Assay Detail
Binding
CHEMBL661733
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Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines: CCK-A agonists that demonstrate oral activity as satiety agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.49 | 8.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1121 | SINCALIDE | 4.0 | 1 | 8.88 |
| CHEMBL316164 | — | — | 1 | 8.08 |
| CHEMBL88602 | — | — | 1 | 7.96 |
| CHEMBL293226 | — | — | 1 | 7.64 |
| CHEMBL310466 | — | — | 1 | 7.37 |
| CHEMBL88545 | — | — | 1 | 7.06 |
| CHEMBL431212 | — | — | 1 | 6.97 |
| CHEMBL430451 | — | — | 1 | 6.92 |
| CHEMBL89953 | — | — | 1 | 6.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1121 | SINCALIDE | IC50 | = | 1.318 | nM | 8.88 |
| CHEMBL316164 | — | IC50 | = | 8.318 | nM | 8.08 |
| CHEMBL88602 | — | IC50 | = | 10.96 | nM | 7.96 |
| CHEMBL293226 | — | IC50 | = | 22.91 | nM | 7.64 |
| CHEMBL310466 | — | IC50 | = | 42.66 | nM | 7.37 |
| CHEMBL88545 | — | IC50 | = | 87.1 | nM | 7.06 |
| CHEMBL431212 | — | IC50 | = | 107.15 | nM | 6.97 |
| CHEMBL430451 | — | IC50 | = | 120.23 | nM | 6.92 |
| CHEMBL89953 | — | IC50 | = | 309.03 | nM | 6.51 |