Found 379 hits of ic50 for UniProtKB: P43003 Target/Host
(Institution) | Ligand | Target/Host
Links | Ligand
Links | Trg + Lig
Links | Ki
nM | ΔG°
kcal/mole | IC50
nM | Kd
nM | EC50/IC50
nM | koff
s-1 | kon
M-1s-1 | pH | Temp
°C |
|---|
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50327884
((2S,3S)-2-amino-3-(3-(4-(trifluoromethyl)benzamido...)Show SMILES N[C@@H]([C@H](OCc1cccc(NC(=O)c2ccc(cc2)C(F)(F)F)c1)C(O)=O)C(O)=O |r| Show InChI InChI=1S/C19H17F3N2O6/c20-19(21,22)12-6-4-11(5-7-12)16(25)24-13-3-1-2-10(8-13)9-30-15(18(28)29)14(23)17(26)27/h1-8,14-15H,9,23H2,(H,24,25)(H,26,27)(H,28,29)/t14-,15-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet 
| Purchase
CHEMBL
MCE
KEGG
PC cid
PC sid
PDB
UniChem
Patents
| Article
PubMed
| n/a | n/a | 3.5 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Groningen
Curated by ChEMBL
| Assay Description
Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method |
J Med Chem 61: 7741-7753 (2018)
Article DOI: 10.1021/acs.jmedchem.8b00700
BindingDB Entry DOI: 10.7270/Q2G44ST4 |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50327884
((2S,3S)-2-amino-3-(3-(4-(trifluoromethyl)benzamido...)Show SMILES N[C@@H]([C@H](OCc1cccc(NC(=O)c2ccc(cc2)C(F)(F)F)c1)C(O)=O)C(O)=O |r| Show InChI InChI=1S/C19H17F3N2O6/c20-19(21,22)12-6-4-11(5-7-12)16(25)24-13-3-1-2-10(8-13)9-30-15(18(28)29)14(23)17(26)27/h1-8,14-15H,9,23H2,(H,24,25)(H,26,27)(H,28,29)/t14-,15-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| Purchase
CHEMBL
MCE
KEGG
PC cid
PC sid
PDB
UniChem
Patents
| Article
PubMed
| n/a | n/a | 3.60 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Groningen
Curated by ChEMBL
| Assay Description
Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method |
J Med Chem 61: 7741-7753 (2018)
Article DOI: 10.1021/acs.jmedchem.8b00700
BindingDB Entry DOI: 10.7270/Q2G44ST4 |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50366616
(CHEMBL4176427)Show SMILES N[C@@H]([C@H](OCc1cccc(NC(=O)CCc2ccc(cc2)C(F)(F)F)c1)C(O)=O)C(O)=O |r| Show InChI InChI=1S/C21H21F3N2O6/c22-21(23,24)14-7-4-12(5-8-14)6-9-16(27)26-15-3-1-2-13(10-15)11-32-18(20(30)31)17(25)19(28)29/h1-5,7-8,10,17-18H,6,9,11,25H2,(H,26,27)(H,28,29)(H,30,31)/t17-,18-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| KEGG
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 5.10 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Groningen
Curated by ChEMBL
| Assay Description
Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method |
J Med Chem 61: 7741-7753 (2018)
Article DOI: 10.1021/acs.jmedchem.8b00700
BindingDB Entry DOI: 10.7270/Q2G44ST4 |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50366616
(CHEMBL4176427)Show SMILES N[C@@H]([C@H](OCc1cccc(NC(=O)CCc2ccc(cc2)C(F)(F)F)c1)C(O)=O)C(O)=O |r| Show InChI InChI=1S/C21H21F3N2O6/c22-21(23,24)14-7-4-12(5-8-14)6-9-16(27)26-15-3-1-2-13(10-15)11-32-18(20(30)31)17(25)19(28)29/h1-5,7-8,10,17-18H,6,9,11,25H2,(H,26,27)(H,28,29)(H,30,31)/t17-,18-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| KEGG
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 5.10 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Groningen
Curated by ChEMBL
| Assay Description
Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method |
J Med Chem 61: 7741-7753 (2018)
Article DOI: 10.1021/acs.jmedchem.8b00700
BindingDB Entry DOI: 10.7270/Q2G44ST4 |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50366648
(CHEMBL4173045)Show SMILES N[C@@H]([C@H](OCc1cccc(NC(=O)c2cccc(c2)C(F)(F)F)c1)C(O)=O)C(O)=O |r| Show InChI InChI=1S/C19H17F3N2O6/c20-19(21,22)12-5-2-4-11(8-12)16(25)24-13-6-1-3-10(7-13)9-30-15(18(28)29)14(23)17(26)27/h1-8,14-15H,9,23H2,(H,24,25)(H,26,27)(H,28,29)/t14-,15-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| KEGG
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 6.10 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Groningen
Curated by ChEMBL
| Assay Description
Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method |
J Med Chem 61: 7741-7753 (2018)
Article DOI: 10.1021/acs.jmedchem.8b00700
