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TargetSodium-dependent noradrenaline transporter
LigandBDBM30130
Substrate/CompetitorBDBM22166
Meas. Tech.PDE4 Enzyme Assay
Ki 1560±n/a nM
EC50 1020±n/a nM
Citation Cashman, JRVoelker, TZhang, HTO'Donnell, JM Dual inhibitors of phosphodiesterase-4 and serotonin reuptake. J Med Chem52:1530-9 (2009) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Sodium-dependent noradrenaline 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
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BDBM30130
NameBDBM30130
Synonyms:CHEMBL1201082 | CHEMBL41 | Fluoxetin | Fluoxetine | Prozac | US9120771, Fluoxetine | cid_62857
TypeSmall organic molecule
Emp. Form.C17H18F3NO
Mol. Mass.309.3261
SMILESCNCCC(Oc1ccc(cc1)C(F)(F)F)c1ccccc1
Structure
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BDBM22166
NameBDBM22166
Synonyms:3-(4-iodophenyl)tropane-2-carboxylic acid methyl ester | Beta-CIT | CHEMBL215376 | RTI 55, (exo,exo)-isomer, Iodine (125) labeled | RTI-258 | RTI-55 | [125I]RTI-55 | methyl (1R,2S,3S,5S)-3-(4-iodophenyl)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate
Typeradiolabeled ligand
Emp. Form.C16H20INO2
Mol. Mass.385.24
SMILES[H][C@]12CC[C@]([H])([C@H]([C@H](C1)c1ccc(I)cc1)C(=O)OC)N2C |TLB:16:6:20:3.2|
Structure
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