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Target
Sodium- and chloride-dependent GABA transporter 1
Ligand
BDBM50570589
Substrate
n/a
Meas. Tech.
ChEMBL_2112582 (CHEMBL4821432)
IC50
87100±n/a nM
Citation
 Pasieka, A; Panek, D; Jo?czyk, J; Gody?, J; Sza?aj, N; Latacz, G; Tabor, J; Mezeiova, E; Chantegreil, F; Dias, J; Knez, D; Lu, J; Pi, R; Korabecny, J; Brazzolotto, X; Gobec, S; Höfner, G; Wanner, K; Wi?ckowska, A; Malawska, B Discovery of multifunctional anti-Alzheimer's agents with a unique mechanism of action including inhibition of the enzyme butyrylcholinesterase and ?-aminobutyric acid transporters. Eur J Med Chem 218:0 (2021) [PubMed]  Article 
Target
Name:
Sodium- and chloride-dependent GABA transporter 1
Synonyms:
GABA transporter | Gabt1 | Gat-1 | Gat1 | SC6A1_RAT | Slc6a1 | Solute carrier family 6 member 1
Type:
PROTEIN
Mol. Mass.:
67006.26
Organism:
Rattus norvegicus
Description:
ChEMBL_1472611
Residue:
599
Sequence:
MATDNSKVADGQISTEVSEAPVASDKPKTLVVKVQKKAGDLPDRDTWKGRFDFLMSCVGYAIGLGNVWRFPYLCGKNGGGAFLIPYFLTLIFAGVPLFLLECSLGQYTSIGGLGVWKLAPMFKGVGLAAAVLSFWLNIYYIVIISWAIYYLYNSFTTTLPWKQCDNPWNTDRCFSNYSLVNTTNMTSAVVEFWERNMHQMTDGLDKPGQIRWPLAITLAIAWVLVYFCIWKGVGWTGKVVYFSATYPYIMLIILFFRGVTLPGAKEGILFYITPNFRKLSDSEVWLDAATQIFFSYGLGLGSLIALGSYNSFHNNVYRDSIIVCCINSCTSMFAGFVIFSIVGFMAHVTKRSIADVAASGPGLAFLAYPEAVTQLPISPLWAILFFSMLLMLGIDSQFCTVEGFITALVDEYPRLLRNRRELFIAAVCIVSYLIGLSNITQGGIYVFKLFDYYSASGMSLLFLVFFECVSISWFYGVNRFYDNIQEMVGSRPCIWWKLCWSFFTPIIVAGVFLFSAVQMTPLTMGSYVFPKWGQGVGWLMALSSMVLIPGYMAYMFLTLKGSLKQRLQVMIQPSEDIVRPENGPEQPQAGSSASKEAYI
  
Inhibitor
Name:
BDBM50570589
Synonyms:
CHEMBL4870994
Type:
Small organic molecule
Emp. Form.:
C32H34N2O3
Mol. Mass.:
494.624
SMILES:
COc1ccccc1CNC[C@H](O)[C@H](Cc1ccccc1)NC(=O)C(c1ccccc1)c1ccccc1 |r|
Structure:
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