BindingDB Entry DOI: 10.7270/Q2G44ST4 |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50366648
(CHEMBL4173045)Show SMILES N[C@@H]([C@H](OCc1cccc(NC(=O)c2cccc(c2)C(F)(F)F)c1)C(O)=O)C(O)=O |r| Show InChI InChI=1S/C19H17F3N2O6/c20-19(21,22)12-5-2-4-11(8-12)16(25)24-13-6-1-3-10(7-13)9-30-15(18(28)29)14(23)17(26)27/h1-8,14-15H,9,23H2,(H,24,25)(H,26,27)(H,28,29)/t14-,15-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| KEGG
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 6.20 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Groningen
Curated by ChEMBL
| Assay Description
Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method |
J Med Chem 61: 7741-7753 (2018)
Article DOI: 10.1021/acs.jmedchem.8b00700
BindingDB Entry DOI: 10.7270/Q2G44ST4 |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50366614
(CHEMBL4176482)Show SMILES N[C@@H]([C@H](OCc1ccccc1)C(=O)Nc1ccc(Oc2cc(F)c(F)cc2Br)cc1)C(O)=O |r| Show InChI InChI=1S/C23H19BrF2N2O5/c24-16-10-17(25)18(26)11-19(16)33-15-8-6-14(7-9-15)28-22(29)21(20(27)23(30)31)32-12-13-4-2-1-3-5-13/h1-11,20-21H,12,27H2,(H,28,29)(H,30,31)/t20-,21-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| KEGG
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 11 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Groningen
Curated by ChEMBL
| Assay Description
Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method |
J Med Chem 61: 7741-7753 (2018)
Article DOI: 10.1021/acs.jmedchem.8b00700
BindingDB Entry DOI: 10.7270/Q2G44ST4 |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50366614
(CHEMBL4176482)Show SMILES N[C@@H]([C@H](OCc1ccccc1)C(=O)Nc1ccc(Oc2cc(F)c(F)cc2Br)cc1)C(O)=O |r| Show InChI InChI=1S/C23H19BrF2N2O5/c24-16-10-17(25)18(26)11-19(16)33-15-8-6-14(7-9-15)28-22(29)21(20(27)23(30)31)32-12-13-4-2-1-3-5-13/h1-11,20-21H,12,27H2,(H,28,29)(H,30,31)/t20-,21-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| KEGG
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 11 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Groningen
Curated by ChEMBL
| Assay Description
Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method |
J Med Chem 61: 7741-7753 (2018)
Article DOI: 10.1021/acs.jmedchem.8b00700
BindingDB Entry DOI: 10.7270/Q2G44ST4 |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50366609
(CHEMBL4177507)Show SMILES N[C@@H]([C@H](OCc1ccccc1)C(=O)Nc1ccc-2c(Cc3ccccc-23)c1)C(O)=O |r| Show InChI InChI=1S/C24H22N2O4/c25-21(24(28)29)22(30-14-15-6-2-1-3-7-15)23(27)26-18-10-11-20-17(13-18)12-16-8-4-5-9-19(16)20/h1-11,13,21-22H,12,14,25H2,(H,26,27)(H,28,29)/t21-,22-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| KEGG
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 12 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Groningen
Curated by ChEMBL
| Assay Description
Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method |
J Med Chem 61: 7741-7753 (2018)
Article DOI: 10.1021/acs.jmedchem.8b00700
BindingDB Entry DOI: 10.7270/Q2G44ST4 |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50366609
(CHEMBL4177507)Show SMILES N[C@@H]([C@H](OCc1ccccc1)C(=O)Nc1ccc-2c(Cc3ccccc-23)c1)C(O)=O |r| Show InChI InChI=1S/C24H22N2O4/c25-21(24(28)29)22(30-14-15-6-2-1-3-7-15)23(27)26-18-10-11-20-17(13-18)12-16-8-4-5-9-19(16)20/h1-11,13,21-22H,12,14,25H2,(H,26,27)(H,28,29)/t21-,22-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| KEGG
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 12 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Groningen
Curated by ChEMBL
| Assay Description
Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method |
J Med Chem 61: 7741-7753 (2018)
Article DOI: 10.1021/acs.jmedchem.8b00700
BindingDB Entry DOI: 10.7270/Q2G44ST4 |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50366626
(CHEMBL4165811)Show SMILES N[C@@H]([C@H](OCc1cccc(NC(=O)Cc2ccc(cc2)C(F)(F)F)c1)C(O)=O)C(O)=O |r| Show InChI InChI=1S/C20H19F3N2O6/c21-20(22,23)13-6-4-11(5-7-13)9-15(26)25-14-3-1-2-12(8-14)10-31-17(19(29)30)16(24)18(27)28/h1-8,16-17H,9-10,24H2,(H,25,26)(H,27,28)(H,29,30)/t16-,17-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| KEGG
