DL-TBOA [Ligand Id: 4631] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL79140 (L-Threo-Benzyloxy Aspartate) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Excitatory amino acid transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3085] [GtoPdb: 868] [UniProtKB: P43003] | ||||||||
| ChEMBL | Concentration required for blocking [14C]glutamate uptake in COS-1 cells expressing human Excitatory amino acid transporter 1 | B | 4.64 | pIC50 | 23000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2407-2410 [PMID:11078189] |
| ChEMBL | Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method | B | 5.68 | pIC50 | 2100 | nM | IC50 | J Med Chem (2018) 61: 7741-7753 [PMID:30011368] |
| ChEMBL | Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method | B | 5.68 | pIC50 | 2089.3 | nM | IC50 | J Med Chem (2018) 61: 7741-7753 [PMID:30011368] |
| ChEMBL | Inhibition of [3H]-D-Asp uptake at human EAAT1 expressed in HEK293 cells measured after 3 mins by TopCount method | B | 5.79 | pIC50 | 1621.81 | nM | IC50 | J Med Chem (2016) 59: 8771-8786 [PMID:27636002] |
| ChEMBL | Inhibition of [3H]-D-Asp uptake at human EAAT1 expressed in HEK293 cells measured after 3 mins by TopCount method | B | 5.8 | pIC50 | 1600 | nM | IC50 | J Med Chem (2016) 59: 8771-8786 [PMID:27636002] |
| Excitatory amino acid transporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4973] [GtoPdb: 869] [UniProtKB: P43004] | ||||||||
| ChEMBL | Concentration required for blocking [14C]glutamate uptake in COS-1 cells expressing human Excitatory amino acid transporter 2 | B | 4.19 | pIC50 | 64000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2407-2410 [PMID:11078189] |
| ChEMBL | Concentration required for blocking [14C]glutamate uptake in COS-1 cells expressing human Excitatory amino acid transporter 2 | B | 5.42 | pIC50 | 3800 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2407-2410 [PMID:11078189] |
| ChEMBL | Inhibition of human GLT1 expressed in Xenopus laevis Oocytes assessed as reduction of [3H]-glutamate uptake after 10 mins by scintillation counting | B | 5.42 | pIC50 | 3800 | nM | IC50 | J Med Chem (2010) 53: 7236-7250 [PMID:20812729] |
| ChEMBL | Inhibition of human EAAT2 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method | B | 5.72 | pIC50 | 1905.46 | nM | IC50 | J Med Chem (2018) 61: 7741-7753 [PMID:30011368] |
| ChEMBL | Inhibition of human EAAT2 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method | B | 5.72 | pIC50 | 1900 | nM | IC50 | J Med Chem (2018) 61: 7741-7753 [PMID:30011368] |
| ChEMBL | Inhibition of [3H]-D-Asp uptake at human EAAT2 expressed in HEK293 cells measured after 3 mins by TopCount method | B | 6.02 | pIC50 | 960 | nM | IC50 | J Med Chem (2016) 59: 8771-8786 [PMID:27636002] |
| ChEMBL | Inhibition of [3H]-D-Asp uptake at human EAAT2 expressed in HEK293 cells measured after 3 mins by TopCount method | B | 6.02 | pIC50 | 954.99 | nM | IC50 | J Med Chem (2016) 59: 8771-8786 [PMID:27636002] |
| Excitatory amino acid transporter 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2721] [GtoPdb: 870] [UniProtKB: P43005] | ||||||||
| ChEMBL | Concentration required for blocking [14C]glutamate uptake in COS-1 cells expressing human Excitatory amino acid transporter 3 | B | 4.68 | pIC50 | 21000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2407-2410 [PMID:11078189] |
| GtoPdb | - | - | 5.1 | pIC50 | 8000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2407-10 [PMID:11078189] |
| ChEMBL | Concentration required for blocking [14C]glutamate uptake in COS-1 cells expressing human Excitatory amino acid transporter 3 | B | 5.15 | pIC50 | 7000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2407-2410 [PMID:11078189] |
| ChEMBL | Inhibition of [14C]glutamate uptake at human EAAT3 expressed in african green monkey COS1 cells | B | 5.15 | pIC50 | 7000 | nM | IC50 | Bioorg Med Chem (2008) 16: 7740-7748 [PMID:18650095] |
| ChEMBL | Inhibition of human EAAC1 expressed in Xenopus laevis Oocytes assessed as reduction of [3H]-glutamate uptake after 10 mins by scintillation counting | B | 5.15 | pIC50 | 7000 | nM | IC50 | J Med Chem (2010) 53: 7236-7250 [PMID:20812729] |
| ChEMBL | Inhibition of human EAAT3 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method | B | 5.42 | pIC50 | 3801.89 | nM | IC50 | J Med Chem (2018) 61: 7741-7753 [PMID:30011368] |
| ChEMBL | Inhibition of human EAAT3 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method | B | 5.42 | pIC50 | 3800 | nM | IC50 | J Med Chem (2018) 61: 7741-7753 [PMID:30011368] |
| ChEMBL | Inhibition of [3H]-D-Asp uptake at human EAAT3 expressed in HEK293 cells measured after 3 mins by TopCount method | B | 5.43 | pIC50 | 3715.35 | nM | IC50 | J Med Chem (2016) 59: 8771-8786 [PMID:27636002] |
| ChEMBL | Inhibition of [3H]-D-Asp uptake at human EAAT3 expressed in HEK293 cells measured after 3 mins by TopCount method | B | 5.43 | pIC50 | 3700 | nM | IC50 | J Med Chem (2016) 59: 8771-8786 [PMID:27636002] |
| Excitatory amino acid transporter 4 in Human [GtoPdb: 871] [UniProtKB: P48664] | ||||||||
| GtoPdb | - | - | 5.4 | pKi | 4400 | nM | Ki | J Neurochem (2001) 79: 297-302 [PMID:11677257] |
| Excitatory amino acid transporter 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3700] [GtoPdb: 871] [UniProtKB: O35921] | ||||||||
| ChEMBL | Inhibition of rat EAAT4 expressed in tsA201 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method | B | 5.64 | pIC50 | 2300 | nM | IC50 | J Med Chem (2018) 61: 7741-7753 [PMID:30011368] |
| ChEMBL | Inhibition of rat EAAT4 expressed in tsA201 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method | B | 5.64 | pIC50 | 2290.87 | nM | IC50 | J Med Chem (2018) 61: 7741-7753 [PMID:30011368] |
| Excitatory amino acid transporter 5 in Human [GtoPdb: 872] [UniProtKB: O00341] | ||||||||
| GtoPdb | - | - | 5.5 | pKi | 3200 | nM | Ki | J Neurochem (2001) 79: 297-302 [PMID:11677257] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
