Assay Detail
Binding
CHEMBL662392
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Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Cholecystokinin receptor type A (CHEMBL2871) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 | 6.52 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1121 | SINCALIDE | 4.0 | 1 | 10.00 |
| CHEMBL9506 | DEVAZEPIDE | 2.0 | 1 | 10.00 |
| CHEMBL9387 | L-365260 | — | 1 | 6.64 |
| CHEMBL291033 | — | — | 1 | 6.42 |
| CHEMBL337384 | — | — | 1 | 6.36 |
| CHEMBL131754 | — | — | 1 | 6.30 |
| CHEMBL130578 | — | — | 1 | 6.24 |
| CHEMBL1328 | PENTAGASTRIN | 4.0 | 1 | 6.22 |
| CHEMBL2114401 | — | — | 1 | 6.21 |
| CHEMBL321946 | — | — | 1 | 6.19 |
| CHEMBL334346 | — | — | 1 | 6.13 |
| CHEMBL423329 | — | — | 1 | 6.11 |
| CHEMBL2112695 | — | — | 1 | 6.09 |
| CHEMBL337661 | — | — | 1 | 6.07 |
| CHEMBL2112692 | — | — | 1 | 5.60 |
| CHEMBL2111884 | — | — | 1 | 5.51 |
| CHEMBL133101 | — | — | 1 | 4.75 |
| CHEMBL337461 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1121 | SINCALIDE | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL9506 | DEVAZEPIDE | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL9387 | L-365260 | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL291033 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL337384 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL131754 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL130578 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL1328 | PENTAGASTRIN | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL2114401 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL321946 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL334346 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL423329 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL2112695 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL337661 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL2112692 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2111884 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL133101 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL337461 | — | IC50 | > | 1000.0 | nM | - |