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Target
Excitatory amino acid transporter 2
Ligand
BDBM50401541
Substrate
n/a
Meas. Tech.
ChEMBL_882148 (CHEMBL2214980)
IC50
>300000±n/a nM
Citation
 Huynh, TH; Abrahamsen, B; Madsen, KK; Gonzalez-Franquesa, A; Jensen, AA; Bunch, L Design, synthesis and pharmacological characterization of coumarin-based fluorescent analogs of excitatory amino acid transporter subtype 1 selective inhibitors, UCPH-101 and UCPH-102. Bioorg Med Chem 20:6831-9 (2012) [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:
BDBM50401541
Synonyms:
CHEMBL2207074
Type:
Small organic molecule
Emp. Form.:
C21H18N2O5
Mol. Mass.:
378.378
SMILES:
COc1ccc2c(cc(=O)oc2c1)C1CC(=O)C2=C(C1)OC(=N)C(C#N)C2C |c:19|
Structure:
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