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Target
Sodium-dependent serotonin transporter
Ligand
BDBM376880
Substrate
n/a
Meas. Tech.
Competition Binding Assay
IC50
<100000±n/a nM
Citation
 Cremonesi, S; Micheli, F; Semeraro, T; Tarsi, L; Luker, T; Leslie, C N-(hetero)aryl-substituted heteroyclic derivatives useful for the treatment of diseases or conditions related to the central nervous system US Patent  US9920053 Publication Date 3/20/2018 
Target
Name:
Sodium-dependent serotonin transporter
Synonyms:
5-HT Transporter | 5HT transporter | 5HTT | HTT | SC6A4_HUMAN | SERT | SLC6A4 | Serotonin Transporter (SERT) | Serotonin transporter (5HTT) | Serotonin transporter protein (SERT) | Sodium-dependent serotonin transporter (SERT) | Solute carrier family 6 member 4
Type:
Multi-pass membrane protein
Mol. Mass.:
70322.51
Organism:
Homo sapiens (Human)
Description:
P31645
Residue:
630
Sequence:
METTPLNSQKQLSACEDGEDCQENGVLQKVVPTPGDKVESGQISNGYSAVPSPGAGDDTRHSIPATTTTLVAELHQGERETWGKKVDFLLSVIGYAVDLGNVWRFPYICYQNGGGAFLLPYTIMAIFGGIPLFYMELALGQYHRNGCISIWRKICPIFKGIGYAICIIAFYIASYYNTIMAWALYYLISSFTDQLPWTSCKNSWNTGNCTNYFSEDNITWTLHSTSPAEEFYTRHVLQIHRSKGLQDLGGISWQLALCIMLIFTVIYFSIWKGVKTSGKVVWVTATFPYIILSVLLVRGATLPGAWRGVLFYLKPNWQKLLETGVWIDAAAQIFFSLGPGFGVLLAFASYNKFNNNCYQDALVTSVVNCMTSFVSGFVIFTVLGYMAEMRNEDVSEVAKDAGPSLLFITYAEAIANMPASTFFAIIFFLMLITLGLDSTFAGLEGVITAVLDEFPHVWAKRRERFVLAVVITCFFGSLVTLTFGGAYVVKLLEEYATGPAVLTVALIEAVAVSWFYGITQFCRDVKEMLGFSPGWFWRICWVAISPLFLLFIICSFLMSPPQLRLFQYNYPYWSIILGYCIGTSSFICIPTYIAYRLIITPGTFKERIIKSITPETPTEIPCGDIRLNAV
  
Inhibitor
Name:
BDBM376880
Synonyms:
1-({1-[4-(3-fluorophenoxy)-6-(trifluoromethyl)pyrimidin-2-yl]-4-hydroxypiperidin-4-yl}methyl)pyrrolidin-2-one (E10) | US9920053, Example 10
Type:
Small organic molecule
Emp. Form.:
C21H22F4N4O3
Mol. Mass.:
454.418
SMILES:
OC1(CN2CCCC2=O)CCN(CC1)c1nc(Oc2cccc(F)c2)cc(n1)C(F)(F)F
Structure:
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