phencyclidine [Ligand Id: 4282] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL275528 (Phencyclidine)
  • Acetylcholine receptor protein alpha chain in Torpedo californica [ChEMBL: CHEMBL3097] [UniProtKB: P02710]
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  • butyrylcholinesterase/Butyrylcholinesterase in Mouse [ChEMBL: CHEMBL2528] [GtoPdb: 2471] [UniProtKB: Q03311]
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  • GluN2C in Human [GtoPdb: 458] [UniProtKB: Q14957]
  • GluN2C/Glutamate [NMDA] receptor subunit epsilon 3 in Rat [ChEMBL: CHEMBL401] [GtoPdb: 458] [UniProtKB: Q00961]
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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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  • 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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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 5.5 pIC50 3130 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 6.66 pIC50 217 nM IC50 J Pesticide Sci (1995) 20: 49-56
butyrylcholinesterase/Butyrylcholinesterase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2528] [GtoPdb: 2471] [UniProtKB: Q03311]
ChEMBL -Log (Ki) value for butyrylcholinesterase by inhibiting DFP B 6.28 pKi 524.81 nM Ki J. Med. Chem. (1984) 27: 1267-1271 [PMID:6481761]
ChEMBL Compound was evaluated for the protection of butyrylcholinesterase against DFT in mice B 6.28 pKi 520 nM Ki J. Med. Chem. (1984) 27: 1267-1271 [PMID:6481761]
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 7.64 pKi 23 nM Ki J. Med. Chem. (1998) 41: 393-400 [PMID:9464369]
ChEMBL Affinity to NMDA receptor, using [3H]MK-801 as radioligand in pig brain cortex membranes B 7.82 pKi 15.3 nM Ki J. Med. Chem. (2001) 44: 2814-2826 [PMID:11495592]
GtoPdb Measured vs. exogenously expressed zeta1/epsilon3 (GRIN1/GRIN2C) subunits, at pH 6.9 - 7.11 pIC50 77 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 - 7.11 pIC50 77 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 Displacement of [3H]MK801 from NMDA receptor in rat brain neuronal membrane B 6.57 pKi 270 nM Ki Bioorg. Med. Chem. (2009) 17: 3456-3462 [PMID:19345586]
ChEMBL Displacement of [3H]TCP from NMDA receptor in rat brain membrane B 7.15 pKi 70.79 nM Ki Bioorg. Med. Chem. (2007) 15: 4265-4282 [PMID:17434739]
ChEMBL Displacement of [3H]TCP from NMDA receptor in rat brain membrane B 7.15 pKi 70 nM Ki Bioorg. Med. Chem. (2007) 15: 4265-4282 [PMID:17434739]
ChEMBL Evaluated in vitro binding affinity against PCP receptor using [3H]TCP as radioligand in rat brain membranes B 7.22 pKi 60 nM Ki J. Med. Chem. (1990) 33: 1452-1458 [PMID:2329567]
ChEMBL Binding affinity was determined towards NMDA receptor using [3H]thienylcyclidine as radioligand B 7.42 pKi 38 nM Ki J. Med. Chem. (1994) 37: 4438-4448 [PMID:7528282]
ChEMBL Ability to inhibit glutamate induced accumulation of [45 [Ca2+]] in cultured rat cortical neurons F 6.7 pIC50 200 nM IC50 J. Med. Chem. (1993) 36: 1977-1995 [PMID:8336337]
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 6.74 pIC50 180 nM IC50 J. Med. Chem. (1992) 35: 4135-4142 [PMID:1433216]
ChEMBL Displacement of [3H]MK-801 from NMDA receptor in Wistar rat brain membranes by scintillation counting analysis B 6.96 pIC50 110 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 4131-4135 [PMID:26296478]
ChEMBL Displacement of [3H]TCP from the TCP site of NMDA receptor in rat brain homogenate B 7.33 pIC50 47 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 2983-2986 [PMID:9873659]
ChEMBL Evaluated for their affinity at the PCP site for displacement of [3H]TCP in rat brain homogenates B 7.44 pIC50 36.5 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 7.44 pIC50 36.5 nM IC50 J. Med. Chem. (1993) 36: 1977-1995 [PMID:8336337]
