Assay Detail
Binding
CHEMBL653062
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Capacity to inhibit [3H]-p CCK 8 binding to membrane preparations of CHO cells transfected with the rat CCK-B receptor
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Gastrin/cholecystokinin type B receptor (CHEMBL3508) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Novel constrained CCK-B dipeptoid antagonists derived from pipecolic acid.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.84 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL286247 | — | — | 1 | 7.85 |
| CHEMBL405468 | — | — | 1 | 7.85 |
| CHEMBL9387 | L-365260 | — | 1 | 7.82 |
| CHEMBL289021 | — | — | 1 | 7.82 |
| CHEMBL30524 | — | — | 1 | 7.73 |
| CHEMBL285419 | — | — | 1 | 7.62 |
| CHEMBL339451 | — | — | 1 | 7.55 |
| CHEMBL423119 | — | — | 1 | 7.49 |
| CHEMBL283040 | — | — | 1 | 6.76 |
| CHEMBL418593 | — | — | 1 | 6.26 |
| CHEMBL30605 | — | — | 1 | 6.10 |
| CHEMBL263803 | — | — | 1 | 6.10 |
| CHEMBL34037 | — | — | 1 | 6.09 |
| CHEMBL434199 | — | — | 1 | 6.05 |
| CHEMBL2114379 | — | — | 1 | 5.98 |
| CHEMBL283913 | — | — | 1 | 5.81 |
| CHEMBL105618 | — | — | 1 | 5.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL286247 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL405468 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL9387 | L-365260 | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL289021 | — | Ki | = | 15.3 | nM | 7.82 |
| CHEMBL30524 | — | Ki | = | 18.6 | nM | 7.73 |
| CHEMBL285419 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL339451 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL423119 | — | Ki | = | 32.7 | nM | 7.49 |
| CHEMBL283040 | — | Ki | = | 175.2 | nM | 6.76 |
| CHEMBL418593 | — | Ki | = | 543.0 | nM | 6.26 |
| CHEMBL30605 | — | Ki | = | 789.0 | nM | 6.10 |
| CHEMBL263803 | — | Ki | = | 791.0 | nM | 6.10 |
| CHEMBL34037 | — | Ki | = | 812.0 | nM | 6.09 |
| CHEMBL434199 | — | Ki | = | 896.0 | nM | 6.05 |
| CHEMBL2114379 | — | Ki | = | 1040.0 | nM | 5.98 |
| CHEMBL283913 | — | Ki | = | 1538.0 | nM | 5.81 |
| CHEMBL105618 | — | Ki | = | 3400.0 | nM | 5.47 |