Assay Detail
Binding
CHEMBL662569
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Displacement of [125I]-BH CCK-8S from Cholecystokinin type B receptor in guinea pig cortex
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Gastrin/cholecystokinin type B receptor (CHEMBL298) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
C5-piperazinyl-1,4-benzodiazepines, water-soluble, orally bioa vailable CCKB/gastrin receptor antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.81 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL420783 | L-740093 | — | 1 | 10.00 |
| CHEMBL103119 | — | — | 1 | 8.74 |
| CHEMBL102633 | — | — | 1 | 8.31 |
| CHEMBL9387 | L-365260 | — | 1 | 8.07 |
| CHEMBL101528 | — | — | 1 | 8.01 |
| CHEMBL105273 | — | — | 1 | 7.93 |
| CHEMBL100502 | — | — | 1 | 7.74 |
| CHEMBL103791 | — | — | 1 | 7.51 |
| CHEMBL103229 | — | — | 1 | 6.92 |
| CHEMBL319180 | — | — | 1 | 6.57 |
| CHEMBL102537 | — | — | 1 | 6.06 |
| CHEMBL431832 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL420783 | L-740093 | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL103119 | — | IC50 | = | 1.81 | nM | 8.74 |
| CHEMBL102633 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL9387 | L-365260 | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL101528 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL105273 | — | IC50 | = | 11.8 | nM | 7.93 |
| CHEMBL100502 | — | IC50 | = | 18.3 | nM | 7.74 |
| CHEMBL103791 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL103229 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL319180 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL102537 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL431832 | — | IC50 | > | 3000.0 | nM | - |