Assay Detail
Binding
CHEMBL663173
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Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type B receptor in the mouse cerebral cortex
34
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Gastrin/cholecystokinin type B receptor (CHEMBL2854) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 7.58 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL138534 | — | — | 1 | 9.82 |
| CHEMBL141370 | — | — | 1 | 9.00 |
| CHEMBL2062154 | CI-988 | 1.0 | 1 | 8.77 |
| CHEMBL138233 | — | — | 1 | 8.60 |
| CHEMBL138084 | — | — | 1 | 8.52 |
| CHEMBL138112 | — | — | 1 | 8.46 |
| CHEMBL344882 | — | — | 1 | 8.33 |
| CHEMBL344380 | — | — | 1 | 8.21 |
| CHEMBL138657 | — | — | 1 | 8.20 |
| CHEMBL337529 | — | — | 1 | 8.19 |
| CHEMBL141630 | — | — | 1 | 8.03 |
| CHEMBL342932 | — | — | 1 | 7.91 |
| CHEMBL2112795 | — | — | 1 | 7.85 |
| CHEMBL344211 | — | — | 1 | 7.71 |
| CHEMBL138952 | — | — | 1 | 7.70 |
| CHEMBL139601 | — | — | 1 | 7.59 |
| CHEMBL62205 | — | — | 2 | 7.50 |
| CHEMBL337310 | — | — | 1 | 7.41 |
| CHEMBL263969 | — | — | 1 | 7.37 |
| CHEMBL140073 | — | — | 1 | 7.34 |
| CHEMBL138311 | — | — | 1 | 7.30 |
| CHEMBL342907 | — | — | 1 | 7.18 |
| CHEMBL436411 | — | — | 2 | 7.11 |
| CHEMBL139001 | — | — | 1 | 7.08 |
| CHEMBL139101 | — | — | 1 | 6.92 |
| CHEMBL142063 | — | — | 1 | 6.88 |
| CHEMBL344220 | — | — | 1 | 6.72 |
| CHEMBL341560 | — | — | 1 | 6.67 |
| CHEMBL138190 | — | — | 1 | 6.57 |
| CHEMBL140701 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL138534 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL141370 | — | IC50 | = | 0.99 | nM | 9.00 |
| CHEMBL2062154 | CI-988 | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL138233 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL138084 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL138112 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL344882 | — | IC50 | = | 4.65 | nM | 8.33 |
| CHEMBL344380 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL138657 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL337529 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL141630 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL342932 | — | IC50 | = | 12.2 | nM | 7.91 |
| CHEMBL2112795 | — | IC50 | = | 14.2 | nM | 7.85 |
| CHEMBL344211 | — | IC50 | = | 19.7 | nM | 7.71 |
| CHEMBL138952 | — | IC50 | = | 19.9 | nM | 7.70 |
| CHEMBL139601 | — | IC50 | = | 25.5 | nM | 7.59 |
| CHEMBL62205 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL337310 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL263969 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL140073 | — | IC50 | = | 45.5 | nM | 7.34 |
| CHEMBL62205 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL138311 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL342907 | — | IC50 | = | 65.4 | nM | 7.18 |
| CHEMBL436411 | — | IC50 | = | 78.5 | nM | 7.11 |
| CHEMBL139001 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL139101 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL142063 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL436411 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL344220 | — | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL341560 | — | IC50 | = | 213.5 | nM | 6.67 |
| CHEMBL138190 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL140701 | — | IC50 | = | 314.0 | nM | 6.50 |
| CHEMBL443284 | — | IC50 | = | 327.0 | nM | 6.49 |
| CHEMBL138127 | — | IC50 | = | 1766.0 | nM | 5.75 |