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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 |
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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] |
ChEMBL | Substrate uptake by the Excitatory Amino Acid Transporter 1 (EAAT1, SLC1A3) as assessed by the fluorescent FLIPR membrane potential dye in HEK-293 JumpIN-SLC1A3 cells (PubChem AID: 1745864) | F | 4.82 | pEC50 | 15000 | nM | EC50 | Membrane potential based transport assay for SLC1A3 using HEK293 JumpIn SLC1A3 OE cells |
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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]