gabapentin [Ligand Id: 5483] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL940 (CI-945, DM-1796, Gabapentin, Gabapentina, Gabapentine, 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
