Assay Detail
Binding
CHEMBL822825
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Inhibition of specific binding of [3H]gabapentin to Gabapentin binding sites located on the alpha-2-delta subunit of calcium channel.
24
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Identification of novel ligands for the gabapentin binding site on the alpha2delta subunit of a calcium channel and their evaluation as anticonvulsant agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.20 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL553506 | — | — | 1 | 7.38 |
| CHEMBL554650 | — | — | 1 | 7.14 |
| CHEMBL940 | GABAPENTIN | 4.0 | 1 | 6.85 |
| CHEMBL543088 | — | — | 2 | 6.85 |
| CHEMBL538236 | — | — | 1 | 6.55 |
| CHEMBL543321 | — | — | 1 | 6.42 |
| CHEMBL537990 | — | — | 1 | 6.36 |
| CHEMBL538003 | — | — | 1 | 6.16 |
| CHEMBL537998 | — | — | 1 | 6.06 |
| CHEMBL3216409 | — | — | 1 | 5.89 |
| CHEMBL543560 | — | — | 1 | 5.88 |
| CHEMBL542374 | — | — | 1 | 5.62 |
| CHEMBL3216854 | — | — | 1 | 5.48 |
| CHEMBL541295 | — | — | 1 | 5.20 |
| CHEMBL543564 | — | — | 1 | 5.15 |
| CHEMBL539515 | — | — | 1 | - |
| CHEMBL542851 | — | — | 1 | - |
| CHEMBL3215738 | — | — | 1 | - |
| CHEMBL540785 | — | — | 1 | - |
| CHEMBL3215976 | — | — | 1 | - |
| CHEMBL540534 | — | — | 1 | - |
| CHEMBL3215991 | — | — | 1 | - |
| CHEMBL554652 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL553506 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL554650 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL940 | GABAPENTIN | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL543088 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL538236 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL543321 | — | IC50 | = | 385.0 | nM | 6.42 |
| CHEMBL537990 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL538003 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL537998 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL3216409 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL543560 | — | IC50 | = | 1312.0 | nM | 5.88 |
| CHEMBL542374 | — | IC50 | = | 2380.0 | nM | 5.62 |
| CHEMBL3216854 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL541295 | — | IC50 | = | 6270.0 | nM | 5.20 |
| CHEMBL543564 | — | IC50 | = | 7020.0 | nM | 5.15 |
| CHEMBL539515 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL542851 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3215738 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL540785 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL543088 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3215976 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL540534 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3215991 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL554652 | — | IC50 | > | 10000.0 | nM | - |