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Target
Excitatory amino acid transporter 2
Ligand
BDBM86714
Substrate
n/a
Ki
157±n/a nM
Comments
PDSP_6775
Citation
 Dunlop, J; McIlvain, HB; Carrick, TA; Jow, B; Lu, Q; Kowal, D; Lin, S; Greenfield, A; Grosanu, C; Fan, K; Petroski, R; Williams, J; Foster, A; Butera, J Characterization of novel aryl-ether, biaryl, and fluorene aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT2. Mol Pharmacol 68:974-82 (2005) [PubMed]  Article 
Target
Name:
Excitatory amino acid transporter 2
Synonyms:
EAA2_HUMAN | EAAT2 | GLT1 | Glutamate/aspartate transporter II | SLC1A2 | Sodium-dependent glutamate/aspartate transporter 2 | Solute carrier family 1 member 2
Type:
Enzyme Catalytic Domain
Mol. Mass.:
62103.57
Organism:
Homo sapiens (Human)
Description:
Excitatory Amino Acid EAAT2 0 0::P43004
Residue:
574
Sequence:
MASTEGANNMPKQVEVRMHDSHLGSEEPKHRHLGLRLCDKLGKNLLLTLTVFGVILGAVCGGLLRLASPIHPDVVMLIAFPGDILMRMLKMLILPLIISSLITGLSGLDAKASGRLGTRAMVYYMSTTIIAAVLGVILVLAIHPGNPKLKKQLGPGKKNDEVSSLDAFLDLIRNLFPENLVQACFQQIQTVTKKVLVAPPPDEEANATSAVVSLLNETVTEVPEETKMVIKKGLEFKDGMNVLGLIGFFIAFGIAMGKMGDQAKLMVDFFNILNEIVMKLVIMIMWYSPLGIACLICGKIIAIKDLEVVARQLGMYMVTVIIGLIIHGGIFLPLIYFVVTRKNPFSFFAGIFQAWITALGTASSAGTLPVTFRCLEENLGIDKRVTRFVLPVGATINMDGTALYEAVAAIFIAQMNGVVLDGGQIVTVSLTATLASVGAASIPSAGLVTMLLILTAVGLPTEDISLLVAVDWLLDRMRTSVNVVGDSFGAGIVYHLSKSELDTIDSQHRVHEDIEMTKTQSIYDDMKNHRESNSNQCVYAAHNSVIVDECKVTLAANGKSADCSVEEEPWKREK
  
Inhibitor
Name:
BDBM86714
Synonyms:
WAY 212922 | WAY-212922
Type:
Small organic molecule
Emp. Form.:
C18H15F3N2O3
Mol. Mass.:
364.3185
SMILES:
N[C@@H](CC(=O)Nc1ccc-2c(Cc3cc(ccc-23)C(F)(F)F)c1)C(O)=O
Structure:
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