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 21 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Groningen
Curated by ChEMBL
| Assay Description
Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method |
J Med Chem 61: 7741-7753 (2018)
Article DOI: 10.1021/acs.jmedchem.8b00700
BindingDB Entry DOI: 10.7270/Q2G44ST4 |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50366626
(CHEMBL4165811)Show SMILES N[C@@H]([C@H](OCc1cccc(NC(=O)Cc2ccc(cc2)C(F)(F)F)c1)C(O)=O)C(O)=O |r| Show InChI InChI=1S/C20H19F3N2O6/c21-20(22,23)13-6-4-11(5-7-13)9-15(26)25-14-3-1-2-12(8-14)10-31-17(19(29)30)16(24)18(27)28/h1-8,16-17H,9-10,24H2,(H,25,26)(H,27,28)(H,29,30)/t16-,17-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| KEGG
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 21 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Groningen
Curated by ChEMBL
| Assay Description
Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method |
J Med Chem 61: 7741-7753 (2018)
Article DOI: 10.1021/acs.jmedchem.8b00700
BindingDB Entry DOI: 10.7270/Q2G44ST4 |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50327884
((2S,3S)-2-amino-3-(3-(4-(trifluoromethyl)benzamido...)Show SMILES N[C@@H]([C@H](OCc1cccc(NC(=O)c2ccc(cc2)C(F)(F)F)c1)C(O)=O)C(O)=O |r| Show InChI InChI=1S/C19H17F3N2O6/c20-19(21,22)12-6-4-11(5-7-12)16(25)24-13-3-1-2-10(8-13)9-30-15(18(28)29)14(23)17(26)27/h1-8,14-15H,9,23H2,(H,24,25)(H,26,27)(H,28,29)/t14-,15-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| Purchase
CHEMBL
MCE
KEGG
PC cid
PC sid
PDB
UniChem
Patents
| Article
PubMed
| n/a | n/a | 22 | n/a | n/a | n/a | n/a | n/a | n/a |
The Scripps Research Institute
Curated by ChEMBL
| Assay Description
Inhibition of EAAT1 (unknown origin) transiently expressed in COS1 cells by [14C]glutamate based uptake assay |
J Med Chem 63: 3834-3867 (2020)
Article DOI: 10.1021/acs.jmedchem.9b01237
BindingDB Entry DOI: 10.7270/Q26113PD |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50366656
(CHEMBL4162363)Show SMILES N[C@@H]([C@H](OCc1cccc(NC(=O)c2ccccc2C(F)(F)F)c1)C(O)=O)C(O)=O |r| Show InChI InChI=1S/C19H17F3N2O6/c20-19(21,22)13-7-2-1-6-12(13)16(25)24-11-5-3-4-10(8-11)9-30-15(18(28)29)14(23)17(26)27/h1-8,14-15H,9,23H2,(H,24,25)(H,26,27)(H,28,29)/t14-,15-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| KEGG
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 31 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Groningen
Curated by ChEMBL
| Assay Description
Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method |
J Med Chem 61: 7741-7753 (2018)
Article DOI: 10.1021/acs.jmedchem.8b00700
BindingDB Entry DOI: 10.7270/Q2G44ST4 |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50366656
(CHEMBL4162363)Show SMILES N[C@@H]([C@H](OCc1cccc(NC(=O)c2ccccc2C(F)(F)F)c1)C(O)=O)C(O)=O |r| Show InChI InChI=1S/C19H17F3N2O6/c20-19(21,22)13-7-2-1-6-12(13)16(25)24-11-5-3-4-10(8-11)9-30-15(18(28)29)14(23)17(26)27/h1-8,14-15H,9,23H2,(H,24,25)(H,26,27)(H,28,29)/t14-,15-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| KEGG
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 31 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Groningen
Curated by ChEMBL
| Assay Description
Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method |
J Med Chem 61: 7741-7753 (2018)
Article DOI: 10.1021/acs.jmedchem.8b00700
BindingDB Entry DOI: 10.7270/Q2G44ST4 |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50410456
(CHEMBL2113122)Show SMILES N[C@@H](CC(=O)Nc1ccc(cc1)-c1cccc(c1)C(F)(F)F)C(O)=O |r| Show InChI InChI=1S/C17H15F3N2O3/c18-17(19,20)12-3-1-2-11(8-12)10-4-6-13(7-5-10)22-15(23)9-14(21)16(24)25/h1-8,14H,9,21H2,(H,22,23)(H,24,25)/t14-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 100 | n/a | n/a | n/a | n/a | n/a | n/a |
Wyeth Research
Curated by ChEMBL
| Assay Description
Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 1 |
Bioorg Med Chem Lett 15: 4985-8 (2005)
Article DOI: 10.1016/j.bmcl.2005.08.003
