Assay Detail
Binding
CHEMBL641407
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards alpha2-delta subunit of a voltage gated calcium channel using [3H]gabapentin in human brain membrane (A710 membrane)
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Voltage-dependent calcium channel subunit alpha-2/delta-1 (CHEMBL1919) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
N-Acridin-9-yl-butane-1,4-diamine derivatives: high-affinity ligands of the alpha2delta subunit of voltage gated calcium channels.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.38 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL418138 | — | — | 1 | 8.05 |
| CHEMBL57657 | — | — | 1 | 7.75 |
| CHEMBL940 | GABAPENTIN | 4.0 | 1 | 7.57 |
| CHEMBL57487 | — | — | 1 | 7.42 |
| CHEMBL56743 | — | — | 1 | 7.37 |
| CHEMBL299461 | — | — | 1 | 7.28 |
| CHEMBL56397 | — | — | 1 | 6.96 |
| CHEMBL58047 | — | — | 1 | 6.80 |
| CHEMBL59367 | — | — | 1 | 6.66 |
| CHEMBL59368 | — | — | 1 | 6.57 |
| CHEMBL292915 | — | — | 1 | 6.38 |
| CHEMBL300325 | — | — | 1 | 6.12 |
| CHEMBL59208 | — | — | 1 | 6.02 |
| CHEMBL56880 | — | — | 1 | 5.96 |
| CHEMBL56754 | — | — | 1 | 5.29 |
| CHEMBL293816 | — | — | 1 | 5.23 |
| CHEMBL59089 | — | — | 1 | 5.22 |
| CHEMBL299681 | — | — | 1 | 5.00 |
| CHEMBL292822 | — | — | 1 | 4.96 |
| CHEMBL61092 | — | — | 1 | 4.89 |
| CHEMBL57635 | — | — | 1 | - |
| CHEMBL57766 | — | — | 1 | - |
| CHEMBL58526 | — | — | 1 | - |
| CHEMBL58470 | — | — | 1 | - |
| CHEMBL56482 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL418138 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL57657 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL940 | GABAPENTIN | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL57487 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL56743 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL299461 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL56397 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL58047 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL59367 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL59368 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL292915 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL300325 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL59208 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL56880 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL56754 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL293816 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL59089 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL299681 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL292822 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL61092 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL57635 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL57766 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL58526 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL58470 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL56482 | — | IC50 | > | 10000.0 | nM | - |