dizocilpine [Ligand Id: 2403] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL284237 (Dizocilpine, MK-801)
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  • GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Rat [ChEMBL: CHEMBL341] [GtoPdb: 405] [UniProtKB: P23576]
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  • GluN2A/Glutamate [NMDA] receptor subunit epsilon 1 in Human [ChEMBL: CHEMBL1972] [GtoPdb: 456] [UniProtKB: Q12879]
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  • GluN1/Glutamate (NMDA) receptor subunit zeta 1 in Rat [ChEMBL: CHEMBL330] [GtoPdb: 455] [UniProtKB: P35439]
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  • Prolylcarboxypeptidase/Lysosomal Pro-X carboxypeptidase in Human [ChEMBL: CHEMBL2335] [GtoPdb: 1584] [UniProtKB: P42785]
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  • μ receptor/Mu opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
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  • Kir3.2 in Mouse [GtoPdb: 435] [UniProtKB: P48542]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907607] [GtoPdb: 419410416414408406413405407415409404412411417] [UniProtKB: O09028P15431P18506P18508P19969P20236P23574P23576P28471P28473P30191P62813P63079P63138Q91ZM7Q9ES14]
ChEMBL In vitro inhibition of [3H]flunitrazepam displacement from GABA-A receptor B 4 pKi >100000 nM Ki J. Med. Chem. (1993) 36: 2499-2507 [PMID:8355251]
GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL341] [GtoPdb: 405] [UniProtKB: P23576]
ChEMBL Tested for in vitro inhibition of the displacement of [3H]mazindol from GABA receptor B 4.39 pKi 40867 nM Ki J. Med. Chem. (1993) 36: 2499-2507 [PMID:8355251]
GluN2D/GluN3B/GluN1/GluN2A/GluN2B/GluN2C/GluN3A/Glutamate [NMDA] receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094124] [GtoPdb: 459461455456457458460] [UniProtKB: O15399O60391Q05586Q12879Q13224Q14957Q8TCU5]
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 8.17 pKi 6.8 nM Ki J. Med. Chem. (1998) 41: 393-400 [PMID:9464369]
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 8.92 pKi 1.2 nM Ki J. Med. Chem. (1998) 41: 393-400 [PMID:9464369]
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455456457458459461460] [UniProtKB: P35439Q00959Q00960Q00961Q62645Q8VHN2Q9R1M7]
ChEMBL Binding affinity to rat brain NMDA receptor B 7.43 pKd 37.2 nM Kd Bioorg. Med. Chem. Lett. (2015) 25: 5583-5588 [PMID:26525866]
ChEMBL Inhibition of N-methyl-D-aspartate glutamate receptor (NMDA receptor) from homogenized rat brain membrane, using [3H]-MK-801 as a radioligand B 6.68 pKi 211 nM Ki J. Med. Chem. (1990) 33: 789-808 [PMID:1688947]
ChEMBL Inhibition of N-methyl-D-aspartate glutamate receptor (NMDA receptor) from homogenized rat brain membrane, using [3H]-MK-801 as a radioligand B 7.25 pKi 56 nM Ki J. Med. Chem. (1990) 33: 789-808 [PMID:1688947]
ChEMBL Displacement of [3H]MK801 from NMDA receptor in rat brain neuronal membrane B 7.37 pKi 43 nM Ki Bioorg. Med. Chem. (2009) 17: 3456-3462 [PMID:19345586]
ChEMBL Inhibition of N-methyl-D-aspartate glutamate receptor (NMDA receptor) from homogenized rat brain membrane, using [3H]-MK-801 as a radioligand B 7.51 pKi 31 nM Ki J. Med. Chem. (1990) 33: 789-808 [PMID:1688947]
ChEMBL Displacement of [3H]MK801 from NMDA receptor in rat brain neuronal membrane B 8.05 pKi 9 nM Ki Bioorg. Med. Chem. (2009) 17: 3456-3462 [PMID:19345586]
ChEMBL Tested for in vitro inhibition of the displacement of [3H]TCP from NMDA receptor B 8.2 pKi 6.3 nM Ki J. Med. Chem. (1993) 36: 2499-2507 [PMID:8355251]
ChEMBL Tested for in vitro inhibition of the displacement of (+)-[3H]dizocilpine from NMDA receptor B 8.6 pKi 2.5 nM Ki J. Med. Chem. (1993) 36: 2499-2507 [PMID:8355251]
ChEMBL Displacement of [3H]TCP from NMDA receptor of rat brain membranes B 8.66 pKi 2.2 nM Ki J. Med. Chem. (1995) 38: 2483-2489 [PMID:7608913]
