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ChEMBL ligand: CHEMBL117785 (Nitoman, NSC-169886, Revocon, RO 1-9569, RO-1-9569, RO-19569, Tetmodis, Tetrabenazine, Xenazine, Xenazine 25) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Vesicular monoamine transporter 2 in Human [GtoPdb: 1012] [UniProtKB: Q05940] | ||||||||
GtoPdb | - | - | 7 | pKi | 97 | nM | Ki | Proc Natl Acad Sci USA (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 USA (1996) 93: 5166-71 [PMID:8643547] |
ChEMBL data shown on this page come from version 32:
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]