Assay Detail
Binding
CHEMBL1781077
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]gabapentin from voltage gated calcium channel alpha2delta from pig cerebral cortex by scintillation counting
28
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Tissue | Cerebral cortex |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Part 2: Design, synthesis and evaluation of hydroxyproline-derived α2δ ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.12 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1778785 | — | — | 1 | 8.40 |
| CHEMBL1778875 | — | — | 1 | 8.15 |
| CHEMBL1778788 | — | — | 1 | 7.96 |
| CHEMBL1778874 | — | — | 1 | 7.85 |
| CHEMBL1778791 | — | — | 1 | 7.77 |
| CHEMBL1778873 | — | — | 1 | 7.58 |
| CHEMBL1778789 | — | — | 1 | 7.52 |
| CHEMBL1778783 | — | — | 1 | 7.50 |
| CHEMBL1778767 | — | — | 1 | 7.32 |
| CHEMBL1778792 | — | — | 1 | 7.28 |
| CHEMBL1778782 | — | — | 1 | 7.14 |
| CHEMBL1059 | PREGABALIN | 4.0 | 1 | 7.10 |
| CHEMBL1778872 | — | — | 1 | 7.03 |
| CHEMBL1778786 | — | — | 1 | 6.99 |
| CHEMBL940 | GABAPENTIN | 4.0 | 1 | 6.85 |
| CHEMBL1778780 | — | — | 1 | 6.71 |
| CHEMBL1778793 | — | — | 1 | 6.57 |
| CHEMBL1778877 | — | — | 1 | 6.49 |
| CHEMBL1778787 | — | — | 1 | 6.40 |
| CHEMBL1778779 | — | — | 1 | 6.28 |
| CHEMBL1778876 | — | — | 2 | 5.90 |
| CHEMBL1778790 | — | — | 1 | 5.78 |
| CHEMBL1778784 | — | — | 1 | - |
| CHEMBL1778871 | — | — | 1 | - |
| CHEMBL1778781 | — | — | 1 | - |
| CHEMBL1778878 | — | — | 1 | - |
| CHEMBL1778879 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1778785 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1778875 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1778788 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1778874 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1778791 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1778873 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1778789 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1778783 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1778767 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL1778792 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL1778782 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL1059 | PREGABALIN | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1778872 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL1778786 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL940 | GABAPENTIN | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1778780 | — | IC50 | = | 195.0 | nM | 6.71 |
| CHEMBL1778793 | — | IC50 | = | 269.0 | nM | 6.57 |
| CHEMBL1778877 | — | IC50 | = | 325.0 | nM | 6.49 |
| CHEMBL1778787 | — | IC50 | = | 399.0 | nM | 6.40 |
| CHEMBL1778779 | — | IC50 | = | 523.0 | nM | 6.28 |
| CHEMBL1778876 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL1778790 | — | IC50 | = | 1680.0 | nM | 5.78 |
| CHEMBL1778871 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1778784 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1778876 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1778781 | — | IC50 | > | 8000.0 | nM | - |
| CHEMBL1778878 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1778879 | — | IC50 | > | 1000.0 | nM | - |