Assay Detail
Binding
CHEMBL866241
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]gabapentin from alpha-2delta calcium channel in pig brain membrane
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Voltage-dependent calcium channel alpha2delta subunit (CHEMBL3985) ↗| Type | SINGLE PROTEIN |
| Organism | Sus scrofa |
Publication
Heteroaromatic side-chain analogs of pregabalin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.31 | 7.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1059 | PREGABALIN | 4.0 | 1 | 7.14 |
| CHEMBL208216 | — | — | 1 | 6.75 |
| CHEMBL382876 | — | — | 1 | 6.38 |
| CHEMBL381742 | — | — | 1 | 6.29 |
| CHEMBL382417 | — | — | 1 | 6.08 |
| CHEMBL377707 | — | — | 1 | 5.84 |
| CHEMBL208302 | — | — | 1 | 5.67 |
| CHEMBL206142 | — | — | 1 | - |
| CHEMBL205704 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1059 | PREGABALIN | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL208216 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL382876 | — | IC50 | = | 421.0 | nM | 6.38 |
| CHEMBL381742 | — | IC50 | = | 518.0 | nM | 6.29 |
| CHEMBL382417 | — | IC50 | = | 832.0 | nM | 6.08 |
| CHEMBL377707 | — | IC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL208302 | — | IC50 | = | 2140.0 | nM | 5.67 |
| CHEMBL206142 | — | IC50 | > | 10000000.0 | nM | - |
| CHEMBL205704 | — | IC50 | > | 10000000.0 | nM | - |