ketamine [Ligand Id: 4233] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL742 (PMI-150, Ketamine, NSC-70151, Ketalar)
  • Acetylcholine receptor protein alpha chain in Torpedo californica [ChEMBL: CHEMBL3097] [UniProtKB: P02710]
  • This target only has 0 pki data point
  • 0
1 CHEMBL742_lig_chart_1 Acetylcholine receptor protein alpha chain Torpedo californica
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  • Acetylcholinesterase in Electrophorus electricus [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
  • This target only has 0 pki data point
  • 0
2 CHEMBL742_lig_chart_2 Acetylcholinesterase Electrophorus electricus
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  • Cholinesterase in Equus caballus [ChEMBL: CHEMBL5763] [UniProtKB: P81908]
  • This target only has 0 pki data point
  • 0
3 CHEMBL742_lig_chart_3 Cholinesterase Equus caballus
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4 CHEMBL742_lig_chart_4 Glutamate [NMDA] receptor Human
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5 CHEMBL742_lig_chart_5 GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A HumanRat
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  • GluN1/GluN2A/Glutamate NMDA receptor; GRIN1/GRIN2A in Human [ChEMBL: CHEMBL1907604] [GtoPdb: 455456] [UniProtKB: Q05586Q12879]
  • This target only has 0 pki data point
  • 0
6 CHEMBL742_lig_chart_6 Glutamate NMDA receptor; GRIN1/GRIN2A Human
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  • GluN1/GluN2B/Glutamate NMDA receptor; GRIN1/GRIN2B in Human [ChEMBL: CHEMBL1907603] [GtoPdb: 455457] [UniProtKB: Q05586Q13224]
  • This target only has 0 pki data point
  • 0
7 CHEMBL742_lig_chart_7 Glutamate NMDA receptor; GRIN1/GRIN2B Human
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
  • This target only has 0 pki data point
  • 0
8 CHEMBL742_lig_chart_8 Voltage-gated L-type calcium channel alpha-1C subunit Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acetylcholine receptor protein alpha chain in Torpedo californica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3097] [UniProtKB: P02710]
ChEMBL Displacement of [3H]PCP from nAChR in Torpedo nobiliana electric organs membranes by scintillation counting method B 4.95 pIC50 11100 nM IC50 J Pesticide Sci (1995) 20: 49-56
ChEMBL Displacement of [3H]PCP from nAChR in Torpedo nobiliana electric organs membranes in presence of 100 uM carbachol by scintillation counting method B 5.31 pIC50 4950 nM IC50 J Pesticide Sci (1995) 20: 49-56
Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
ChEMBL Inhibition of electric eel AChE by modified Ellman's method B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2010) 53: 3611-3617 [PMID:20361801]
Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908]
ChEMBL Inhibition of equine serum BChE by modified Ellman's method B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2010) 53: 3611-3617 [PMID:20361801]
GluN2D/GluN3B/GluN1/GluN2A/GluN2B/GluN2C/GluN3A/Glutamate [NMDA] receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094124] [GtoPdb: 459461455456457458460] [UniProtKB: O15399O60391Q05586Q12879Q13224Q14957Q8TCU5]
ChEMBL Binding affinity to NMDA receptor (unknown origin) B 5.72 pKi 1900 nM Ki Bioorg Med Chem (2019) 27: 1226-1231 [PMID:30792105]
ChEMBL The compound was tested for its ability to block PCP N-methyl-D-aspartate glutamate receptor at the PCP (phencyclidine) binding site in postmortem human frontal cortex. B 6.38 pKi 420 nM Ki J. Med. Chem. (1998) 41: 393-400 [PMID:9464369]
