[3H]L-aspartic acid [Ligand Id: 4534] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL274323 (Aspartate, Aspartic acid, Aspartic acid, l-, Aspartic acid,l, Deamidated asparagine, FEMA NO. 3656, L-aspartic acid, NSC-3973) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Dihydrodipicolinate synthase in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4083] [UniProtKB: P0A6L2] | ||||||||
| ChEMBL | Reversible inhibition of Escherichia coli dihydrodipicolinate synthase using ASA as substrate | B | 4.05 | pKi | 90000 | nM | Ki | Medchemcomm (2019) 10: 1581-1588 |
| Excitatory amino acid transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3085] [GtoPdb: 868] [UniProtKB: P43003] | ||||||||
| 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 | 5.03 | pIC50 | 9332.54 | 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 | 5.03 | pIC50 | 9300 | nM | IC50 | J Med Chem (2018) 61: 7741-7753 [PMID:30011368] |
| Excitatory amino acid transporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4973] [GtoPdb: 869] [UniProtKB: P43004] | ||||||||
| 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 | 4.48 | pIC50 | 33113.11 | 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 | 4.49 | pIC50 | 32000 | nM | IC50 | J Med Chem (2018) 61: 7741-7753 [PMID:30011368] |
| Excitatory amino acid transporter 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2721] [GtoPdb: 870] [UniProtKB: P43005] | ||||||||
| 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 | 4.7 | pIC50 | 20000 | 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 | 4.71 | pIC50 | 19498.45 | nM | IC50 | J Med Chem (2018) 61: 7741-7753 [PMID:30011368] |
| 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 | 4.96 | pIC50 | 11000 | 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 | 4.96 | pIC50 | 10964.78 | nM | IC50 | J Med Chem (2018) 61: 7741-7753 [PMID:30011368] |
| GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7] | ||||||||
| ChEMBL | Displacement of [3H]CPP from N-methyl-D-aspartate glutamate receptor in rat brain membrane | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (1992) 35: 1345-1370 [PMID:1533422] |
| ChEMBL | Compound was evaluated for the inhibition of [3H]-CGS-19,755 binding at N-methyl-D-aspartate glutamate receptor | B | 5.79 | pIC50 | 1638 | nM | IC50 | J Med Chem (1992) 35: 4608-4612 [PMID:1361579] |
| Glutamate transporter homolog in Pyrococcus horikoshii (strain ATCC 700860 / DSM 12428 / JCM 9974 /NBRC 100139 / OT-3) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4296295] [UniProtKB: O59010] | ||||||||
| ChEMBL | Binding affinity to Pyrococcus horikoshii sodium-coupled aspartate transporter L130W mutant fluorescence-based assay in presence of NaCl | B | 9 | pKd | 1 | nM | Kd | Nature (2007) 445: 387-393 [PMID:17230192] |
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]