ChEMBL Binding affinity against phencyclidine (PCP) site of N-methyl-D-aspartate glutamate receptor from rat brain, using [3H]- TCP as radioligand. B 8.66 pKi 2.2 nM Ki J. Med. Chem. (1995) 38: 1826-1830 [PMID:7752207]
ChEMBL Binding affinity at TCP site of NMDA receptor was determined in rat brain homogenate by [3H]TCP displacement. B 8.7 pKi 2 nM Ki J. Med. Chem. (1995) 38: 21-27 [PMID:7837234]
ChEMBL In vitro radioligand binding assay for the N-methyl-D-aspartate glutamate receptor is performed using [3H]MK-801 and rat brain membrane suspensions B 8.77 pKi 1.7 nM Ki J. Med. Chem. (1997) 40: 4281-4289 [PMID:9435897]
ChEMBL In vitro binding to N-methyl-D-aspartate glutamate receptor using [3H]MK-801 (1 nM) and rat brain membrane suspensions B 8.89 pKi 1.3 nM Ki Bioorg. Med. Chem. Lett. (2002) 12: 1583-1586 [PMID:12039567]
ChEMBL Evaluated for its affinity to bind PCP N-methyl-D-aspartate (NMDA) glutamate receptor in rat brain membrane using [3H]MK-801 as radioligand B 6.49 pIC50 320 nM IC50 J. Med. Chem. (1990) 33: 1296-1305 [PMID:1691788]
ChEMBL Ability to inhibit glutamate induced accumulation of [45 [Ca2+]] in cultured rat cortical neurons F 7.24 pIC50 58 nM IC50 J. Med. Chem. (1993) 36: 1977-1995 [PMID:8336337]
ChEMBL Evaluated for its affinity to bind PCP N-methyl-D-aspartate (NMDA) glutamate receptor in rat brain membrane using [3H]MK-801 as radioligand B 7.25 pIC50 56 nM IC50 J. Med. Chem. (1990) 33: 1296-1305 [PMID:1691788]
ChEMBL Evaluated for its affinity to bind PCP N-methyl-D-aspartate (NMDA) glutamate receptor in rat brain membrane using [3H]MK-801 as radioligand B 7.44 pIC50 36 nM IC50 J. Med. Chem. (1990) 33: 1296-1305 [PMID:1691788]
ChEMBL Binding affinity against PCP binding site associated with N-methyl-D-aspartate glutamate receptor from rat synaptic plasma membrane(SPM) determined using [3H]TCP as radioligand. B 8 pIC50 10 nM IC50 J. Med. Chem. (1992) 35: 4135-4142 [PMID:1433216]
ChEMBL Inhibition against NMDA receptor by displacement of [3H]TCP binding from rat cortical membranes B 8.05 pIC50 8.9 nM IC50 J. Med. Chem. (1994) 37: 3008-3015 [PMID:7932522]
ChEMBL The compound was tested in vitro for the displacement of the radioligand (+)-[3H]-MK-801 from synaptic plasma membranes from rat cortex against N-methyl-D-aspartate glutamate receptor B 8.25 pIC50 5.6 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 2411-2415 [PMID:11078190]
ChEMBL Potency towards NMDA receptor measured as inhibition of (+)-[3-3H]MK-801 binding from synaptic plasma membrane obtained from rat cortex B 8.25 pIC50 5.6 nM IC50 Bioorg. Med. Chem. Lett. (1999) 9: 1915-1920 [PMID:10450953]
ChEMBL Inhibition of [3H]MK-801 binding to the PCP receptor site in guinea pig brain homogenate B 8.38 pIC50 4.2 nM IC50 J. Med. Chem. (1993) 36: 1938-1946 [PMID:8101572]
ChEMBL Functional NMDA receptor antagonism expressed as inhibition of NMDA/glycine induced increase in cytosolic calcium in cultured rat cerebellar granule cells F 8.47 pIC50 3.4 nM IC50 Bioorg. Med. Chem. Lett. (1999) 9: 1915-1920 [PMID:10450953]
ChEMBL The compound was tested in vitro for the inhibition of N-methyl-D-aspartate glutamate receptor in rat cerebellar granule cells (RCGCs). B 8.47 pIC50 3.4 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 2411-2415 [PMID:11078190]
ChEMBL Inhibitory concentration of compound required to displace [3H]TCP 1-[ 1-(2-thienyl)cyclohexyl]piperidine in whole rat brain homogenate B 8.52 pIC50 3 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 49-54
ChEMBL Evaluated for their affinity at the PCP site for displacement of [3H]TCP in rat brain homogenates B 8.53 pIC50 2.92 nM IC50 J. Med. Chem. (1993) 36: 654-670 [PMID:8459395]
ChEMBL Binding affinity towards PCP site of the NMDA receptor was measured by displacement of [3H]TPC in whole rat brain homogenate B 8.53 pIC50 2.92 nM IC50 J. Med. Chem. (1993) 36: 1977-1995 [PMID:8336337]
