Assay Detail
Binding
CHEMBL652242
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Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-B receptor in the mouse cerebral cortex
22
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Gastrin/cholecystokinin type B receptor (CHEMBL2854) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
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 | 22 | 6.54 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2062154 | CI-988 | 1.0 | 1 | 8.77 |
| CHEMBL62832 | — | — | 1 | 8.21 |
| CHEMBL262456 | — | — | 1 | 8.09 |
| CHEMBL62205 | — | — | 1 | 7.50 |
| CHEMBL292194 | — | — | 1 | 7.24 |
| CHEMBL418464 | — | — | 1 | 7.17 |
| CHEMBL302194 | — | — | 1 | 6.90 |
| CHEMBL417412 | — | — | 1 | 6.89 |
| CHEMBL60386 | — | — | 1 | 6.85 |
| CHEMBL292957 | — | — | 1 | 6.77 |
| CHEMBL64770 | — | — | 1 | 6.70 |
| CHEMBL293178 | — | — | 2 | 6.47 |
| CHEMBL303020 | — | — | 1 | 6.16 |
| CHEMBL292422 | — | — | 1 | 6.06 |
| CHEMBL59985 | — | — | 1 | 5.81 |
| CHEMBL434020 | — | — | 1 | 5.72 |
| CHEMBL294735 | — | — | 1 | 5.66 |
| CHEMBL64623 | — | — | 1 | 5.64 |
| CHEMBL64155 | — | — | 1 | 5.55 |
| CHEMBL292956 | — | — | 1 | 5.17 |
| CHEMBL59859 | — | — | 1 | 4.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2062154 | CI-988 | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL62832 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL262456 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL62205 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL292194 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL418464 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL302194 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL417412 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL60386 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL292957 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL64770 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL293178 | — | IC50 | = | 342.0 | nM | 6.47 |
| CHEMBL303020 | — | IC50 | = | 693.0 | nM | 6.16 |
| CHEMBL292422 | — | IC50 | = | 877.0 | nM | 6.06 |
| CHEMBL293178 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL59985 | — | IC50 | = | 1559.0 | nM | 5.81 |
| CHEMBL434020 | — | IC50 | = | 1910.0 | nM | 5.72 |
| CHEMBL294735 | — | IC50 | = | 2169.0 | nM | 5.66 |
| CHEMBL64623 | — | IC50 | = | 2280.0 | nM | 5.64 |
| CHEMBL64155 | — | IC50 | = | 2820.0 | nM | 5.55 |
| CHEMBL292956 | — | IC50 | = | 6780.0 | nM | 5.17 |
| CHEMBL59859 | — | IC50 | = | 20390.0 | nM | 4.69 |