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ChEMBL ligand: CHEMBL191838 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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GluN1/GluN2A/Glutamate NMDA receptor; Grin1/Grin2a in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096680] [GtoPdb: 455, 456] [UniProtKB: P35439, Q00959] | ||||||||
ChEMBL | Antagonist activity at rat recombinant GluN1/GluN2A receptor expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced response by two-electrode voltage-clamp electrophysiology assay | F | 4.66 | pKi | 22000 | nM | Ki | J Med Chem (2012) 55: 327-341 [PMID:22111545] |
ChEMBL | Inhibitory constant against (S)-glutamate and glycine evoked currents mediated by N-methyl-D-aspartate glutamate receptor NR1a/NR2A expressed in Xenopus oocytes | B | 4.85 | pKi | 14190 | nM | Ki | J Med Chem (2005) 48: 2627-2637 [PMID:15801853] |
GluN1/GluN2B/Glutamate NMDA receptor; Grin1/Grin2b in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096666] [GtoPdb: 455, 457] [UniProtKB: P35439, Q00960] | ||||||||
ChEMBL | Inhibitory constant against (S)-glutamate and glycine evoked currents mediated by N-methyl-D-aspartate glutamate receptor NR1a/NR2B expressed in Xenopus oocytes | B | 4.71 | pKi | 19290 | nM | Ki | J Med Chem (2005) 48: 2627-2637 [PMID:15801853] |
ChEMBL | Antagonist activity rat recombinant GluN1/GluN2B receptor expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced response by two-electrode voltage-clamp electrophysiology assay | F | 4.76 | pKi | 17200 | nM | Ki | J Med Chem (2012) 55: 327-341 [PMID:22111545] |
GluN1/GluN2C/Glutamate NMDA receptor; Grin1/Grin2c in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096911] [GtoPdb: 455, 458] [UniProtKB: P35439, Q00961] | ||||||||
ChEMBL | Antagonist activity rat recombinant GluN1/GluN2C receptor expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced response by two-electrode voltage-clamp electrophysiology assay | F | 5.28 | pKi | 5200 | nM | Ki | J Med Chem (2012) 55: 327-341 [PMID:22111545] |
ChEMBL | Inhibitory constant against (S)-glutamate and glycine evoked currents mediated by N-methyl-D-aspartate glutamate receptor NR1a/NR2C expressed in Xenopus oocytes | B | 5.37 | pKi | 4220 | nM | Ki | J Med Chem (2005) 48: 2627-2637 [PMID:15801853] |
GluN1/GluN2D/Ionotropic glutamate receptor NMDA 1/2D in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038506] [GtoPdb: 455, 459] [UniProtKB: P35439, Q62645] | ||||||||
ChEMBL | Antagonist activity rat recombinant GluN1/GluN2D receptor expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced response by two-electrode voltage-clamp electrophysiology assay | F | 5.62 | pKi | 2400 | nM | Ki | J Med Chem (2012) 55: 327-341 [PMID:22111545] |
ChEMBL data shown on this page come from version 32:
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]