Assay Detail
Binding
CHEMBL663169
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Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to mouse cerebral cortex cholecystokinin type B receptor
18
Total Activities
18
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
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 | 18 | 7.82 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1121 | SINCALIDE | 4.0 | 1 | 9.52 |
| CHEMBL1328 | PENTAGASTRIN | 4.0 | 1 | 9.10 |
| CHEMBL337384 | — | — | 1 | 9.10 |
| CHEMBL131754 | — | — | 1 | 8.59 |
| CHEMBL334346 | — | — | 1 | 8.47 |
| CHEMBL9387 | L-365260 | — | 1 | 8.29 |
| CHEMBL423329 | — | — | 1 | 8.20 |
| CHEMBL2112695 | — | — | 1 | 8.06 |
| CHEMBL337661 | — | — | 1 | 7.64 |
| CHEMBL9506 | DEVAZEPIDE | 2.0 | 1 | 7.51 |
| CHEMBL321946 | — | — | 1 | 7.50 |
| CHEMBL2111884 | — | — | 1 | 7.37 |
| CHEMBL291033 | — | — | 1 | 7.32 |
| CHEMBL133101 | — | — | 1 | 7.20 |
| CHEMBL2112692 | — | — | 1 | 6.80 |
| CHEMBL130578 | — | — | 1 | 6.77 |
| CHEMBL337461 | — | — | 1 | 6.75 |
| CHEMBL2114401 | — | — | 1 | 6.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1121 | SINCALIDE | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1328 | PENTAGASTRIN | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL337384 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL131754 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL334346 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL9387 | L-365260 | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL423329 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL2112695 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL337661 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL9506 | DEVAZEPIDE | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL321946 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL2111884 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL291033 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL133101 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL2112692 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL130578 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL337461 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2114401 | — | IC50 | = | 330.0 | nM | 6.48 |