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Target
Sodium- and chloride-dependent GABA transporter 1
Ligand
BDBM50368628
Substrate
n/a
Meas. Tech.
ChEMBL_976655 (CHEMBL2417030)
IC50
49±n/a nM
Citation
 Nakada, K; Yoshikawa, M; Ide, S; Suemasa, A; Kawamura, S; Kobayashi, T; Masuda, E; Ito, Y; Hayakawa, W; Katayama, T; Yamada, S; Arisawa, M; Minami, M; Shuto, S Cyclopropane-based conformational restriction of GABA by a stereochemical diversity-oriented strategy: identification of an efficient lead for potent inhibitors of GABA transports. Bioorg Med Chem 21:4938-50 (2013) [PubMed]  Article 
Target
Name:
Sodium- and chloride-dependent GABA transporter 1
Synonyms:
GABA transporter 1 | GABATR | GABT1 | GAT-1 | GAT1 | SC6A1_HUMAN | SLC6A1 | Sodium- and chloride-dependent GABA transporter 1 | Solute carrier family 6 member 1
Type:
PROTEIN
Mol. Mass.:
67079.40
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1454196
Residue:
599
Sequence:
MATNGSKVADGQISTEVSEAPVANDKPKTLVVKVQKKAADLPDRDTWKGRFDFLMSCVGYAIGLGNVWRFPYLCGKNGGGAFLIPYFLTLIFAGVPLFLLECSLGQYTSIGGLGVWKLAPMFKGVGLAAAVLSFWLNIYYIVIISWAIYYLYNSFTTTLPWKQCDNPWNTDRCFSNYSMVNTTNMTSAVVEFWERNMHQMTDGLDKPGQIRWPLAITLAIAWILVYFCIWKGVGWTGKVVYFSATYPYIMLIILFFRGVTLPGAKEGILFYITPNFRKLSDSEVWLDAATQIFFSYGLGLGSLIALGSYNSFHNNVYRDSIIVCCINSCTSMFAGFVIFSIVGFMAHVTKRSIADVAASGPGLAFLAYPEAVTQLPISPLWAILFFSMLLMLGIDSQFCTVEGFITALVDEYPRLLRNRRELFIAAVCIISYLIGLSNITQGGIYVFKLFDYYSASGMSLLFLVFFECVSISWFYGVNRFYDNIQEMVGSRPCIWWKLCWSFFTPIIVAGVFIFSAVQMTPLTMGNYVFPKWGQGVGWLMALSSMVLIPGYMAYMFLTLKGSLKQRIQVMVQPSEDIVRPENGPEQPQAGSSTSKEAYI
  
Inhibitor
Name:
BDBM50368628
Synonyms:
ABT-569 | Abbott-70569 | Abbott-70569.1 | Gabitril | NNC-05-0328 | NO-05-0328 | TIAGABINE HYDROCHLORIDE | Tiagabine
Type:
Small organic molecule
Emp. Form.:
C20H25NO2S2
Mol. Mass.:
375.548
SMILES:
[#6]-c1ccsc1\[#6](=[#6]\[#6]-[#6]-[#7]-1-[#6]-[#6]-[#6]-[#6@H](-[#6]-1)-[#6](-[#8])=O)-c1sccc1-[#6]
Structure:
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