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Target
Sodium-dependent serotonin transporter
Ligand
BDBM50295058
Substrate
n/a
Meas. Tech.
ChEMBL_574190 (CHEMBL1060391)
Ki
32.8±n/a nM
Citation
 Zhou, D; Stack, GP; Lo, J; Failli, AA; Evrard, DA; Harrison, BL; Hatzenbuhler, NT; Tran, M; Croce, S; Yi, S; Golembieski, J; Hornby, GA; Lai, M; Lin, Q; Schechter, LE; Smith, DL; Shilling, AD; Huselton, C; Mitchell, P; Beyer, CE; Andree, TH Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists. J Med Chem 52:4955-9 (2009) [PubMed]  Article 
Target
Name:
Sodium-dependent serotonin transporter
Synonyms:
5-HT Transporter | 5-HTT | 5HT transporter | 5HTT | Anandamid membrane transporter, AMT | Anandamide membrane transporter, AMT | Monoamine transporters; Norepinephrine & serotonin | SC6A4_RAT | Slc6a4 | Sodium-dependent serotonin transporter | Sodium-dependent serotonin transporter (SERT) | imipramine receptor
Type:
Multi-pass membrane protein
Mol. Mass.:
70168.43
Organism:
Rattus norvegicus (rat)
Description:
P31652
Residue:
630
Sequence:
METTPLNSQKVLSECKDREDCQENGVLQKGVPTTADRAEPSQISNGYSAVPSTSAGDEASHSIPAATTTLVAEIRQGERETWGKKMDFLLSVIGYAVDLGNIWRFPYICYQNGGGAFLLPYTIMAIFGGIPLFYMELALGQYHRNGCISIWRKICPIFKGIGYAICIIAFYIASYYNTIIAWALYYLISSLTDRLPWTSCTNSWNTGNCTNYFAQDNITWTLHSTSPAEEFYLRHVLQIHQSKGLQDLGTISWQLTLCIVLIFTVIYFSIWKGVKTSGKVVWVTATFPYIVLSVLLVRGATLPGAWRGVVFYLKPNWQKLLETGVWVDAAAQIFFSLGPGFGVLLAFASYNKFNNNCYQDALVTSVVNCMTSFVSGFVIFTVLGYMAEMRNEDVSEVAKDAGPSLLFITYAEAIANMPASTFFAIIFFLMLITLGLDSTFAGLEGVITAVLDEFPHIWAKRREWFVLIVVITCVLGSLLTLTSGGAYVVTLLEEYATGPAVLTVALIEAVAVSWFYGITQFCSDVKEMLGFSPGWFWRICWVAISPLFLLFIICSFLMSPPQLRLFQYNYPHWSIVLGYCIGMSSVICIPTYIIYRLISTPGTLKERIIKSITPETPTEIPCGDIRMNAV
  
Inhibitor
Name:
BDBM50295058
Synonyms:
(2S)-8-Methyl-2-{[(2R)-2-methyl-4-quinolin-2-ylpiperazin-1-yl]methyl}-2,3-dihydro[1,4]dioxino-[2,3-f]quinoline | CHEMBL551107
Type:
Small organic molecule
Emp. Form.:
C27H28N4O2
Mol. Mass.:
440.5368
SMILES:
C[C@@H]1CN(CCN1C[C@H]1COc2ccc3nc(C)ccc3c2O1)c1ccc2ccccc2n1 |r|
Structure:
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