | 1 | 5.14 |
| CHEMBL59985 | — | — | 1 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL302194 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL64155 | — | IC50 | = | 583.0 | nM | 6.23 |
| CHEMBL60386 | — | IC50 | = | 616.0 | nM | 6.21 |
| CHEMBL62205 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL62832 | — | IC50 | = | 681.0 | nM | 6.17 |
| CHEMBL434020 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL303020 | — | IC50 | = | 1909.0 | nM | 5.72 |
| CHEMBL262456 | — | IC50 | = | 2185.0 | nM | 5.66 |
| CHEMBL417412 | — | IC50 | = | 2649.0 | nM | 5.58 |
| CHEMBL292194 | — | IC50 | = | 2859.0 | nM | 5.54 |
| CHEMBL294735 | — | IC50 | = | 3620.0 | nM | 5.44 |
| CHEMBL2062154 | CI-988 | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL292422 | — | IC50 | = | 5349.0 | nM | 5.27 |
| CHEMBL64623 | — | IC50 | = | 6939.0 | nM | 5.16 |
| CHEMBL292956 | — | IC50 | = | 7220.0 | nM | 5.14 |
| CHEMBL59985 | — | IC50 | = | 19800.0 | nM | 4.70 |