Target
Sodium-dependent noradrenaline transporter
Ligand
BDBM50275830
Substrate
n/a
Meas. Tech.
ChEMBL_493240 (CHEMBL948470)
IC50
6±n/a nM
Citation
 Dyck, BTamiya, JJovic, FPick, RRBradbury, MJO'Brien, JWen, JJohns, MMadan, AFleck, BAFoster, ACLi, BZhang, MTran, JAVickers, TGrey, JSaunders, JChen, C Characterization of thien-2-yl 1S,2R-milnacipran analogues as potent norepinephrine/serotonin transporter inhibitors for the treatment of neuropathic pain. J Med Chem 51:7265-72 (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:
BDBM50275830
Synonyms:
CHEMBL513248 | N,N-Dipropargyl (1R,2R)-2-(Aminomethyl)-1-(2-thienyl)cyclopropanecarboxamide
Type:
Small organic molecule
Emp. Form.:
C15H16N2OS
Mol. Mass.:
272.365
SMILES:
NC[C@@H]1C[C@@]1(C(=O)N(CC#C)CC#C)c1cccs1 |r|
Structure:
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