Ki Summary

Reaction Details

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Target

Excitatory amino acid transporter 1

Ligand

BDBM50328508

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_665667 (CHEMBL1261598)

IC50

3200±n/a nM

Citation

Erichsen, MN; Huynh, TH; Abrahamsen, B; Bastlund, JF; Bundgaard, C; Monrad, O; Bekker-Jensen, A; Nielsen, CW; Frydenvang, K; Jensen, AA; Bunch, L Structure-activity relationship study of first selective inhibitor of excitatory amino acid transporter subtype 1: 2-Amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101). J Med Chem53:7180-91 (2010) [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

BDBM50328508

n/a

Name

BDBM50328508

Synonyms:

2-Amino-4-(4-methoxyphenyl)-7-(naphthalene-2-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile | CHEMBL1259007

Type

Small organic molecule

Emp. Form.

C27H22N2O3

Mol. Mass.

422.4752

SMILES

COc1ccc(cc1)C1C(C#N)C(=N)OC2=C1C(=O)CC(C2)c1ccc2ccccc2c1 |c:16|

Structure