Assay Detail
Binding
CHEMBL662430
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
42
Total Activities
32
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
Cholecystokinin dipeptoid antagonists: design, synthesis, and anxiolytic profile of some novel CCK-A and CCK-B selective and "mixed" CCK-A/CCK-B antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 6.92 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL9506 | DEVAZEPIDE | 2.0 | 1 | 10.00 |
| CHEMBL1121 | SINCALIDE | 4.0 | 1 | 10.00 |
| CHEMBL2111204 | — | — | 1 | 8.55 |
| CHEMBL3349028 | — | — | 7 | 8.41 |
| CHEMBL153095 | — | — | 1 | 8.05 |
| CHEMBL2111261 | — | — | 1 | 7.59 |
| CHEMBL153787 | — | — | 1 | 7.33 |
| CHEMBL152682 | — | — | 3 | 7.18 |
| CHEMBL3350686 | — | — | 1 | 7.18 |
| CHEMBL359292 | — | — | 1 | 7.16 |
| CHEMBL359076 | — | — | 1 | 6.81 |
| CHEMBL317675 | — | — | 1 | 6.73 |
| CHEMBL357027 | — | — | 1 | 6.71 |
| CHEMBL9387 | L-365260 | — | 1 | 6.64 |
| CHEMBL437039 | — | — | 3 | 6.60 |
| CHEMBL291033 | — | — | 1 | 6.42 |
| CHEMBL436065 | — | — | 1 | 6.41 |
| CHEMBL356419 | — | — | 1 | 6.36 |
| CHEMBL345303 | — | — | 1 | 6.29 |
| CHEMBL2304064 | — | — | 1 | 6.27 |
| CHEMBL1328 | PENTAGASTRIN | 4.0 | 1 | 6.22 |
| CHEMBL356810 | — | — | 1 | 6.20 |
| CHEMBL153760 | — | — | 1 | 6.15 |
| CHEMBL356599 | — | — | 1 | 6.13 |
| CHEMBL423329 | — | — | 1 | 6.11 |
| CHEMBL357564 | — | — | 1 | 6.11 |
| CHEMBL356446 | — | — | 1 | 6.11 |
| CHEMBL345512 | — | — | 1 | 6.10 |
| CHEMBL359361 | — | — | 1 | 6.02 |
| CHEMBL347278 | — | — | 1 | 5.98 |
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 |
| CHEMBL2111204 | — | IC50 | = | 2.82 | nM | 8.55 |
| CHEMBL3349028 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3349028 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL153095 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL3349028 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3349028 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3349028 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2111261 | — | IC50 | = | 25.5 | nM | 7.59 |
| CHEMBL153787 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL152682 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL3350686 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL359292 | — | IC50 | = | 69.7 | nM | 7.16 |
| CHEMBL3349028 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL152682 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL359076 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL317675 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL357027 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL9387 | L-365260 | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL437039 | — | IC50 | = | 251.0 | nM | 6.60 |
| CHEMBL152682 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL437039 | — | IC50 | = | 266.0 | nM | 6.58 |
| CHEMBL3349028 | — | IC50 | = | 288.0 | nM | 6.54 |
| CHEMBL437039 | — | IC50 | = | 288.0 | nM | 6.54 |
| CHEMBL291033 | — | IC50 | = | 377.0 | nM | 6.42 |
| CHEMBL436065 | — | IC50 | = | 391.0 | nM | 6.41 |
| CHEMBL356419 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL345303 | — | IC50 | = | 511.0 | nM | 6.29 |
| CHEMBL2304064 | — | IC50 | = | 539.0 | nM | 6.27 |
| CHEMBL1328 | PENTAGASTRIN | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL356810 | — | IC50 | = | 625.0 | nM | 6.20 |
| CHEMBL153760 | — | IC50 | = | 711.0 | nM | 6.15 |
| CHEMBL356599 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL423329 | — | IC50 | = | 775.0 | nM | 6.11 |
| CHEMBL357564 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL356446 | — | IC50 | = | 785.0 | nM | 6.11 |
| CHEMBL345512 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL359361 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL347278 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL153557 | — | IC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL345511 | — | IC50 | = | 4300.0 | nM | 5.37 |