Ki Summary

Reaction Details

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Target

Excitatory amino acid transporter 1

Ligand

BDBM50252051

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_487931 (CHEMBL1016585)

IC50

>1000000±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 Chem51:4085-92 (2008) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

Excitatory amino acid transporter 1

Name:

Excitatory amino acid transporter 1

Synonyms:

Type:

Enzyme Catalytic Domain

Mol. Mass.:

59577.19

Organism:

Homo sapiens (Human)

Description:

Excitatory Amino Acid EAAT1 0 HUMAN::P43003

Residue:

542

Sequence:

MTKSNGEEPKMGGRMERFQQGVRKRTLLAKKKVQNITKEDVKSYLFRNAFVLLTVTAVIV
GTILGFTLRPYRMSYREVKYFSFPGELLMRMLQMLVLPLIISSLVTGMAALDSKASGKMG
MRAVVYYMTTTIIAVVIGIIIVIIIHPGKGTKENMHREGKIVRVTAADAFLDLIRNMFPP
NLVEACFKQFKTNYEKRSFKVPIQANETLVGAVINNVSEAMETLTRITEELVPVPGSVNG
VNALGLVVFSMCFGFVIGNMKEQGQALREFFDSLNEAIMRLVAVIMWYAPVGILFLIAGK
IVEMEDMGVIGGQLAMYTVTVIVGLLIHAVIVLPLLYFLVTRKNPWVFIGGLLQALITAL
GTSSSSATLPITFKCLEENNGVDKRVTRFVLPVGATINMDGTALYEALAAIFIAQVNNFE
LNFGQIITISITATAASIGAAGIPQAGLVTMVIVLTSVGLPTDDITLIIAVDWFLDRLRT
TTNVLGDSLGAGIVEHLSRHELKNRDVEMGNSVIEENEMKKPYQLIAQDNETEKPIDSET
KM

BDBM50252051

n/a

Name

BDBM50252051

Synonyms:

(2S,4R)-2-amino-4-(3-(methylamino)-3-oxopropyl)pentanedioic acid | (2S,4R)-4-(3-Methylamino-3-oxopropyl)glutamic acid | CHEMBL500042

Type

Small organic molecule

Emp. Form.

C9H16N2O5

Mol. Mass.

232.2337

SMILES

CNC(=O)CC[C@H](C[C@H](N)C(O)=O)C(O)=O |r|

Structure