tetrabenazine [Ligand Id: 4834] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL117785 (Xenazine 25, Ro-19569, NSC-169886, Nitoman, Xenazine, Tetrabenazine, RO-1-9569, Revocon, Tetmodis)
  • Vesicular monoamine transporter 2 in Human [GtoPdb: 1012] [UniProtKB: Q05940]
  • Synaptic vesicular amine transporter in Bovine [ChEMBL: CHEMBL4271] [UniProtKB: Q27963]
  • Vesicular monoamine transporter 2/Synaptic vesicular amine transporter in Rat [ChEMBL: CHEMBL4828] [GtoPdb: 1012] [UniProtKB: Q01827]
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  • Vesicular monoamine transporter 1 in Human [GtoPdb: 1011] [UniProtKB: P54219]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Vesicular monoamine transporter 2 in Human [GtoPdb: 1012] [UniProtKB: Q05940]
GtoPdb - - 7 pKi 97 nM Ki Proc. Natl. Acad. Sci. U.S.A. (1996) 93: 5166-71 [PMID:8643547]
Synaptic vesicular amine transporter in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4271] [UniProtKB: Q27963]
ChEMBL Inhibition of dopamine uptake at VMAT in bovine chromaffin granule ghosts B 8.4 pKi 4 nM Ki J. Med. Chem. (2008) 51: 760-768 [PMID:18220329]
Vesicular monoamine transporter 2/Synaptic vesicular amine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4828] [GtoPdb: 1012] [UniProtKB: Q01827]
ChEMBL Inhibition of [3H]dopamine uptake at VMAT2 in rat brain synaptic vesicle by liquid scintillation spectroscopy B 7.27 pKi 54 nM Ki J. Med. Chem. (2009) 52: 7878-7882 [PMID:19691331]
ChEMBL Displacement of [3H]DTBZ from VMAT2 dihydrotetrabenazine binding site in rat brain synaptic vesicle by scintillation counting B 7.89 pKi 13 nM Ki J. Med. Chem. (2009) 52: 7878-7882 [PMID:19691331]
ChEMBL Displacement of [3H]MTBZ from VMAT2 in rat whole brain vesicles by liquid scintillation spectrophotometry B 7.89 pKi 13 nM Ki Bioorg. Med. Chem. (2010) 18: 640-649 [PMID:20036131]
ChEMBL Displacement of [3H]DHTBZ from Sprague-Dawley rat striatum VMAT2 after 1 hr by liquid scintillation counting B 8.12 pKi 7.62 nM Ki Eur. J. Med. Chem. (2011) 46: 1841-1848 [PMID:21396745]
Vesicular monoamine transporter 1 in Human [GtoPdb: 1011] [UniProtKB: P54219]
GtoPdb - - 4.7 pKi 20000 nM Ki Proc. Natl. Acad. Sci. U.S.A. (1996) 93: 5166-71 [PMID:8643547]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]