Assay Detail
Binding
CHEMBL662867
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Inhibition of [125I]CCK-8 binding to cholecystokinin type B receptor in the mouse cerebral cortex
27
Total Activities
26
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
Amide bond replacements incorporated into CCK-B selective "dipeptoids".
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 5.88 | 6.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL286442 | — | — | 2 | 6.90 |
| CHEMBL280502 | — | — | 1 | 6.50 |
| CHEMBL284361 | — | — | 1 | 6.46 |
| CHEMBL287079 | — | — | 1 | 6.41 |
| CHEMBL291033 | — | — | 1 | 6.19 |
| CHEMBL36443 | — | — | 1 | 6.12 |
| CHEMBL286843 | — | — | 1 | 6.08 |
| CHEMBL1237153 | — | — | 1 | 6.01 |
| CHEMBL35580 | — | — | 1 | 5.97 |
| CHEMBL285049 | — | — | 1 | 5.97 |
| CHEMBL445094 | — | — | 1 | 5.97 |
| CHEMBL422941 | — | — | 1 | 5.97 |
| CHEMBL288038 | — | — | 1 | 5.92 |
| CHEMBL285880 | — | — | 1 | 5.91 |
| CHEMBL285762 | — | — | 1 | 5.90 |
| CHEMBL288037 | — | — | 1 | 5.88 |
| CHEMBL287682 | — | — | 1 | 5.82 |
| CHEMBL34300 | — | — | 1 | 5.70 |
| CHEMBL2112071 | — | — | 1 | 5.58 |
| CHEMBL37903 | — | — | 1 | 5.53 |
| CHEMBL289239 | — | — | 1 | 5.45 |
| CHEMBL34422 | — | — | 1 | 5.44 |
| CHEMBL286664 | — | — | 1 | 5.43 |
| CHEMBL35555 | — | — | 1 | 5.39 |
| CHEMBL2062154 | CI-988 | 1.0 | 1 | 5.37 |
| CHEMBL286093 | — | — | 1 | 4.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL286442 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL280502 | — | IC50 | = | 317.0 | nM | 6.50 |
| CHEMBL284361 | — | IC50 | = | 351.0 | nM | 6.46 |
| CHEMBL287079 | — | IC50 | = | 394.0 | nM | 6.41 |
| CHEMBL291033 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL286442 | — | IC50 | = | 708.0 | nM | 6.15 |
| CHEMBL36443 | — | IC50 | = | 757.0 | nM | 6.12 |
| CHEMBL286843 | — | IC50 | = | 827.0 | nM | 6.08 |
| CHEMBL1237153 | — | IC50 | = | 976.0 | nM | 6.01 |
| CHEMBL285049 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL35580 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL422941 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL445094 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL288038 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL285880 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL285762 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL288037 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL287682 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL34300 | — | IC50 | = | 1980.0 | nM | 5.70 |
| CHEMBL2112071 | — | IC50 | = | 2620.0 | nM | 5.58 |
| CHEMBL37903 | — | IC50 | = | 2950.0 | nM | 5.53 |
| CHEMBL289239 | — | IC50 | = | 3530.0 | nM | 5.45 |
| CHEMBL34422 | — | IC50 | = | 3620.0 | nM | 5.44 |
| CHEMBL286664 | — | IC50 | = | 3670.0 | nM | 5.43 |
| CHEMBL35555 | — | IC50 | = | 4060.0 | nM | 5.39 |
| CHEMBL2062154 | CI-988 | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL286093 | — | IC50 | = | 19500.0 | nM | 4.71 |