Assay Detail
Binding
CHEMBL662429
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Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
27
Total Activities
26
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
Amide bond replacements incorporated into CCK-B selective "dipeptoids".
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.14 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2062154 | CI-988 | 1.0 | 1 | 8.77 |
| CHEMBL291033 | — | — | 1 | 7.50 |
| CHEMBL287079 | — | — | 1 | 7.41 |
| CHEMBL284361 | — | — | 1 | 7.15 |
| CHEMBL36443 | — | — | 1 | 6.91 |
| CHEMBL35580 | — | — | 1 | 6.26 |
| CHEMBL285880 | — | — | 1 | 6.22 |
| CHEMBL1237153 | — | — | 1 | 6.11 |
| CHEMBL286843 | — | — | 1 | 6.10 |
| CHEMBL287682 | — | — | 1 | 6.09 |
| CHEMBL285049 | — | — | 1 | 6.07 |
| CHEMBL289239 | — | — | 1 | 6.06 |
| CHEMBL288038 | — | — | 1 | 6.03 |
| CHEMBL288037 | — | — | 1 | 5.97 |
| CHEMBL35555 | — | — | 1 | 5.97 |
| CHEMBL280502 | — | — | 1 | 5.91 |
| CHEMBL445094 | — | — | 1 | 5.90 |
| CHEMBL422941 | — | — | 1 | 5.84 |
| CHEMBL34300 | — | — | 1 | 5.80 |
| CHEMBL286664 | — | — | 1 | 5.79 |
| CHEMBL37903 | — | — | 1 | 5.72 |
| CHEMBL2112071 | — | — | 1 | 5.71 |
| CHEMBL286442 | — | — | 2 | 5.60 |
| CHEMBL34422 | — | — | 1 | 5.20 |
| CHEMBL286093 | — | — | 1 | 5.06 |
| CHEMBL285762 | — | — | 1 | 4.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2062154 | CI-988 | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL291033 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL287079 | — | IC50 | = | 38.8 | nM | 7.41 |
| CHEMBL284361 | — | IC50 | = | 71.2 | nM | 7.15 |
| CHEMBL36443 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL35580 | — | IC50 | = | 547.0 | nM | 6.26 |
| CHEMBL285880 | — | IC50 | = | 595.0 | nM | 6.22 |
| CHEMBL1237153 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL286843 | — | IC50 | = | 801.0 | nM | 6.10 |
| CHEMBL287682 | — | IC50 | = | 808.0 | nM | 6.09 |
| CHEMBL285049 | — | IC50 | = | 852.0 | nM | 6.07 |
| CHEMBL289239 | — | IC50 | = | 863.0 | nM | 6.06 |
| CHEMBL288038 | — | IC50 | = | 932.0 | nM | 6.03 |
| CHEMBL288037 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL35555 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL280502 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL445094 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL422941 | — | IC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL34300 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL286664 | — | IC50 | = | 1630.0 | nM | 5.79 |
| CHEMBL37903 | — | IC50 | = | 1890.0 | nM | 5.72 |
| CHEMBL2112071 | — | IC50 | = | 1970.0 | nM | 5.71 |
| CHEMBL286442 | — | IC50 | = | 2510.0 | nM | 5.60 |
| CHEMBL286442 | — | IC50 | = | 2580.0 | nM | 5.59 |
| CHEMBL34422 | — | IC50 | = | 6340.0 | nM | 5.20 |
| CHEMBL286093 | — | IC50 | = | 8690.0 | nM | 5.06 |
| CHEMBL285762 | — | IC50 | = | 11500.0 | nM | 4.94 |