dizocilpine [Ligand Id: 2403] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL284237 (Dizocilpine, MK-801) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| butyrylcholinesterase/Butyrylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276] | ||||||||
| ChEMBL | Inhibition of human BuChE using butyrylthiocholine iodide as substrate peincubated for 5 mins followed by substrate addition by DTNB-reagent based Ellman's method | B | 4.8 | pIC50 | 16000 | nM | IC50 | Eur J Med Chem (2021) 210: 113059-113059 [PMID:33310288] |
| 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: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14] | ||||||||
| 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: 459, 461, 455, 456, 457, 458, 460] [UniProtKB: O15399, O60391, Q05586, Q12879, Q13224, Q14957, Q8TCU5] | ||||||||
| 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: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7] | ||||||||
| 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: 455, 457] [UniProtKB: Q05586, Q13224] | ||||||||
| 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 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]
