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Target
Sodium-dependent noradrenaline transporter
Ligand
BDBM50254830
Substrate
n/a
Meas. Tech.
ChEMBL_560769 (CHEMBL1011736)
Ki
6567±n/a nM
Citation
 Cashman, JR; Voelker, T; Johnson, R; Janowsky, A Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression. Bioorg Med Chem 17:337-43 (2008) [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:
BDBM50254830
Synonyms:
4-(3,4-dimethoxyphenyl)-2-(5-((R)-3-phenyl-3-(4-(trifluoromethyl)phenoxy)propylamino)pentyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one | CHEMBL499461
Type:
Small organic molecule
Emp. Form.:
C37H42F3N3O4
Mol. Mass.:
649.7423
SMILES:
COc1ccc(cc1OC)C1=NN(CCCCCNCC[C@@H](Oc2ccc(cc2)C(F)(F)F)c2ccccc2)C(=O)C2CC=CCC12 |r,c:46,t:11|
Structure:
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