GluN1/GluN2B/Glutamate NMDA receptor; GRIN1/GRIN2B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907603] [GtoPdb: 455457] [UniProtKB: Q05586Q13224]
ChEMBL Antagonist activity at NR1/2B receptor expressed in xenopus laevis at pH 6.9 by two electrode voltage clamp method F 8.05 pIC50 9 nM IC50 J. Med. Chem. (2008) 51: 3765-3776 [PMID:18540667]
GluN2A/Glutamate [NMDA] receptor subunit epsilon 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1972] [GtoPdb: 456] [UniProtKB: Q12879]
ChEMBL Antagonist activity at NR2A transfected in oocytes F 7.54 pIC50 29 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 3399-3403 [PMID:21524576]
GluN1/Glutamate (NMDA) receptor subunit zeta 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL330] [GtoPdb: 455] [UniProtKB: P35439]
ChEMBL Ability to displace [3H]TCP from high affinity PCP N-methyl-D-aspartate glutamate receptor in rat brain homogenates in vitro was determined B 7.51 pKi 31 nM Ki J. Med. Chem. (1990) 33: 1069-1076 [PMID:2155320]
ChEMBL Ability to displace [3H]TCP from high affinity PCP N-methyl-D-aspartate glutamate receptor in rat brain homogenates in vitro was determined B 8.05 pKi 9 nM Ki J. Med. Chem. (1990) 33: 1069-1076 [PMID:2155320]
ChEMBL Ability to displace [3H]TCP from high affinity PCP N-methyl-D-aspartate glutamate receptor in rat brain homogenates in vitro was determined B 8.1 pKi 8 nM Ki J. Med. Chem. (1990) 33: 1069-1076 [PMID:2155320]
Prolylcarboxypeptidase/Lysosomal Pro-X carboxypeptidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2335] [GtoPdb: 1584] [UniProtKB: P42785]
ChEMBL Inhibition of [3H]-TCP binding to PCP receptor obtained from tissue homogenate preparation of fresh whole rat brain minus cerebellum B 8.28 pIC50 5.3 nM IC50 J. Med. Chem. (1998) 41: 468-477 [PMID:9484497]
ChEMBL Inhibition of [3H]1-[1-(2-thienyl) piperidine ([3H]TCP) binding to phencyclidine receptor B 8.28 pIC50 5.3 nM IC50 J. Med. Chem. (1989) 32: 1242-1248 [PMID:2542555]
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
ChEMBL Tested for in vitro inhibition of the displacement of [3H]FOXY from mu opioid receptor B 4 pKi >100000 nM Ki J. Med. Chem. (1993) 36: 2499-2507 [PMID:8355251]
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL Percent inhibition against Muscarinic acetylcholine receptor M5 at 1 uM B 8.7 pIC50 2 nM IC50 J. Med. Chem. (2005) 48: 6887-6896 [PMID:16250647]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5.4 pIC50 3981.07 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 5.6 pIC50 2511.89 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5.7 pIC50 1995.26 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Inhibition of specific binding of [125I]PIPAG to sigma receptor in Guinea pig brain membranes B 5 pIC50 >10000 nM IC50 J. Med. Chem. (1992) 35: 4683-4689 [PMID:1469697]
ChEMBL Inhibition of specific binding of [3H]NANM of sigma receptor in Guinea pig brain membranes B 5 pIC50 >10000 nM IC50 J. Med. Chem. (1992) 35: 4683-4689 [PMID:1469697]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
ChEMBL Tested for in vitro inhibition of the displacement of (+)-[3H]pentazocine from sigma opioid receptor B 4.23 pKi 59167 nM Ki J. Med. Chem. (1993) 36: 2499-2507 [PMID:8355251]
ChEMBL Inhibition of [3H]NANM binding to sigma receptor obtained from tissue homogenate preparation of fresh whole rat brain minus cerebellum B 5.77 pIC50 1700 nM IC50 J. Med. Chem. (1998) 41: 468-477 [PMID:9484497]
ChEMBL Inhibition of [3H]- N-allylnormetazocine ([3H]NANM) binding to sigma receptor B 5.77 pIC50 1700 nM IC50 J. Med. Chem. (1989) 32: 1242-1248 [PMID:2542555]
Kir3.2 in Mouse [GtoPdb: 435] [UniProtKB: P48542]
GtoPdb - - 3.7 pIC50 - - - Neuron (1996) 16: 941-52 [PMID:8630252]

ChEMBL data shown on this page come from version 27:

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]