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

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ChEMBL ligand: CHEMBL113180
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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: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7]
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: 444, 445, 446, 447] [UniProtKB: P19490, P19491, P19492, P19493]
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: 450, 451, 452, 453, 454] [UniProtKB: P22756, P42260, P42264, Q01812, Q63273]
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 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]