BindingDB Entry DOI: 10.7270/Q25H7FSP |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50410463
(CHEMBL2113115)Show SMILES N[C@@H](CC(=O)Nc1ccc-2c(Cc3cc(F)ccc-23)c1)C(O)=O |r| Show InChI InChI=1S/C17H15FN2O3/c18-11-1-3-13-9(6-11)5-10-7-12(2-4-14(10)13)20-16(21)8-15(19)17(22)23/h1-4,6-7,15H,5,8,19H2,(H,20,21)(H,22,23)/t15-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| Purchase
CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 100 | n/a | n/a | n/a | n/a | n/a | n/a |
Wyeth Research
Curated by ChEMBL
| Assay Description
Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 1 |
Bioorg Med Chem Lett 15: 4985-8 (2005)
Article DOI: 10.1016/j.bmcl.2005.08.003
BindingDB Entry DOI: 10.7270/Q25H7FSP |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50292997
(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 |c:16| Show InChI InChI=1S/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 | PDB
Reactome pathway
KEGG
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PC sid
UniChem
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| Article
PubMed
| n/a | n/a | 120 | n/a | n/a | n/a | n/a | n/a | n/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)) | BDBM50410457
(CHEMBL2113112)Show SMILES Cc1cc(NC(=O)C[C@H](N)C(O)=O)ccc1-c1cccc(c1)C(F)(F)F |r| Show InChI InChI=1S/C18H17F3N2O3/c1-10-7-13(23-16(24)9-15(22)17(25)26)5-6-14(10)11-3-2-4-12(8-11)18(19,20)21/h2-8,15H,9,22H2,1H3,(H,23,24)(H,25,26)/t15-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 130 | n/a | n/a | n/a | n/a | n/a | n/a |
Wyeth Research
Curated by ChEMBL
| Assay Description
Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 1 |
Bioorg Med Chem Lett 15: 4985-8 (2005)
Article DOI: 10.1016/j.bmcl.2005.08.003
BindingDB Entry DOI: 10.7270/Q25H7FSP |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50410455
(CHEMBL2113116)Show SMILES N[C@@H](CC(=O)Nc1ccc-2c(Cc3cc(Cl)ccc-23)c1)C(O)=O |r| Show InChI InChI=1S/C17H15ClN2O3/c18-11-1-3-13-9(6-11)5-10-7-12(2-4-14(10)13)20-16(21)8-15(19)17(22)23/h1-4,6-7,15H,5,8,19H2,(H,20,21)(H,22,23)/t15-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 150 | n/a | n/a | n/a | n/a | n/a | n/a |
Wyeth Research
Curated by ChEMBL
| Assay Description
Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 1 |
Bioorg Med Chem Lett 15: 4985-8 (2005)
Article DOI: 10.1016/j.bmcl.2005.08.003
BindingDB Entry DOI: 10.7270/Q25H7FSP |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50410450
(CHEMBL2113118)Show SMILES N[C@@H](CC(=O)Nc1ccc-2c(Cc3c-2cc(Cl)cc3Cl)c1)C(O)=O |r| Show InChI InChI=1S/C17H14Cl2N2O3/c18-9-5-12-11-2-1-10(21-16(22)7-15(20)17(23)24)3-8(11)4-13(12)14(19)6-9/h1-3,5-6,15H,4,7,20H2,(H,21,22)(H,23,24)/t15-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 200 | n/a | n/a | n/a | n/a | n/a | n/a |
Wyeth Research
Curated by ChEMBL
| Assay Description
Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 1 |
Bioorg Med Chem Lett 15: 4985-8 (2005)
Article DOI: 10.1016/j.bmcl.2005.08.003
BindingDB Entry DOI: 10.7270/Q25H7FSP |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50410464
(CHEMBL2113111)Show SMILES CCc1cc(ccc1NC(=O)C[C@H](N)C(O)=O)-c1ccc(F)c(Cl)c1 |r| Show InChI InChI=1S/C18H18ClFN2O3/c1-2-10-7-11(12-3-5-14(20)13(19)8-12)4-6-16(10)22-17(23)9-15(21)18(24)25/h3-8,15H,2,9,21H2,1H3,(H,22,23)(H,24,25)/t15-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 200 | n/a | n/a | n/a | n/a | n/a | n/a |
Wyeth Research
Curated by ChEMBL
| Assay Description
Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 1 |
Bioorg Med Chem Lett 15: 4985-8 (2005)
Article DOI: 10.1016/j.bmcl.2005.08.003
BindingDB Entry DOI: 10.7270/Q25H7FSP |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50173936
(2-Amino-N-(3-methyl-biphenyl-4-yl)-succinamic acid...)Show InChI InChI=1S/C17H18N2O3/c1-11-9-13(12-5-3-2-4-6-12)7-8-15(11)19-16(20)10-14(18)17(21)22/h2-9,14H,10,18H2,1H3,(H,19,20)(H,21,22) | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
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| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 300 | n/a | n/a | n/a | n/a | n/a | n/a |
Wyeth Research
Curated by ChEMBL
| Assay Description
Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 1 |
Bioorg Med Chem Lett 15: 4985-8 (2005)
Article DOI: 10.1016/j.bmcl.2005.08.003
BindingDB Entry DOI: 10.7270/Q25H7FSP |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50410459
(CHEMBL2113117)Show SMILES N[C@@H](CC(=O)Nc1ccc-2c(Cc3cc(Br)ccc-23)c1)C(O)=O |r| Show InChI InChI=1S/C17H15BrN2O3/c18-11-1-3-13-9(6-11)5-10-7-12(2-4-14(10)13)20-16(21)8-15(19)17(22)23/h1-4,6-7,15H,5,8,19H2,(H,20,21)(H,22,23)/t15-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 300 | n/a | n/a | n/a | n/a | n/a | n/a |
Wyeth Research
Curated by ChEMBL
| Assay Description
Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 1 |
Bioorg Med Chem Lett 15: 4985-8 (2005)
Article DOI: 10.1016/j.bmcl.2005.08.003
BindingDB Entry DOI: 10.7270/Q25H7FSP |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50410451
(CHEMBL1628570)Show SMILES N[C@@H](CC(=O)Nc1ccc-2c(Cc3ccccc-23)c1)C(O)=O |r| Show InChI InChI=1S/C17H16N2O3/c18-15(17(21)22)9-16(20)19-12-5-6-14-11(8-12)7-10-3-1-2-4-13(10)14/h1-6,8,15H,7,9,18H2,(H,19,20)(H,21,22)/t15-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 300 | n/a | n/a | n/a | n/a | n/a | n/a |
Wyeth Research
Curated by ChEMBL
| Assay Description
Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 1 |
Bioorg Med Chem Lett 15: 4985-8 (2005)
Article DOI: 10.1016/j.bmcl.2005.08.003
BindingDB Entry DOI: 10.7270/Q25H7FSP |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50196924
(CHEMBL3960774)Show SMILES N[C@@H](C(NS(=O)(=O)c1ccc(Cl)cc1)C(O)=O)C(O)=O |r| Show InChI InChI=1S/C10H11ClN2O6S/c11-5-1-3-6(4-2-5)20(18,19)13-8(10(16)17)7(12)9(14)15/h1-4,7-8,13H,12H2,(H,14,15)(H,16,17)/t7-,8?/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
KEGG
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 316 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description
Inhibition of [3H]-D-Asp uptake at human EAAT1 expressed in HEK293 cells measured after 3 mins by TopCount method |
J Med Chem 59: 8771-8786 (2016)
Article DOI: 10.1021/acs.jmedchem.6b01066
BindingDB Entry DOI: 10.7270/Q2Z03B4C |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50196924
(CHEMBL3960774)Show SMILES N[C@@H](C(NS(=O)(=O)c1ccc(Cl)cc1)C(O)=O)C(O)=O |r| Show InChI InChI=1S/C10H11ClN2O6S/c11-5-1-3-6(4-2-5)20(18,19)13-8(10(16)17)7(12)9(14)15/h1-4,7-8,13H,12H2,(H,14,15)(H,16,17)/t7-,8?/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
KEGG
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 320 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description
Inhibition of [3H]-D-Asp uptake at human EAAT1 expressed in HEK293 cells measured after 3 mins by TopCount method |
J Med Chem 59: 8771-8786 (2016)
Article DOI: 10.1021/acs.jmedchem.6b01066
BindingDB Entry DOI: 10.7270/Q2Z03B4C |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50197048
(CHEMBL3975687)Show SMILES N[C@@H](C(NS(=O)(=O)c1ccc(Br)cc1)C(O)=O)C(O)=O |r| Show InChI InChI=1S/C10H11BrN2O6S/c11-5-1-3-6(4-2-5)20(18,19)13-8(10(16)17)7(12)9(14)15/h1-4,7-8,13H,12H2,(H,14,15)(H,16,17)/t7-,8?/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
KEGG
PC cid
PC sid
UniChem
| Article
PubMed
| n/a | n/a | 350 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description
Inhibition of [3H]-D-Asp uptake at human EAAT1 expressed in HEK293 cells measured after 3 mins by TopCount method |
J Med Chem 59: 8771-8786 (2016)
Article DOI: 10.1021/acs.jmedchem.6b01066
BindingDB Entry DOI: 10.7270/Q2Z03B4C |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50197048
(CHEMBL3975687)Show SMILES N[C@@H](C(NS(=O)(=O)c1ccc(Br)cc1)C(O)=O)C(O)=O |r| Show InChI InChI=1S/C10H11BrN2O6S/c11-5-1-3-6(4-2-5)20(18,19)13-8(10(16)17)7(12)9(14)15/h1-4,7-8,13H,12H2,(H,14,15)(H,16,17)/t7-,8?/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
KEGG
PC cid
PC sid
UniChem
| Article
PubMed
| n/a | n/a | 363 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description
Inhibition of [3H]-D-Asp uptake at human EAAT1 expressed in HEK293 cells measured after 3 mins by TopCount method |
J Med Chem 59: 8771-8786 (2016)
Article DOI: 10.1021/acs.jmedchem.6b01066
BindingDB Entry DOI: 10.7270/Q2Z03B4C |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50561803
(CHEMBL4790691)Show SMILES OC(=O)C(F)(F)F.Cc1ccc(cc1)S(=O)(=O)n1cc(-c2ccc(cc2)C(F)(F)F)c2ccc(CO[C@@H]([C@H](N)C(O)=O)C(O)=O)cc12 |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| Article
PubMed
| n/a | n/a | 370 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Inhibition of human EAAT1 transfected in HEK293 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 4 mins by TopCount scintillatio... |
Citation and Details
Article DOI: 10.1021/acsmedchemlett.0c00342
BindingDB Entry DOI: 10.7270/Q2WH2TQZ |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50561803
(CHEMBL4790691)Show SMILES OC(=O)C(F)(F)F.Cc1ccc(cc1)S(=O)(=O)n1cc(-c2ccc(cc2)C(F)(F)F)c2ccc(CO[C@@H]([C@H](N)C(O)=O)C(O)=O)cc12 |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| Article
PubMed
| n/a | n/a | 372 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Inhibition of human EAAT1 transfected in HEK293 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 4 mins by TopCount scintillatio... |
Citation and Details
Article DOI: 10.1021/acsmedchemlett.0c00342
BindingDB Entry DOI: 10.7270/Q2WH2TQZ |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50197057
(CHEMBL3974720)Show SMILES Cc1ccc(cc1)S(=O)(=O)NC([C@H](N)C(O)=O)C(O)=O |r| Show InChI InChI=1S/C11H14N2O6S/c1-6-2-4-7(5-3-6)20(18,19)13-9(11(16)17)8(12)10(14)15/h2-5,8-9,13H,12H2,1H3,(H,14,15)(H,16,17)/t8-,9?/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
KEGG
PC cid
PC sid
UniChem
| Article
PubMed
| n/a | n/a | 380 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description
Inhibition of [3H]-D-Asp uptake at human EAAT1 expressed in HEK293 cells measured after 3 mins by TopCount method |
J Med Chem 59: 8771-8786 (2016)
Article DOI: 10.1021/acs.jmedchem.6b01066
BindingDB Entry DOI: 10.7270/Q2Z03B4C |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50197057
(CHEMBL3974720)Show SMILES Cc1ccc(cc1)S(=O)(=O)NC([C@H](N)C(O)=O)C(O)=O |r| Show InChI InChI=1S/C11H14N2O6S/c1-6-2-4-7(5-3-6)20(18,19)13-9(11(16)17)8(12)10(14)15/h2-5,8-9,13H,12H2,1H3,(H,14,15)(H,16,17)/t8-,9?/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
KEGG
PC cid
PC sid
UniChem
| Article
PubMed
| n/a | n/a | 380 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description
Inhibition of [3H]-D-Asp uptake at human EAAT1 expressed in HEK293 cells measured after 3 mins by TopCount method |
J Med Chem 59: 8771-8786 (2016)
Article DOI: 10.1021/acs.jmedchem.6b01066
BindingDB Entry DOI: 10.7270/Q2Z03B4C |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50410465
(CHEMBL2113113)Show SMILES N[C@@H](CC(=O)Nc1ccc(-c2ccc(F)c(Cl)c2)c(c1)C(F)(F)F)C(O)=O |r| Show InChI InChI=1S/C17H13ClF4N2O3/c18-12-5-8(1-4-13(12)19)10-3-2-9(6-11(10)17(20,21)22)24-15(25)7-14(23)16(26)27/h1-6,14H,7,23H2,(H,24,25)(H,26,27)/t14-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 400 | n/a | n/a | n/a | n/a | n/a | n/a |
Wyeth Research
Curated by ChEMBL
| Assay Description
Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 1 |
Bioorg Med Chem Lett 15: 4985-8 (2005)
Article DOI: 10.1016/j.bmcl.2005.08.003
BindingDB Entry DOI: 10.7270/Q25H7FSP |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50328509
(2-Amino-4-methyl-7-(naphthalen-1-yl)-5-oxo-5,6,7,8...)Show SMILES CC1C(C#N)C(=N)OC2=C1C(=O)CC(C2)c1cccc2ccccc12 |c:8| Show InChI InChI=1S/C21H18N2O2/c1-12-17(11-22)21(23)25-19-10-14(9-18(24)20(12)19)16-8-4-6-13-5-2-3-7-15(13)16/h2-8,12,14,17,23H,9-10H2,1H3 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 420 | n/a | n/a | n/a | n/a | n/a | n/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)) | BDBM50328509
(2-Amino-4-methyl-7-(naphthalen-1-yl)-5-oxo-5,6,7,8...)Show SMILES CC1C(C#N)C(=N)OC2=C1C(=O)CC(C2)c1cccc2ccccc12 |c:8| Show InChI InChI=1S/C21H18N2O2/c1-12-17(11-22)21(23)25-19-10-14(9-18(24)20(12)19)16-8-4-6-13-5-2-3-7-15(13)16/h2-8,12,14,17,23H,9-10H2,1H3 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 430 | n/a | n/a | n/a | n/a | n/a | n/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
(Homo sapiens (Human)) | BDBM50366637
(CHEMBL4164207)Show InChI InChI=1S/C11H19NO5/c12-8(10(13)14)9(11(15)16)17-6-7-4-2-1-3-5-7/h7-9H,1-6,12H2,(H,13,14)(H,15,16)/t8-,9-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| KEGG
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 620 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Groningen
Curated by ChEMBL
| Assay Description
Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method |
J Med Chem 61: 7741-7753 (2018)
Article DOI: 10.1021/acs.jmedchem.8b00700
BindingDB Entry DOI: 10.7270/Q2G44ST4 |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50366637
(CHEMBL4164207)Show InChI InChI=1S/C11H19NO5/c12-8(10(13)14)9(11(15)16)17-6-7-4-2-1-3-5-7/h7-9H,1-6,12H2,(H,13,14)(H,15,16)/t8-,9-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| KEGG
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 631 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Groningen
Curated by ChEMBL
| Assay Description
Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method |
J Med Chem 61: 7741-7753 (2018)
Article DOI: 10.1021/acs.jmedchem.8b00700
BindingDB Entry DOI: 10.7270/Q2G44ST4 |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50292997
(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 |c:16| Show InChI InChI=1S/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 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 660 | n/a | n/a | n/a | n/a | n/a | n/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
(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 |c:16| Show InChI InChI=1S/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 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 660 | n/a | n/a | n/a | n/a | n/a | n/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
(Homo sapiens (Human)) | BDBM50292997
(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 |c:16| Show InChI InChI=1S/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 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 660 | n/a | n/a | n/a | n/a | n/a | n/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
(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 |c:16| Show InChI InChI=1S/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 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 660 | n/a | n/a | n/a | n/a | n/a | n/a |
The Scripps Research Institute
Curated by ChEMBL
| Assay Description
Inhibition of EAAT1 (unknown origin) stably expressed in HEK293 cells assessed as reduction in [14C]glutamate uptake incubated for 5 mins by microbet... |
J Med Chem 63: 3834-3867 (2020)
Article DOI: 10.1021/acs.jmedchem.9b01237
BindingDB Entry DOI: 10.7270/Q26113PD |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50410461
(CHEMBL2113126)Show SMILES Cc1cc(NC(=O)C[C@H](N)C(O)=O)ccc1-c1ccc(Cl)c(Cl)c1 |r| Show InChI InChI=1S/C17H16Cl2N2O3/c1-9-6-11(21-16(22)8-15(20)17(23)24)3-4-12(9)10-2-5-13(18)14(19)7-10/h2-7,15H,8,20H2,1H3,(H,21,22)(H,23,24)/t15-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 700 | n/a | n/a | n/a | n/a | n/a | n/a |
Wyeth Research
Curated by ChEMBL
| Assay Description
Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 1 |
Bioorg Med Chem Lett 15: 4985-8 (2005)
Article DOI: 10.1016/j.bmcl.2005.08.003
BindingDB Entry DOI: 10.7270/Q25H7FSP |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50173917
(2-Amino-N-(10-ethyl-10H-phenoxazin-2-yl)-succinami...)Show InChI InChI=1S/C18H19N3O4/c1-2-21-13-5-3-4-6-15(13)25-16-8-7-11(9-14(16)21)20-17(22)10-12(19)18(23)24/h3-9,12H,2,10,19H2,1H3,(H,20,22)(H,23,24) | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
| Article
PubMed
| n/a | n/a | 700 | n/a | n/a | n/a | n/a | n/a | n/a |
Wyeth Research
Curated by ChEMBL
| Assay Description
Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 1 |
Bioorg Med Chem Lett 15: 4985-8 (2005)
Article DOI: 10.1016/j.bmcl.2005.08.003
