CGP37849 [Ligand Id: 4154] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL29811 (CGP-37849)
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  • GluN2A/Glutamate [NMDA] receptor subunit epsilon 1 in Rat [ChEMBL: CHEMBL310] [GtoPdb: 456] [UniProtKB: Q00959]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GluN2D/GluN3B/GluN1/GluN2A/GluN2B/GluN2C/GluN3A/Glutamate [NMDA] receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094124] [GtoPdb: 459461455456457458460] [UniProtKB: O15399O60391Q05586Q12879Q13224Q14957Q8TCU5]
ChEMBL Tested for the inhibitory activity by the inhibition of excitatory L-[3H]Glutamate binding to NMDA recognition sites B 7.59 pIC50 25.7 nM IC50 Bioorg Med Chem Lett (1993) 3: 27-32
ChEMBL Tested for the inhibitory activity by the inhibition of excitatory [3H]CGS-19,755 binding to NMDA recognition sites B 7.74 pIC50 18 nM IC50 Bioorg Med Chem Lett (1993) 3: 27-32
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455456457458459461460] [UniProtKB: P35439Q00959Q00960Q00961Q62645Q8VHN2Q9R1M7]
ChEMBL Compound was evaluated for its ability to displace [3H]CPP or [3H]-CGS- 19755 ligand from N-methyl-D-aspartate (NMDA) receptor B 6 pKi <1000 nM Ki J Med Chem (1992) 35: 1509-1514 [PMID:1533680]
ChEMBL Compound was evaluated for its ability to displace [3H]-CPP ligand from N-methyl-D-aspartate (NMDA) receptor B 7.46 pKi 35 nM Ki J Med Chem (1992) 35: 1509-1514 [PMID:1533680]
ChEMBL Ability to displace [3H]CPP from NMDA receptor in rat brain membrane B 7.46 pIC50 35 nM IC50 J Med Chem (1992) 35: 1345-1370 [PMID:1533422]
GluN2A/Glutamate [NMDA] receptor subunit epsilon 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL310] [GtoPdb: 456] [UniProtKB: Q00959]
ChEMBL Inhibition of [3H]Glu binding to rat N-methyl-D-aspartic acid receptor 2A B 6.66 pIC50 220 nM IC50 J Med Chem (2005) 48: 5489-5494 [PMID:16107147]
ChEMBL Inhibition of [3H]CPP binding to rat N-methyl-D-aspartic acid receptor 2A B 7.46 pIC50 35 nM IC50 J Med Chem (2005) 48: 5489-5494 [PMID:16107147]

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]