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Target
Sodium-dependent dopamine transporter
Ligand
BDBM22412
Substrate
BDBM22397
Meas. Tech.
Ligand Binding Assay
pH
7.4±n/a
Temperature
277.15±n/a K
IC50
4±1 nM
Citation
 Gong, PK; Blough, BE; Brieaddy, LE; Huang, X; Kuhar, MJ; Navarro, HA; Carroll, FI Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2 beta-[5-(substituted phenyl)thiazol-2-yl]tropanes. J Med Chem 50:3686-95 (2007) [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:
BDBM22412
Synonyms:
2-[(1R,2S,3S,5S)-8-methyl-3-(4-methylphenyl)-8-azabicyclo[3.2.1]octan-2-yl]-5-(3-nitrophenyl)-1,3-thiazole | WIN 35,065-2 Analogue, 4p
Type:
Small organic molecule
Emp. Form.:
C24H25N3O2S
Mol. Mass.:
419.539
SMILES:
CN1[C@H]2CC[C@@H]1[C@H]([C@H](C2)c1ccc(C)cc1)c1ncc(s1)-c1cccc(c1)[N+]([O-])=O |TLB:0:1:4.3:7.8.6|
Structure:
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Substrate
Name:
BDBM22397
Synonyms:
WIN 35,428 | [3H]WIN 35,428 | methyl (1R,2S,3S,5S)-3-(4-fluorophenyl)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate
Type:
radiolabeled ligand
Emp. Form.:
C16H20FNO2
Mol. Mass.:
277.3339
SMILES:
COC(=O)[C@@H]1[C@H]2CC[C@@H](C[C@@H]1c1ccc(F)cc1)N2C |TLB:19:18:6.7:10.9.4|
Structure:
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