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Target
Sodium-dependent noradrenaline transporter
Ligand
BDBM35239
Substrate
BDBM35234
Meas. Tech.
Norepinephrine Uptake Assay (IC50)
pH
7.4±n/a
Temperature
310.15±n/a K
Comments
Less than 10% inhibition @ 1000 nM.
Citation
 Heffernan, GD; Coghlan, RD; Manas, ES; McDevitt, RE; Li, Y; Mahaney, PE; Robichaud, AJ; Huselton, C; Alfinito, P; Bray, JA; Cosmi, SA; Johnston, GH; Kenney, T; Koury, E; Winneker, RC; Deecher, DC; Trybulski, EJ Dual acting norepinephrine reuptake inhibitors and 5-HT(2A) receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles. Bioorg Med Chem 17:7802-15 (2009) [PubMed]  Article 
Target
Name:
Sodium-dependent noradrenaline transporter
Synonyms:
Monoamine transporter | NAT1 | NET | NET1 | Noradrenaline Transporter (NET) | Norepinephrine Transporter (NET) | Norepinephrine transporter protein (NET) | SC6A2_HUMAN | SLC6A2 | SLC6A5 | Sodium-dependent noradrenaline transporter (NET) | Solute carrier family 6 member 2
Type:
Multi-pass membrane protein
Mol. Mass.:
69337.72
Organism:
Homo sapiens (Human)
Description:
P23975
Residue:
617
Sequence:
MLLARMNPQVQPENNGADTGPEQPLRARKTAELLVVKERNGVQCLLAPRDGDAQPRETWGKKIDFLLSVVGFAVDLANVWRFPYLCYKNGGGAFLIPYTLFLIIAGMPLFYMELALGQYNREGAATVWKICPFFKGVGYAVILIALYVGFYYNVIIAWSLYYLFSSFTLNLPWTDCGHTWNSPNCTDPKLLNGSVLGNHTKYSKYKFTPAAEFYERGVLHLHESSGIHDIGLPQWQLLLCLMVVVIVLYFSLWKGVKTSGKVVWITATLPYFVLFVLLVHGVTLPGASNGINAYLHIDFYRLKEATVWIDAATQIFFSLGAGFGVLIAFASYNKFDNNCYRDALLTSSINCITSFVSGFAIFSILGYMAHEHKVNIEDVATEGAGLVFILYPEAISTLSGSTFWAVVFFVMLLALGLDSSMGGMEAVITGLADDFQVLKRHRKLFTFGVTFSTFLLALFCITKGGIYVLTLLDTFAAGTSILFAVLMEAIGVSWFYGVDRFSNDIQQMMGFRPGLYWRLCWKFVSPAFLLFVVVVSIINFKPLTYDDYIFPPWANWVGWGIALSSMVLVPIYVIYKFLSTQGSLWERLAYGITPENEHHLVAQRDIRQFQLQHWLAI
  
Inhibitor
Name:
BDBM35239
Synonyms:
3-(phenylsulfonyl)-1H-indole, 28b
Type:
Small organic molecule
Emp. Form.:
C19H22N2O2S
Mol. Mass.:
342.455
SMILES:
CCN(C)CCc1cccc2c(c[nH]c12)S(=O)(=O)c1ccccc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM35234
Synonyms:
DL-[7-3H]norepinephrine | NOREPINEPHRINE | Noradrenaline,(+) | [3H]NE
Type:
radiolabeled ligand
Emp. Form.:
C8H11NO3
Mol. Mass.:
169.1778
SMILES:
NCC(O)c1ccc(O)c(O)c1
Structure:
Search PDB for entries with ligand similarity: