ketamine [Ligand Id: 4233] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL742 (Anaket v, Calypsol, Clorketam 1000, Dl-ketamine, Imalgene 1000, Ketalar, Ketamina, Ketamine, Ketasol 100, Narketan, NSC-70151, PMI-150, Tekam, Ursotamin, Vetaket) |
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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 Pestic 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 Pestic 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: 459, 461, 455, 456, 457, 458, 460] [UniProtKB: O15399, O60391, Q05586, Q12879, Q13224, Q14957, Q8TCU5] | ||||||||
| 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] |
| ChEMBL | Displacement of [3H]-MK801 from NMDA receptor in human frontal cortex in presence of Mg2+ by scintillation counting method | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2020) 63: 13514-13525 [PMID:32915563] |
| ChEMBL | Displacement of [3H]-MK801 from NMDA receptor in human cortex incubated for 2 hrs in presence of Mg2+ by scintillation counting method | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2020) 63: 13514-13525 [PMID:32915563] |
| 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: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: Q05586, Q12879, Q13224, Q14957, O15399, O60391, Q8TCU5] | ||||||||
| 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: 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 whole brain homogenate incubated for 2 hrs in presence of Mg2+ by liquid scintillation counting method | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2020) 63: 13514-13525 [PMID:32915563] |
| ChEMBL | Displacement of [3H]-MK801 from NMDA receptor in rat brain membranes incubated for 2 hrs in presence of Mg2+ by radioligand binding assay | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2020) 63: 13514-13525 [PMID:32915563] |
| ChEMBL | Displacement of [3H]-MK801 from NMDA receptor in rat brain membranes incubated for 60 mins in presence of Mg2+ by liquid scintillation counting method | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2020) 63: 13514-13525 [PMID:32915563] |
| ChEMBL | Displacement of [3H]-MK801 from NMDA receptor in Sprague-Dawley rat cerebral cortex by liquid scintillation counting method | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2020) 63: 13514-13525 [PMID:32915563] |
| ChEMBL | Displacement of [3H]-MK801 from NMDA receptor in rat brain membranes incubated for 45 mins in presence of Mg2+ by scintillation counting method | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2020) 63: 13514-13525 [PMID:32915563] |
| ChEMBL | Displacement of [3H]-TCP from NMDA receptor in rat brain membranes incubated for 45 mins in presence of Mg2+ by scintillation counting method | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2020) 63: 13514-13525 [PMID:32915563] |
| ChEMBL | Displacement of [3H]-MK801 from NMDA receptor in rat brain membranes incubated for 2 hrs in presence of Mg2+/glumate/glycine by radioligand binding assay | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2020) 63: 13514-13525 [PMID:32915563] |
| ChEMBL | Displacement of [3H]-MK801 from NMDA receptor in rat spinal cord incubated for 45 mins by liquid scintillation spectrometry | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2020) 63: 13514-13525 [PMID:32915563] |
| ChEMBL | Displacement of [3H]-MK801 from NMDA receptor in Sprague-Dawley rat cerebellum by liquid scintillation counting method | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2020) 63: 13514-13525 [PMID:32915563] |
| ChEMBL | Displacement of [3H]-MK801 from NMDA receptor in Sprague-Dawley rat brain synaptic membrane incubated for 60 mins by liquid scintillation counting method | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2020) 63: 13514-13525 [PMID:32915563] |
| ChEMBL | Displacement of [3H]-MK801 from NMDA receptor in rat striatum incubated for 2 hrs in presence of Mg2+ by scintillation counting method | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2020) 63: 13514-13525 [PMID:32915563] |
| ChEMBL | Displacement of [3H]-MK801 from NMDA receptor in Sprague-Dawley rat cortex incubated for 2 hrs in presence of Mg2+ by scintillation counting method | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2020) 63: 13514-13525 [PMID:32915563] |
| ChEMBL | Displacement of [3H]-MK801 from NMDA receptor in rat forebrain homogenate incubated for 2 hrs in presence of Mg2+ by liquid scintillation counting method | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2020) 63: 13514-13525 [PMID:32915563] |
| ChEMBL | Inhibition of NMDAR-mediated excitatory postsynaptic potential in Sprague-Dawley rat hippocampus CA1 region by electrophysiology | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2020) 63: 13514-13525 [PMID:32915563] |
| 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: 455, 456] [UniProtKB: Q05586, Q12879] | ||||||||
| ChEMBL | Displacement of [3H]-MK801 from human forebrain GluN1/GluN2B expressed in HEK293 cells by at -70 mV holding potential by patch-clamp assay | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2020) 63: 13514-13525 [PMID:32915563] |
| 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/GluN2A/Glutamate NMDA receptor; Grin1/Grin2a in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096680] [GtoPdb: 455, 456] [UniProtKB: P35439, Q00959] | ||||||||
| ChEMBL | Displacement of [3H]-MK801 from rat brain GluN1/GluN2A expressed in HEK293 cells | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2020) 63: 13514-13525 [PMID:32915563] |
| ChEMBL | Inhibition of eGFP-tagged rat GluN1-1a/GluN2A transfected in human tsA201 cells assessed as inhibition glutamate-induced current measured at -65 mV holding potential applied for 10 secs by whole-cell patch-clamp method | B | 6 | pIC50 | 1000 | nM | IC50 | Eur J Med Chem (2022) 236: 114354-114354 [PMID:35453065] |
| GluN1/GluN2B/Glutamate NMDA receptor; GRIN1/GRIN2B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907603] [GtoPdb: 455, 457] [UniProtKB: Q05586, Q13224] | ||||||||
| 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] |
| GluN1/GluN2B/Glutamate NMDA receptor; Grin1/Grin2b in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096666] [GtoPdb: 455, 457] [UniProtKB: P35439, Q00960] | ||||||||
| ChEMBL | Displacement of [3H]-MK801 from rat brain GluN1/GluN2B expressed in HEK293 cells | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2020) 63: 13514-13525 [PMID:32915563] |
| 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 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]
