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

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ChEMBL ligand: CHEMBL395091 (Esketamina, 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 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]