esketamine [Ligand Id: 9152] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL395091 (Esketamine, Jnj-54135419, (-)-ketamine, Ketamine, (s)-, Ketamine, s-, Keta-s, Ketaved, L-ketamine, S-(-)-ketamine, S-ketamine)
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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 Displacement of [3H]MK801 from NMDA receptor in rat brain neuronal membrane B 6.02 pKi 960 nM Ki Bioorg Med Chem (2009) 17: 3456-3462 [PMID:19345586]
ChEMBL Displacement of [3H]-MK801 from NMDA receptor in rat brain membranes B 6.16 pKi 690 nM Ki J Med Chem (2020) 63: 13514-13525 [PMID:32915563]
ChEMBL Displacement of [3H]-MK801 from NMDA receptor in rat brain homogenate B 6.52 pKi 300 nM Ki J Med Chem (2020) 63: 13514-13525 [PMID:32915563]
ChEMBL Displacement of [3H]MK-801 from NMDA receptor in Wistar rat brain membranes by scintillation counting analysis B 6.19 pIC50 640 nM IC50 Bioorg Med Chem Lett (2015) 25: 4131-4135 [PMID:26296478]
GluN1/GluN2A/Glutamate NMDA receptor; GRIN1/GRIN2A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907604] [GtoPdb: 455, 456] [UniProtKB: Q05586, Q12879]
ChEMBL Antagonist activity against NR1-1a/NR2A NMDA receptor (unknown origin) expressed in mouse recombinant L(tk-) cells assessed as inhibition of glycine and glutamate induced excitotoxicity incubated for 12 hrs by LDH assay B 7.94 pIC50 11.4 nM IC50 J Med Chem (2015) 58: 8601-8615 [PMID:26430967]

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]