Assay Detail
Binding
CHEMBL889348
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Displacement of [3H]BH-CCK-8S from human recombinant CCK2 receptor expressed in NIH3T3 cells
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | NIH3T3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Gastrin/cholecystokinin type B receptor (CHEMBL298) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Optimization of 1,3,4-benzotriazepine-based CCK(2) antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 47 | 8.53 | 9.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL227276 | — | — | 1 | 9.97 |
| CHEMBL324547 | NETAZEPIDE | 2.0 | 1 | 9.86 |
| CHEMBL226583 | — | — | 1 | 9.70 |
| CHEMBL388144 | — | — | 1 | 9.61 |
| CHEMBL387948 | — | — | 1 | 9.55 |
| CHEMBL389711 | — | — | 1 | 9.53 |
| CHEMBL227333 | — | — | 1 | 9.48 |
| CHEMBL227330 | — | — | 1 | 9.47 |
| CHEMBL437736 | — | — | 1 | 9.44 |
| CHEMBL389639 | — | — | 1 | 9.19 |
| CHEMBL227275 | — | — | 1 | 9.18 |
| CHEMBL435143 | — | — | 1 | 9.15 |
| CHEMBL438843 | — | — | 1 | 9.11 |
| CHEMBL226622 | — | — | 1 | 9.10 |
| CHEMBL389713 | — | — | 1 | 9.08 |
| CHEMBL437930 | — | — | 1 | 9.04 |
| CHEMBL226620 | — | — | 1 | 9.00 |
| CHEMBL226533 | — | — | 1 | 9.00 |
| CHEMBL226726 | — | — | 1 | 8.97 |
| CHEMBL388068 | — | — | 1 | 8.92 |
| CHEMBL388143 | — | — | 1 | 8.80 |
| CHEMBL226675 | — | — | 1 | 8.73 |
| CHEMBL227254 | — | — | 1 | 8.71 |
| CHEMBL226673 | — | — | 1 | 8.67 |
| CHEMBL1161950 | — | — | 1 | 8.56 |
| CHEMBL374390 | — | — | 1 | 8.41 |
| CHEMBL541903 | — | — | 1 | 8.39 |
| CHEMBL374389 | — | — | 1 | 8.37 |
| CHEMBL276645 | — | — | 1 | 8.33 |
| CHEMBL227147 | — | — | 1 | 8.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL227276 | — | Ki | = | 0.1072 | nM | 9.97 |
| CHEMBL324547 | NETAZEPIDE | Ki | = | 0.138 | nM | 9.86 |
| CHEMBL226583 | — | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL388144 | — | Ki | = | 0.2455 | nM | 9.61 |
| CHEMBL387948 | — | Ki | = | 0.2818 | nM | 9.55 |
| CHEMBL389711 | — | Ki | = | 0.2951 | nM | 9.53 |
| CHEMBL227333 | — | Ki | = | 0.3311 | nM | 9.48 |
| CHEMBL227330 | — | Ki | = | 0.3388 | nM | 9.47 |
| CHEMBL437736 | — | Ki | = | 0.3631 | nM | 9.44 |
| CHEMBL389639 | — | Ki | = | 0.6457 | nM | 9.19 |
| CHEMBL227275 | — | Ki | = | 0.6607 | nM | 9.18 |
| CHEMBL435143 | — | Ki | = | 0.7079 | nM | 9.15 |
| CHEMBL438843 | — | Ki | = | 0.7762 | nM | 9.11 |
| CHEMBL226622 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL389713 | — | Ki | = | 0.8318 | nM | 9.08 |
| CHEMBL437930 | — | Ki | = | 0.912 | nM | 9.04 |
| CHEMBL226620 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL226533 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL226726 | — | Ki | = | 1.072 | nM | 8.97 |
| CHEMBL388068 | — | Ki | = | 1.202 | nM | 8.92 |
| CHEMBL388143 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL226675 | — | Ki | = | 1.862 | nM | 8.73 |
| CHEMBL227254 | — | Ki | = | 1.95 | nM | 8.71 |
| CHEMBL226673 | — | Ki | = | 2.138 | nM | 8.67 |
| CHEMBL1161950 | — | Ki | = | 2.754 | nM | 8.56 |
| CHEMBL374390 | — | Ki | = | 3.89 | nM | 8.41 |
| CHEMBL541903 | — | Ki | = | 4.074 | nM | 8.39 |
| CHEMBL374389 | — | Ki | = | 4.266 | nM | 8.37 |
| CHEMBL276645 | — | Ki | = | 4.677 | nM | 8.33 |
| CHEMBL227147 | — | Ki | = | 4.786 | nM | 8.32 |
| CHEMBL205455 | — | Ki | = | 5.129 | nM | 8.29 |
| CHEMBL226729 | — | Ki | = | 5.495 | nM | 8.26 |
| CHEMBL374388 | — | Ki | = | 5.623 | nM | 8.25 |
| CHEMBL227277 | — | Ki | = | 6.026 | nM | 8.22 |
| CHEMBL559157 | — | Ki | = | 6.166 | nM | 8.21 |
| CHEMBL390276 | — | Ki | = | 7.586 | nM | 8.12 |
| CHEMBL389933 | — | Ki | = | 9.333 | nM | 8.03 |
| CHEMBL390275 | — | Ki | = | 16.22 | nM | 7.79 |
| CHEMBL541904 | — | Ki | = | 16.98 | nM | 7.77 |
| CHEMBL390519 | — | Ki | = | 19.5 | nM | 7.71 |
| CHEMBL269790 | — | Ki | = | 20.42 | nM | 7.69 |
| CHEMBL227097 | — | Ki | = | 23.99 | nM | 7.62 |
| CHEMBL227369 | — | Ki | = | 23.99 | nM | 7.62 |
| CHEMBL389019 | — | Ki | = | 89.13 | nM | 7.05 |
| CHEMBL226571 | — | Ki | = | 331.13 | nM | 6.48 |
| CHEMBL427277 | — | Ki | = | 489.78 | nM | 6.31 |
| CHEMBL226570 | — | Ki | = | 1202.26 | nM | 5.92 |