Assay Detail
Binding
CHEMBL3821422
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Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Cholecystokinin receptor type A (CHEMBL2871) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Cholecystokinin-1 receptor antagonists: 5-hydroxy-5-aryl-pyrrol-2-ones as anticancer agents
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.34 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3818718 | — | — | 1 | 8.10 |
| CHEMBL3818164 | — | — | 1 | 7.92 |
| CHEMBL3818215 | — | — | 1 | 7.70 |
| CHEMBL3819315 | — | — | 1 | 6.92 |
| CHEMBL1255589 | LORGLUMIDE SODIUM | — | 1 | 6.77 |
| CHEMBL3818578 | — | — | 1 | 6.70 |
| CHEMBL3819054 | — | — | 1 | 6.52 |
| CHEMBL3818781 | — | — | 1 | 6.44 |
| CHEMBL3818410 | — | — | 1 | 6.10 |
| CHEMBL3818822 | — | — | 1 | 5.70 |
| CHEMBL3817873 | — | — | 1 | 5.60 |
| CHEMBL3818165 | — | — | 1 | 5.60 |
| CHEMBL3817870 | — | — | 1 | 5.44 |
| CHEMBL3818705 | — | — | 1 | 5.40 |
| CHEMBL3818303 | — | — | 1 | 5.35 |
| CHEMBL3818437 | — | — | 1 | 5.12 |
| CHEMBL3819216 | — | — | 1 | - |
| CHEMBL3818877 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3818718 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3818164 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3818215 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3819315 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1255589 | LORGLUMIDE SODIUM | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3818578 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3819054 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3818781 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL3818410 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3818822 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3817873 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3818165 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3817870 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL3818705 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3818303 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL3818437 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL3819216 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3818877 | — | IC50 | > | 10000.0 | nM | - |