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Target
Sodium-dependent noradrenaline transporter
Ligand
BDBM376904
Substrate
n/a
Meas. Tech.
Competition Binding Assay
IC50
275±n/a nM
Citation
 Cremonesi, S; Micheli, F; Semeraro, T; Tarsi, L; Luker, T; Leslie, C N-(hetero)aryl-substituted heteroyclic derivatives useful for the treatment of diseases or conditions related to the central nervous system US Patent  US9920053 Publication Date 3/20/2018 
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:
BDBM376904
Synonyms:
N-({1-[4-(3-fluorophenoxy)-6-(trifluoromethyl)pyrimidin-2-yl]-3-hydroxypyrrolidin-3-yl}methyl)azetidine-3-carboxamide (E35) | US9920053, Example 35
Type:
Small organic molecule
Emp. Form.:
C20H21F4N5O3
Mol. Mass.:
455.4061
SMILES:
OC1(CNC(=O)C2CNC2)CCN(C1)c1nc(Oc2cccc(F)c2)cc(n1)C(F)(F)F
Structure:
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