ATPA [Ligand Id: 4140] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL113180
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455456457458459461460] [UniProtKB: P35439Q00959Q00960Q00961Q62645Q8VHN2Q9R1M7]
ChEMBL Tested in vitro for the concentration required to inhibit [3H]CPP radioligand at EAA receptor sites in rat cortical membranes B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1994) 37: 3252-3262 [PMID:7523673]
ChEMBL Concentration required for 50% inhibition of [3H]-CPP binding to N-methyl-D-aspartate glutamate receptor in rat cortical slice preparation B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1992) 35: 3512-3519 [PMID:1383544]
ChEMBL Concentration required for 50% inhibition of [3H]-MK-801 binding to N-methyl-D-aspartate glutamate receptor in rat cortical slice preparation B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1992) 35: 3512-3519 [PMID:1383544]
ChEMBL Inhibition of [3H]-MK-801 binding to EAA receptor sites in rat cortical membranes B 4 pEC50 >100000 nM EC50 J. Med. Chem. (1994) 37: 3252-3262 [PMID:7523673]
GluA1/GluA2/GluA3/GluA4/Glutamate receptor ionotropic, AMPA in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093871] [GtoPdb: 444445446447] [UniProtKB: P19490P19491P19492P19493]
ChEMBL Concentration required for 50% inhibition of [3H]Glu binding to AMPA receptor in rat cortical slice preparation in the presence of 2.5 mM CaCl2 B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1992) 35: 3512-3519 [PMID:1383544]
ChEMBL Tested in vitro for the concentration required to inhibit [3H]AMPA radioligand at EAA receptor sites in rat cortical membranes B 4.96 pIC50 11000 nM IC50 J. Med. Chem. (1994) 37: 3252-3262 [PMID:7523673]
ChEMBL Concentration required for 50% inhibition of [3H]AMPA binding to AMPA receptor in rat cortical slice preparation B 5 pIC50 10000 nM IC50 J. Med. Chem. (1992) 35: 3512-3519 [PMID:1383544]
ChEMBL In vitro binding affinity for Ionotropic glutamate receptor AMPA site was determined using [3H]AMPA as radioligand in rat cortex B 5.68 pIC50 2100 nM IC50 J. Med. Chem. (1997) 40: 520-527 [PMID:9046343]
GluK1/GluK2/GluK3/GluK4/GluK5/Glutamate receptor ionotropic, kainate in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094119] [GtoPdb: 450451452453454] [UniProtKB: P22756P42260P42264Q01812Q63273]
ChEMBL Concentration required for 50% inhibition of [3H]-kainic acid binding to ionotropic glutamate receptor ionotropic kainate in rat cortical slice preparation B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1992) 35: 3512-3519 [PMID:1383544]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]