BindingDB Entry DOI: 10.7270/Q25H7FSP |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50561801
(CHEMBL4759043)Show SMILES OC(=O)C(F)(F)F.Cc1ccc(cc1)S(=O)(=O)n1cc(-c2ccsc2)c2ccc(CO[C@@H]([C@H](N)C(O)=O)C(O)=O)cc12 |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| Article
PubMed
| n/a | n/a | 708 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Inhibition of human EAAT1 transfected in HEK293 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 4 mins by TopCount scintillatio... |
Citation and Details
Article DOI: 10.1021/acsmedchemlett.0c00342
BindingDB Entry DOI: 10.7270/Q2WH2TQZ |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50561801
(CHEMBL4759043)Show SMILES OC(=O)C(F)(F)F.Cc1ccc(cc1)S(=O)(=O)n1cc(-c2ccsc2)c2ccc(CO[C@@H]([C@H](N)C(O)=O)C(O)=O)cc12 |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| Article
PubMed
| n/a | n/a | 710 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Inhibition of human EAAT1 transfected in HEK293 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 4 mins by TopCount scintillatio... |
Citation and Details
Article DOI: 10.1021/acsmedchemlett.0c00342
BindingDB Entry DOI: 10.7270/Q2WH2TQZ |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50197054
(CHEMBL3937517)Show SMILES N[C@@H]([C@H](NS(=O)(=O)c1ccccc1)C(O)=O)C(O)=O |r| Show InChI InChI=1S/C10H12N2O6S/c11-7(9(13)14)8(10(15)16)12-19(17,18)6-4-2-1-3-5-6/h1-5,7-8,12H,11H2,(H,13,14)(H,15,16)/t7-,8-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
KEGG
PC cid
PC sid
UniChem
| Article
PubMed
| n/a | n/a | 794 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description
Inhibition of [3H]-D-Asp uptake at human EAAT1 expressed in HEK293 cells measured after 3 mins by TopCount method |
J Med Chem 59: 8771-8786 (2016)
Article DOI: 10.1021/acs.jmedchem.6b01066
BindingDB Entry DOI: 10.7270/Q2Z03B4C |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50197026
(CHEMBL3909952)Show SMILES N[C@@H](C(NS(=O)(=O)c1ccc(F)c(F)c1)C(O)=O)C(O)=O |r| Show InChI InChI=1S/C10H10F2N2O6S/c11-5-2-1-4(3-6(5)12)21(19,20)14-8(10(17)18)7(13)9(15)16/h1-3,7-8,14H,13H2,(H,15,16)(H,17,18)/t7-,8?/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
KEGG
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 794 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description
Inhibition of [3H]-D-Asp uptake at human EAAT1 expressed in HEK293 cells measured after 3 mins by TopCount method |
J Med Chem 59: 8771-8786 (2016)
Article DOI: 10.1021/acs.jmedchem.6b01066
BindingDB Entry DOI: 10.7270/Q2Z03B4C |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50197026
(CHEMBL3909952)Show SMILES N[C@@H](C(NS(=O)(=O)c1ccc(F)c(F)c1)C(O)=O)C(O)=O |r| Show InChI InChI=1S/C10H10F2N2O6S/c11-5-2-1-4(3-6(5)12)21(19,20)14-8(10(17)18)7(13)9(15)16/h1-3,7-8,14H,13H2,(H,15,16)(H,17,18)/t7-,8?/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
KEGG
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 800 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description
Inhibition of [3H]-D-Asp uptake at human EAAT1 expressed in HEK293 cells measured after 3 mins by TopCount method |
J Med Chem 59: 8771-8786 (2016)
Article DOI: 10.1021/acs.jmedchem.6b01066
BindingDB Entry DOI: 10.7270/Q2Z03B4C |
More data for this
Ligand-Target Pair | |
Excitatory amino acid transporter 1
(Homo sapiens (Human)) | BDBM50197054
(CHEMBL3937517)Show SMILES N[C@@H]([C@H](NS(=O)(=O)c1ccccc1)C(O)=O)C(O)=O |r| Show InChI InChI=1S/C10H12N2O6S/c11-7(9(13)14)8(10(15)16)12-19(17,18)6-4-2-1-3-5-6/h1-5,7-8,12H,11H2,(H,13,14)(H,15,16)/t7-,8-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
KEGG
PC cid
PC sid
UniChem
| Article
PubMed
| n/a | n/a | 800 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description
Inhibition of [3H]-D-Asp uptake at human EAAT1 expressed in HEK293 cells measured after 3 mins by TopCount method |
J Med Chem 59: 8771-8786 (2016)
Article DOI: 10.1021/acs.jmedchem.6b01066
BindingDB Entry DOI: 10.7270/Q2Z03B4C |
More data for this
Ligand-Target Pair | |
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