Assay Detail
Binding
CHEMBL662400
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Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
115
Total Activities
115
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
Development of 1,4-benzodiazepine cholecystokinin type B antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 115 | 6.51 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2111920 | — | — | 1 | 9.59 |
| CHEMBL2111922 | — | — | 1 | 8.89 |
| CHEMBL434255 | — | — | 1 | 8.52 |
| CHEMBL335951 | — | — | 1 | 8.52 |
| CHEMBL134340 | — | — | 1 | 8.36 |
| CHEMBL70380 | — | — | 1 | 8.33 |
| CHEMBL137398 | — | — | 1 | 8.21 |
| CHEMBL136919 | — | — | 1 | 8.12 |
| CHEMBL137066 | — | — | 1 | 8.09 |
| CHEMBL136408 | — | — | 1 | 8.08 |
| CHEMBL132603 | — | — | 1 | 8.05 |
| CHEMBL335666 | — | — | 1 | 8.00 |
| CHEMBL137043 | — | — | 1 | 7.96 |
| CHEMBL136412 | — | — | 1 | 7.85 |
| CHEMBL2112751 | — | — | 1 | 7.68 |
| CHEMBL135702 | — | — | 1 | 7.58 |
| CHEMBL334592 | — | — | 1 | 7.47 |
| CHEMBL132875 | — | — | 1 | 7.43 |
| CHEMBL336749 | — | — | 1 | 7.34 |
| CHEMBL342614 | — | — | 1 | 7.25 |
| CHEMBL343767 | — | — | 1 | 7.24 |
| CHEMBL2112753 | — | — | 1 | 7.22 |
| CHEMBL336972 | — | — | 1 | 7.21 |
| CHEMBL137567 | — | — | 1 | 7.21 |
| CHEMBL82685 | — | — | 1 | 7.19 |
| CHEMBL135364 | — | — | 1 | 7.17 |
| CHEMBL135498 | — | — | 1 | 6.98 |
| CHEMBL355092 | — | — | 1 | 6.96 |
| CHEMBL40668 | — | — | 1 | 6.96 |
| CHEMBL135715 | — | — | 1 | 6.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2111920 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL2111922 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL434255 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL335951 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL134340 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL70380 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL137398 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL136919 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL137066 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL136408 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL132603 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL335666 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL137043 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL136412 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2112751 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL135702 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL334592 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL132875 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL336749 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL342614 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL343767 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL2112753 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL336972 | — | IC50 | = | 61.4 | nM | 7.21 |
| CHEMBL137567 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL82685 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL135364 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL135498 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL40668 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL135715 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL355092 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL335865 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL137516 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL135060 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL134750 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL135909 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL2112754 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL137684 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL137726 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL135289 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL135218 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL136608 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL337722 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL137240 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL417521 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL336221 | — | IC50 | = | 258.0 | nM | 6.59 |
| CHEMBL342201 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL2111924 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL135433 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL137238 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL135167 | — | IC50 | = | 310.0 | nM | 6.51 |