Reaction Details Report a problem with these data
Target
Excitatory amino acid transporter 2
Ligand
BDBM50251893
Substrate
n/a
Meas. Tech.
ChEMBL_487937 (CHEMBL1016591)
Ki
410000±n/a nM
Citation
Sagot, E; Jensen, AA; Pickering, DS; Pu, X; Umberti, M; Stensbøl, TB; Nielsen, B; Assaf, Z; Aboab, B; Bolte, J; Gefflaut, T; Bunch, L Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human excitatory amino acid transporter subtype 2. J Med Chem 51:4085-92 (2008) [PubMed] Article
More Info.:
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:
Human
Description:
Excitatory Amino Acid EAAT2 0 0::P43004
Residue:
574
Sequence:
MASTEGANNMPKQVEVRMHDSHLGSEEPKHRHLGLRLCDKLGKNLLLTLTVFGVILGAVCGGLLRLASPIHPDVVMLIAFPGDILMRMLKMLILPLIISSLITGLSGLDAKASGRLGTRAMVYYMSTTIIAAVLGVILVLAIHPGNPKLKKQLGPGKKNDEVSSLDAFLDLIRNLFPENLVQACFQQIQTVTKKVLVAPPPDEEANATSAVVSLLNETVTEVPEETKMVIKKGLEFKDGMNVLGLIGFFIAFGIAMGKMGDQAKLMVDFFNILNEIVMKLVIMIMWYSPLGIACLICGKIIAIKDLEVVARQLGMYMVTVIIGLIIHGGIFLPLIYFVVTRKNPFSFFAGIFQAWITALGTASSAGTLPVTFRCLEENLGIDKRVTRFVLPVGATINMDGTALYEAVAAIFIAQMNGVVLDGGQIVTVSLTATLASVGAASIPSAGLVTMLLILTAVGLPTEDISLLVAVDWLLDRMRTSVNVVGDSFGAGIVYHLSKSELDTIDSQHRVHEDIEMTKTQSIYDDMKNHRESNSNQCVYAAHNSVIVDECKVTLAANGKSADCSVEEEPWKREK
Inhibitor
Name:
BDBM50251893
Synonyms:
(2S,4R)-2-amino-4-(3-(benzylamino)-3-oxopropyl)pentanedioic acid | (2S,4R)-4-(3-Benzylamino-3-oxopropyl)glutamic acid | CHEMBL518313
Type:
Small organic molecule
Emp. Form.:
C15H20N2O5
Mol. Mass.:
308.3297
SMILES:
N[C@@H](C[C@@H](CCC(=O)NCc1ccccc1)C(O)=O)C(O)=O |r|