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Compile Data Set for Download or QSAR

Found 5 hits Enz. Inhib. hit(s) with Target = 'Excitatory amino acid transporter 1' and Monomerid = 50292997   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Excitatory amino acid transporter 1


(Homo sapiens (Human))
BDBM50292997
PNG
(2-Amino-4-(4-methoxyphenyl)-7-(naphthalene-1-yl)-5...)
Show SMILES COc1ccc(cc1)C1C(C#N)C(=N)OC2=C1C(=O)CC(C2)c1cccc2ccccc12
Show InChI InChI=1/C27H22N2O3/c1-31-19-11-9-17(10-12-19)25-22(15-28)27(29)32-24-14-18(13-23(30)26(24)25)21-8-4-6-16-5-2-3-7-20(16)21/h2-12,18,22,25,29H,13-14H2,1H3
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PC cid
PC sid
UniChem

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Article
PubMed
n/an/a 120n/an/an/an/an/an/a



University of Copenhagen

Curated by ChEMBL


Assay Description
Activity at human EAAT1 expressed in HEK293 cells assessed as inhibition of Glu-induced fluorescent response by FLIPR membrane potential blue assay


J Med Chem 52: 912-5 (2009)


Article DOI: 10.1021/jm8013458
BindingDB Entry DOI: 10.7270/Q2PV6KCP
More data for this
Ligand-Target Pair
Excitatory amino acid transporter 1


(Homo sapiens (Human))
BDBM50292997
PNG
(2-Amino-4-(4-methoxyphenyl)-7-(naphthalene-1-yl)-5...)
Show SMILES COc1ccc(cc1)C1C(C#N)C(=N)OC2=C1C(=O)CC(C2)c1cccc2ccccc12
Show InChI InChI=1/C27H22N2O3/c1-31-19-11-9-17(10-12-19)25-22(15-28)27(29)32-24-14-18(13-23(30)26(24)25)21-8-4-6-16-5-2-3-7-20(16)21/h2-12,18,22,25,29H,13-14H2,1H3
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PC cid
PC sid
UniChem

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Article
PubMed
n/an/a 660n/an/an/an/an/an/a



University of Copenhagen

Curated by ChEMBL


Assay Description
Displacement of [3H]D-Asp from human EAAT1 receptor expressed in HEK293 cells


J Med Chem 52: 912-5 (2009)


Article DOI: 10.1021/jm8013458
BindingDB Entry DOI: 10.7270/Q2PV6KCP
More data for this
Ligand-Target Pair
Excitatory amino acid transporter 1


(Homo sapiens (Human))
BDBM50292997
PNG
(2-Amino-4-(4-methoxyphenyl)-7-(naphthalene-1-yl)-5...)
Show SMILES COc1ccc(cc1)C1C(C#N)C(=N)OC2=C1C(=O)CC(C2)c1cccc2ccccc12
Show InChI InChI=1/C27H22N2O3/c1-31-19-11-9-17(10-12-19)25-22(15-28)27(29)32-24-14-18(13-23(30)26(24)25)21-8-4-6-16-5-2-3-7-20(16)21/h2-12,18,22,25,29H,13-14H2,1H3
Reactome pathway
KEGG

UniProtKB/SwissProt

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GoogleScholar
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/a 660n/an/an/an/an/an/a



University of Copenhagen

Curated by ChEMBL


Assay Description
Inhibition of human EAAT1 expressed in HEK293 cells assessed as inhibition of 3[H]-D-Aspartate uptake after 6 mins by scintillation counting method


J Med Chem 55: 5403-12 (2012)


Article DOI: 10.1021/jm300345z
BindingDB Entry DOI: 10.7270/Q2Q81F5W
More data for this
Ligand-Target Pair
Excitatory amino acid transporter 1


(Homo sapiens (Human))
BDBM50292997
PNG
(2-Amino-4-(4-methoxyphenyl)-7-(naphthalene-1-yl)-5...)
Show SMILES COc1ccc(cc1)C1C(C#N)C(=N)OC2=C1C(=O)CC(C2)c1cccc2ccccc12
Show InChI InChI=1/C27H22N2O3/c1-31-19-11-9-17(10-12-19)25-22(15-28)27(29)32-24-14-18(13-23(30)26(24)25)21-8-4-6-16-5-2-3-7-20(16)21/h2-12,18,22,25,29H,13-14H2,1H3
Reactome pathway
KEGG

UniProtKB/SwissProt

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CHEMBL
PC cid
PC sid
UniChem

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Article
PubMed
n/an/a 660n/an/an/an/an/an/a



University of Copenhagen

Curated by ChEMBL


Assay Description
Inhibition of human EAAT1 expressed in HEK293 cells by [3H]D-Asp uptake assay


J Med Chem 53: 7180-91 (2010)


Article DOI: 10.1021/jm1009154
BindingDB Entry DOI: 10.7270/Q2VM4CGX
More data for this
Ligand-Target Pair
Excitatory amino acid transporter 1


(Rattus norvegicus)
BDBM50292997
PNG
(2-Amino-4-(4-methoxyphenyl)-7-(naphthalene-1-yl)-5...)
Show SMILES COc1ccc(cc1)C1C(C#N)C(=N)OC2=C1C(=O)CC(C2)c1cccc2ccccc12
Show InChI InChI=1/C27H22N2O3/c1-31-19-11-9-17(10-12-19)25-22(15-28)27(29)32-24-14-18(13-23(30)26(24)25)21-8-4-6-16-5-2-3-7-20(16)21/h2-12,18,22,25,29H,13-14H2,1H3
Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/a 970n/an/an/an/an/an/a



University of Copenhagen

Curated by ChEMBL


Assay Description
Activity at rat EAAT1 expressed in TSA201 cells assessed as inhibition of Glu-induced fluorescent response by FLIPR membrane potential blue assay


J Med Chem 52: 912-5 (2009)


Article DOI: 10.1021/jm8013458
BindingDB Entry DOI: 10.7270/Q2PV6KCP
More data for this
Ligand-Target Pair