Assay Detail
Binding
CHEMBL1014616
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Displacement of [3H]gabapentin from alpha2-delta subunit of voltage gated calcium channel in pig brain membrane
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Oxadiazolone bioisosteres of pregabalin and gabapentin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.60 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL940 | GABAPENTIN | 4.0 | 1 | 7.16 |
| CHEMBL464046 | — | — | 1 | 7.16 |
| CHEMBL1059 | PREGABALIN | 4.0 | 1 | 7.10 |
| CHEMBL464045 | — | — | 1 | 7.08 |
| CHEMBL258019 | — | — | 1 | 7.00 |
| CHEMBL442646 | — | — | 1 | 6.80 |
| CHEMBL404384 | — | — | 1 | 6.68 |
| CHEMBL452981 | — | — | 1 | 5.94 |
| CHEMBL444244 | — | — | 1 | 5.82 |
| CHEMBL464044 | — | — | 1 | 5.25 |
| CHEMBL378431 | — | — | 1 | - |
| CHEMBL507012 | — | — | 1 | - |
| CHEMBL464908 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL940 | GABAPENTIN | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL464046 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1059 | PREGABALIN | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL464045 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL258019 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL442646 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL404384 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL452981 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL444244 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL464044 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL378431 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL507012 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL464908 | — | IC50 | > | 10000.0 | nM | - |