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 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]