Assay Detail
Binding
CHEMBL663082
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Inhibition of [3H]pCCK-8 binding to Guinea pig cortex membrane Cholecystokinin type B receptor
9
Total Activities
9
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
Structure-based design of new constrained cyclic agonists of the cholecystokinin CCK-B receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.66 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1121 | SINCALIDE | 4.0 | 1 | 9.19 |
| CHEMBL333477 | — | — | 1 | 9.10 |
| CHEMBL2371221 | — | — | 1 | 7.82 |
| CHEMBL2371222 | — | — | 1 | 7.82 |
| CHEMBL120632 | TETRAGASTRIN | -1.0 | 1 | 7.71 |
| CHEMBL2371224 | — | — | 1 | 7.40 |
| CHEMBL3143501 | — | — | 1 | 7.29 |
| CHEMBL2371225 | — | — | 1 | 7.21 |
| CHEMBL2371223 | — | — | 1 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1121 | SINCALIDE | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL333477 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL2371221 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2371222 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL120632 | TETRAGASTRIN | Ki | = | 19.5 | nM | 7.71 |
| CHEMBL2371224 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL3143501 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL2371225 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL2371223 | — | Ki | = | 4372.0 | nM | 5.36 |