Target
Sodium-dependent dopamine transporter
Ligand
BDBM50056566
Substrate
n/a
Meas. Tech.
ChEMBL_61846 (CHEMBL670183)
IC50
2.2±n/a nM
Citation
 Matecka, DLewis, DRothman, RBDersch, CMWojnicki, FHGlowa, JRDeVries, ACPert, ARice, KC Heteroaromatic analogs of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as high-affinity dopamine reuptake inhibitors. J Med Chem 40:705-16 (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:
BDBM50056566
Synonyms:
1-{2-[Bis-(4-fluoro-phenyl)-methoxy]-ethyl}-4-((E)-3-thiophen-2-yl-allyl)-piperazine | CHEMBL159320
Type:
Small organic molecule
Emp. Form.:
C26H28F2N2OS
Mol. Mass.:
454.575
SMILES:
Fc1ccc(cc1)C(OCCN1CCN(C\C=C\c2cccs2)CC1)c1ccc(F)cc1
Structure:
Search PDB for entries with ligand similarity: