Reaction Details Report a problem with these data
Target
Synaptic vesicular amine transporter
Ligand
BDBM50017701
Substrate
n/a
Meas. Tech.
[3H]TBZOH Binding Assay
pH
7.5000±n/a
Temperature
298.1500±n/a K
IC50
8.3±2.9 nM
Kd
5.2±0.8 nM
Comments
extracted
Citation
 Ugolev, Y; Segal, T; Yaffe, D; Gros, Y; Schuldiner, S Identification of conformationally sensitive residues essential for inhibition of vesicular monoamine transport by the noncompetitive inhibitor tetrabenazine. J Biol Chem 288:32160-71 (2013) [PubMed]  Article 
Target
Name:
Synaptic vesicular amine transporter
Synonyms:
VAT2 | Vesicular amine transporter 2 | Monoamine transporter | Solute carrier family 18 member 2 | Synaptic vesicular amine transporter | VMAT2_RAT | Slc18a2 | Svat | Vmat2 | Vesicular monoamine transporter 2 (VMAT2)
Type:
Protein
Mol. Mass.:
55689.58
Organism:
Rat
Description:
Q01827
Residue:
515
Sequence:
MALSDLVLLRWLRDSRHSRKLILFIVFLALLLDNMLLTVVVPIIPSYLYSIKHEKNSTEIQTTRPELVVSTSESIFSYYNNSTVLITGNATGTLPGGQSHKATSTQHTVANTTVPSDCPSEDRDLLNENVQVGLLFASKATVQLLTNPFIGLLTNRIGYPIPMFAGFCIMFISTVMFAFSSSYAFLLIARSLQGIGSSCSSVAGMGMLASVYTDDEERGKPMGIALGGLAMGVLVGPPFGSVLYEFVGKTAPFLVLAALVLLDGAIQLFVLQPSRVQPESQKGTPLTTLLKDPYILIAAGSICFANMGIAMLEPALPIWMMETMCSRKWQLGVAFLPASISYLIGTNIFGILAHKMGRWLCALLGMVIVGISILCIPFAKNIYGLIAPNFGVGFAIGMVDSSMMPIMGYLVDLRHVSVYGSVYAIADVAFCMGYAIGPSAGGAIAKAIGFPWLMTIIGIIDIAFAPLCFFLRSPPAKEEKMAILMDHNCPIKRKMYTQNNVQSYPIGDDEESESD
  
Inhibitor
Name:
BDBM50017701
Synonyms:
3-isobutyl-9,10-dimethoxy-3,4,6,7-tetrahydro-1H-pyrido[2,1-a]isoquinolin-2(11bH)-one | 3-Isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-pyrido[2,1-a]isoquinolin-2-one | CHEMBL117785 | TETRABENAZINE | Tetrabenazine (TBZ)
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
COc1cc2CCN3CC(CC(C)C)C(=O)CC3c2cc1OC
Structure:
Search PDB for entries with ligand similarity: