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TargetMonoamine transporter
LigandBDBM50237600
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1661733
IC50 5060±n/a nM
Citation Tosh, DKJanowsky, AEshleman, AJWarnick, EGao, ZGChen, ZGizewski, EAuchampach, JASalvemini, DJacobson, KA Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters. J Med Chem60:3109-3123 (2017) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Monoamine transporter
Name:Monoamine transporter
Synonyms:NET | Noradrenaline Transporter (NET) | Norepinephrine Transporter (NET) | Norepinephrine transporter protein (NET) | SLC6A2 | Serotonin Transporter (SERT) | 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:Competition binding assay was determined using hNET stably expressed in HEK293 cells.
Residue:617
Sequence:
MLLARMNPQVQPENNGADTGPEQPLRARKTAELLVVKERNGVQCLLAPRDGDAQPRETWG
KKIDFLLSVVGFAVDLANVWRFPYLCYKNGGGAFLIPYTLFLIIAGMPLFYMELALGQYN
REGAATVWKICPFFKGVGYAVILIALYVGFYYNVIIAWSLYYLFSSFTLNLPWTDCGHTW
NSPNCTDPKLLNGSVLGNHTKYSKYKFTPAAEFYERGVLHLHESSGIHDIGLPQWQLLLC
LMVVVIVLYFSLWKGVKTSGKVVWITATLPYFVLFVLLVHGVTLPGASNGINAYLHIDFY
RLKEATVWIDAATQIFFSLGAGFGVLIAFASYNKFDNNCYRDALLTSSINCITSFVSGFA
IFSILGYMAHEHKVNIEDVATEGAGLVFILYPEAISTLSGSTFWAVVFFVMLLALGLDSS
MGGMEAVITGLADDFQVLKRHRKLFTFGVTFSTFLLALFCITKGGIYVLTLLDTFAAGTS
ILFAVLMEAIGVSWFYGVDRFSNDIQQMMGFRPGLYWRLCWKFVSPAFLLFVVVVSIINF
KPLTYDDYIFPPWANWVGWGIALSSMVLVPIYVIYKFLSTQGSLWERLAYGITPENEHHL
VAQRDIRQFQLQHWLAI
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50237600
NameBDBM50237600
Synonyms:CHEMBL4071867
TypeSmall organic molecule
Emp. Form.C21H20ClN5O3S
Mol. Mass.457.933
SMILES[H][C@]12C[C@]1([C@@H](O)[C@@H](O)[C@@H]2n1cnc2c(NC)nc(cc12)C#Cc1ccc(Cl)s1)C(=O)NC |r|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
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