Target
Sodium-dependent dopamine transporter
Ligand
BDBM287955
Substrate
n/a
Meas. Tech.
Assay for Dopamine Reuptake Inhibition
pH
7.4±n/a
EC50
62.0±15 nM
Comments
extracted
Citation
 Ananthan, SRothman, RB Quinazolines as biogenic amine transport modulators US Patent  US10087148 Publication Date 10/2/2018 
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:
BDBM287955
Synonyms:
N-(4-(4-((2-(4-methylpiperazin-1-yl)-2- phenylethyl)amino)quinazolin-2- yl)phenyl)methanesulfonamide | US10087148, Example 23
Type:
Small organic molecule
Emp. Form.:
C28H32N6O2S
Mol. Mass.:
516.658
SMILES:
CN1CCN(CC1)C(CNc1nc(nc2ccccc12)-c1ccc(NS(C)(=O)=O)cc1)c1ccccc1
Structure:
Search PDB for entries with ligand similarity: