Target
Sodium-dependent dopamine transporter
Ligand
BDBM30133
Substrate
BDBM22166
Meas. Tech.
Radioligand Binding Assay (Ki) and Inhibition of Substrate Uptake (EC50/IC50)
pH
7.4±n/a
Temperature
295.15±n/a K
Ki
66988±14450 nM
EC50
>100000±n/a nM
Citation
 Cashman, JRVoelker, TZhang, HTO'Donnell, JM Dual inhibitors of phosphodiesterase-4 and serotonin reuptake. J Med Chem 52:1530-9 (2009) [PubMed]  Article 
Target
Name:
Sodium-dependent dopamine transporter
Synonyms:
DA transporter | DAT | DAT1 | Dopamine transporter (DAT) | Dopamine transporter protein (DAT) | Monoamine transporter | SC6A3_HUMAN | SLC6A3 | Sodium-dependent dopamine transporter | Sodium-dependent dopamine transporter (DAT) | Solute carrier family 6 member 3
Type:
Multi-pass membrane protein
Mol. Mass.:
68497.11
Organism:
Homo sapiens (Human)
Description:
Q01959
Residue:
620
Sequence:
MSKSKCSVGLMSSVVAPAKEPNAVGPKEVELILVKEQNGVQLTSSTLTNPRQSPVEAQDRETWGKKIDFLLSVIGFAVDLANVWRFPYLCYKNGGGAFLVPYLLFMVIAGMPLFYMELALGQFNREGAAGVWKICPILKGVGFTVILISLYVGFFYNVIIAWALHYLFSSFTTELPWIHCNNSWNSPNCSDAHPGDSSGDSSGLNDTFGTTPAAEYFERGVLHLHQSHGIDDLGPPRWQLTACLVLVIVLLYFSLWKGVKTSGKVVWITATMPYVVLTALLLRGVTLPGAIDGIRAYLSVDFYRLCEASVWIDAATQVCFSLGVGFGVLIAFSSYNKFTNNCYRDAIVTTSINSLTSFSSGFVVFSFLGYMAQKHSVPIGDVAKDGPGLIFIIYPEAIATLPLSSAWAVVFFIMLLTLGIDSAMGGMESVITGLIDEFQLLHRHRELFTLFIVLATFLLSLFCVTNGGIYVFTLLDHFAAGTSILFGVLIEAIGVAWFYGVGQFSDDIQQMTGQRPSLYWRLCWKLVSPCFLLFVVVVSIVTFRPPHYGAYIFPDWANALGWVIATSSMAMVPIYAAYKFCSLPGSFREKLAYAIAPEKDRELVDRGEVRQFTLRHWLKV
  
Inhibitor
Name:
BDBM30133
Synonyms:
tetrahydrofuranyl ethylamine, 24
Type:
Small organic molecule
Emp. Form.:
C16H24FNO2
Mol. Mass.:
281.3657
SMILES:
CNCCC1CCC(CCc2cc(F)ccc2OC)O1
Structure:
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Substrate
Name:
BDBM22166
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
Type:
radiolabeled 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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