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Target
Sodium- and chloride-dependent GABA transporter 1
Ligand
BDBM50003618
Substrate
n/a
Meas. Tech.
ChEMBL_202583 (CHEMBL806333)
IC50
260±n/a nM
Citation
Dhar, TG; Borden, LA; Tyagarajan, S; Smith, KE; Branchek, TA; Weinshank, RL; Gluchowski, C Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3. J Med Chem 37:2334-42 (1994) [PubMed] Article
More Info.:
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:
BDBM50003618
Synonyms:
1-{2-[Bis-(4-trifluoromethyl-phenyl)-methoxy]-ethyl}-1,2,5,6-tetrahydro-pyridine-3-carboxylic acid; hydrochloride | CHEMBL542207 | CHEMBL77287
Type:
Small organic molecule
Emp. Form.:
C23H21F6NO3
Mol. Mass.:
473.4082
SMILES:
OC(=O)C1=CCCN(CCOC(c2ccc(cc2)C(F)(F)F)c2ccc(cc2)C(F)(F)F)C1 |t:3|