tetrabenazine [Ligand Id: 4834] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| Vesicular monoamine transporter 2/Synaptic vesicular amine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1893] [GtoPdb: 1012] [UniProtKB: Q05940] | ||||||||
| GtoPdb | - | - | 7 | pKi | 97 | nM | Ki | Proc Natl Acad Sci USA (1996) 93: 5166-71 [PMID:8643547] |
| ChEMBL | Substrate uptake and inhibition of the Vesicular Amine Transporter 2 (VMAT2, SLC18A2) as assessed by uptake of a fluorescent substrate (FFN206) in HEK-293 JumpIN-SLC18A2 cells (PubChem AID: 1794817) | F | 7.7 | pIC50 | 19.8 | nM | IC50 | FFN206 based assay for SLC18A2 using HEK-293 SLC18A2 OE cells |
| 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/Vesicular amine transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1838] [GtoPdb: 1011] [UniProtKB: P54219] | ||||||||
| GtoPdb | - | - | 4.7 | pKi | 20000 | nM | Ki | Proc Natl Acad Sci USA (1996) 93: 5166-71 [PMID:8643547] |
| ChEMBL | Substrate uptake and inhibition of the chromaffin granule amine transporter (VAT1, VMAT1, SLC18A1) as assessed by uptake of a fluorescent substrate (FFN206) in HEK-293 JumpIN-SLC18A1 cells (PubChem AID: 1794818) | F | 5 | pIC50 | >10000 | nM | IC50 | FFN206 based assay for SLC18A1 using HEK-293 SLC18A1 OE cells |
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]
