gabapentin [Ligand Id: 5483] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL940 (CI-945, DM-1796, Gabapentin, GOE 3450, GOE-3450, Gralise, Neurontin, NSC-742194, NSC-759254) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Voltage-dependent calcium channel alpha2delta subunit in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3985] [UniProtKB: O77773] | ||||||||
| ChEMBL | Displacement of [3H]gabapentin from calcium channel alpha2delta in pig cerebral cortex membrane after 30 mins | B | 6.85 | pIC50 | 140 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 362-365 [PMID:19897364] |
| ChEMBL | Displacement of [3H]gabapentin from alpha-2delta calcium channel in pig brain membrane | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 2333-2336 [PMID:15946842] |
| Voltage-gated calcium channel alpha2/delta subunit 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1919] [UniProtKB: P54289] | ||||||||
| ChEMBL | Binding affinity towards alpha2-delta subunit of a voltage gated calcium channel using [3H]gabapentin in human brain membrane (A710 membrane) | B | 7.57 | pIC50 | 27 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1913-1916 [PMID:15050626] |
| Voltage-gated calcium channel alpha2/delta subunit 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4676] [UniProtKB: O08532] | ||||||||
| ChEMBL | Displacement of [3H]L-leucine from alpha-2delta containing calcium channel in murine brain | B | 6.92 | pKi | 120.23 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 1138-1141 [PMID:16380257] |
| ChEMBL | Displacement of [3H]L-leucine from alpha-2delta containing calcium channel in murine brain | B | 6.92 | pKi | 120 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 1138-1141 [PMID:16380257] |
| Voltage-gated calcium channel alpha2/delta subunit 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3420] [UniProtKB: P54290] | ||||||||
| ChEMBL | Inhibition of potassium-evoked [3H]norepinephrine release from rat neocortex | F | 5.05 | pIC50 | 8900 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 2333-2336 [PMID:15946842] |
| Kv7.3 in Human [GtoPdb: 562] [UniProtKB: O43525] | ||||||||
| GtoPdb | - | - | 8.28 | pEC50 | 5.3 | nM | EC50 | Mol Pharmacol (2018) 94: 1155-1163 [PMID:30021858] |
| Kv7.5 in Human [GtoPdb: 564] [UniProtKB: Q9NR82] | ||||||||
| GtoPdb | - | - | 8.72 | pEC50 | 1.9 | nM | EC50 | Mol Pharmacol (2018) 94: 1155-1163 [PMID:30021858] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
