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Target
Sodium-dependent dopamine transporter
Ligand
BDBM50054727
Substrate
n/a
Meas. Tech.
ChEMBL_61858 (CHEMBL671002)
IC50
7.3±n/a nM
Citation
 Matecka, D; Rothman, RB; Radesca, L; de Costa, BR; Dersch, CM; Partilla, JS; Pert, A; Glowa, JR; Wojnicki, FH; Rice, KC Development of novel, potent, and selective dopamine reuptake inhibitors through alteration of the piperazine ring of 1-[2-(diphenylmethoxy)ethyl]-and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909). J Med Chem 39:4704-16 (1997) [PubMed]  Article 
Target
Name:
Sodium-dependent dopamine transporter
Synonyms:
DA transporter | Monoamine transporters; Norepininephrine & dopamine | SC6A3_RAT | Slc6a3 | Sodium-dependent dopamine transporter | Sodium-dependent dopamine transporter (DAT)
Type:
Multi-pass membrane protein
Mol. Mass.:
68749.45
Organism:
Rattus norvegicus (rat)
Description:
P23977
Residue:
619
Sequence:
MSKSKCSVGPMSSVVAPAKESNAVGPREVELILVKEQNGVQLTNSTLINPPQTPVEAQERETWSKKIDFLLSVIGFAVDLANVWRFPYLCYKNGGGAFLVPYLLFMVIAGMPLFYMELALGQFNREGAAGVWKICPVLKGVGFTVILISFYVGFFYNVIIAWALHYFFSSFTMDLPWIHCNNTWNSPNCSDAHASNSSDGLGLNDTFGTTPAAEYFERGVLHLHQSRGIDDLGPPRWQLTACLVLVIVLLYFSLWKGVKTSGKVVWITATMPYVVLTALLLRGVTLPGAMDGIRAYLSVDFYRLCEASVWIDAATQVCFSLGVGFGVLIAFSSYNKFTNNCYRDAIITTSINSLTSFSSGFVVFSFLGYMAQKHNVPIRDVATDGPGLIFIIYPEAIATLPLSSAWAAVFFLMLLTLGIDSAMGGMESVITGLVDEFQLLHRHRELFTLGIVLATFLLSLFCVTNGGIYVFTLLDHFAAGTSILFGVLIEAIGVAWFYGVQQFSDDIKQMTGQRPNLYWRLCWKLVSPCFLLYVVVVSIVTFRPPHYGAYIFPDWANALGWIIATSSMAMVPIYATYKFCSLPGSFREKLAYAITPEKDHQLVDRGEVRQFTLRHWLLL
  
Inhibitor
Name:
BDBM50054727
Synonyms:
1,4-Bis-{2-[bis-(4-fluoro-phenyl)-methoxy]-ethyl}-piperazine | CHEMBL102119
Type:
Small organic molecule
Emp. Form.:
C34H34F4N2O2
Mol. Mass.:
578.6396
SMILES:
Fc1ccc(cc1)C(OCCN1CCN(CCOC(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1ccc(F)cc1
Structure:
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