GtoPdb Measured vs. exogenously expressed zeta1/epsilon3 (GRIN1/GRIN2C) subunits, at pH 6.9 - 6.18 pIC50 660 nM IC50 J Physiol (Lond.) (2007) 581: 107-28 [PMID:17303642]
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A in Human [GtoPdb: 455456457458459461460] [UniProtKB: Q05586Q12879Q13224Q14957O15399O60391Q8TCU5]
GtoPdb Measured vs. exogenously expressed zeta1/epsilon3 (GRIN1/GRIN2C) subunits, at pH 6.9 - 6.18 pIC50 660 nM IC50 J Physiol (Lond.) (2007) 581: 107-28 [PMID:17303642]
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455456457458459461460] [UniProtKB: P35439Q00959Q00960Q00961Q62645Q8VHN2Q9R1M7]
ChEMBL Ability to inhibit glutamate induced accumulation of [45 [Ca2+]] in cultured rat cortical neurons F 5.05 pIC50 8860 nM IC50 J. Med. Chem. (1993) 36: 1977-1995 [PMID:8336337]
ChEMBL Binding affinity towards PCP site of the NMDA receptor was measured by displacement of [3H]TPC in whole rat brain homogenate B 6.07 pIC50 860 nM IC50 J. Med. Chem. (1993) 36: 1977-1995 [PMID:8336337]
ChEMBL Displacement of [3H] MK-801 from NMDA glutamate ion channel in Wistar rat brain membranes (minus cerebellum) after 3 hrs by scintillation counting analysis B 6.15 pIC50 700 nM IC50 Bioorg Med Chem (2019) 27: 1226-1231 [PMID:30792105]
ChEMBL Inhibition of [3H]-MK-801 binding to NMDA receptor from rat cerebral cortical synaptic membrane B 6.21 pIC50 610 nM IC50 J. Med. Chem. (1996) 39: 4844-4852 [PMID:8941398]
ChEMBL Inhibition of [3H]MK-801 binding to N-methyl-D-aspartate glutamate receptor of rat cerebral cortical synaptic membrane B 6.21 pIC50 610 nM IC50 J. Med. Chem. (1998) 41: 3507-3514 [PMID:9719604]
GluN1/GluN2A/Glutamate NMDA receptor; GRIN1/GRIN2A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907604] [GtoPdb: 455456] [UniProtKB: Q05586Q12879]
ChEMBL Inhibition of dexamethasone-induced human NR1-1a/NR2A receptor-mediated excitotoxicity in (S)-glutamate/glycine-stimulated mouse L12-G10 cells assessed as LDH release after 30 mins B 5.21 pIC50 6100 nM IC50 J. Med. Chem. (2010) 53: 3611-3617 [PMID:20361801]
ChEMBL Antagonist activity at NR1/NR2A receptor (unknown origin) expressed in Xenopus laevis oocytes assessed as inhibition of glutamate/glycine-induced current at pH 7.6 at -40mV holding potential by two-electrode voltage-clamp electrophysiology B 5.48 pIC50 3310 nM IC50 Bioorg. Med. Chem. (2014) 22: 1983-1992 [PMID:24630693]
ChEMBL Inhibition of human recombinant NR1/NR2A receptor expressed in U2OS assessed as change in intracellular calcium level by FLIPR assay B 5.9 pIC50 1258.93 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 2059-2063 [PMID:21334205]
GluN1/GluN2B/Glutamate NMDA receptor; GRIN1/GRIN2B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907603] [GtoPdb: 455457] [UniProtKB: Q05586Q13224]
ChEMBL Inhibition of human recombinant NR1/NR2B receptor expressed in U2OS assessed as change in intracellular calcium level by FLIPR assay B 5.3 pIC50 5011.87 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 2059-2063 [PMID:21334205]
ChEMBL Inhibition of dexamethasone-induced human NR1-1a/NR2B receptor-mediated excitotoxicity in (S)-glutamate/glycine-stimulated mouse L13-E6 cells assessed as LDH release after 30 mins B 5.49 pIC50 3200 nM IC50 J. Med. Chem. (2010) 53: 3611-3617 [PMID:20361801]
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
ChEMBL Inhibition of Cav1.2 calcium current measured using whole cell patch clamp in human atrial myocytes F 5.74 pIC50 1800 nM IC50 IC50 data for the L-type calcium channel extracted from a set of literature articles

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]