ChEMBL Inhibition of [3H]-MK-801 binding to NMDA receptor from rat cerebral cortical synaptic membrane B 8.01 pIC50 9.8 nM IC50 J. Med. Chem. (1996) 39: 4844-4852 [PMID:8941398]
GluN1/GluN2A/Glutamate NMDA receptor; GRIN1/GRIN2A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907604] [GtoPdb: 455456] [UniProtKB: Q05586Q12879]
ChEMBL Inhibition of human recombinant NR1/NR2A receptor expressed in U2OS assessed as change in intracellular calcium level by FLIPR assay B 6.4 pIC50 398.11 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 2059-2063 [PMID:21334205]
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 7.93 pIC50 11.8 nM IC50 J. Med. Chem. (2015) 58: 8601-8615 [PMID:26430967]
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 5.9 pIC50 1258.93 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 2059-2063 [PMID:21334205]
GluN2C in Human [GtoPdb: 458] [UniProtKB: Q14957]
GtoPdb Measured vs. exogenously expressed zeta1/epsilon3 (GRIN1/GRIN2C) subunits, at pH 6.9 - 7.11 pIC50 77 nM IC50 J. Physiol. (Lond.) (2007) 581: 107-28 [PMID:17303642]
GluN2C/Glutamate [NMDA] receptor subunit epsilon 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL401] [GtoPdb: 458] [UniProtKB: Q00961]
ChEMBL Binding affinity to sigma site of Phencyclidine receptor by displacement of [3H]-(+)-SKF- 10,047 B 6.28 pKi 530 nM Ki J. Med. Chem. (1988) 31: 1571-1575 [PMID:3397994]
ChEMBL Binding affinity of compound against Phencyclidine receptor by displacement of [3H]TCP B 7.04 pKi 91 nM Ki J. Med. Chem. (1988) 31: 1571-1575 [PMID:3397994]
ChEMBL Binding affinity against phencyclidine receptor was determined by the displacement of [3H]TCP of whole rat brain minus cerebellum. B 7.22 pKi 60 nM Ki J. Med. Chem. (1988) 31: 1625-1628 [PMID:2840502]
ChEMBL Inhibition activity against binding of phencyclidine receptor was determined by the displacement of [3H]-TCP of whole rat brain minus cerebellum. B 6.22 pIC50 600 nM IC50 J. Med. Chem. (1988) 31: 1625-1628 [PMID:2840502]
GluN1/Glutamate (NMDA) receptor subunit zeta 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL330] [GtoPdb: 455] [UniProtKB: P35439]
ChEMBL Compound was evaluated for its ability to displace [3H]TCP from PCP N-methyl-D-aspartate glutamate receptor in rat brain B 7.19 pKi 64.5 nM Ki J. Med. Chem. (1992) 35: 4704-4712 [PMID:1469699]
ChEMBL Binding affinity by displacement of [3H]TCP from PCP N-methyl-D-aspartate glutamate receptor of tissue homogenate preparation of rat brain without cerebellum (in vitro) B 7.28 pKi 53 nM Ki J. Med. Chem. (1991) 34: 2615-2623 [PMID:1875352]
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 7.04 pIC50 91 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 7.04 pIC50 91 nM IC50 J. Med. Chem. (1989) 32: 1242-1248 [PMID:2542555]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Inhibition of [3H](+)-pentazocine binding to sigma receptor of guinea pig brain homogenates B 5.75 pKi 1767 nM Ki J. Med. Chem. (1993) 36: 1188-1193 [PMID:8098066]
ChEMBL Compound was evaluated for its ability to displace [3H](+)-pentazocine from sigma receptor in Guinea pig brain B 5.96 pKi 1090 nM Ki J. Med. Chem. (1992) 35: 4704-4712 [PMID:1469699]
ChEMBL Inhibition of specific binding of [3H]DTG to sigma binding site in Guinea pig brain membranes B 5.98 pIC50 1050 nM IC50 J. Med. Chem. (1992) 35: 4683-4689 [PMID:1469697]
ChEMBL Inhibition of specific binding of [3H]3-PPP to sigma binding site in Guinea pig brain membranes B 6 pIC50 1000 nM IC50 J. Med. Chem. (1992) 35: 4683-4689 [PMID:1469697]
ChEMBL Inhibition of specific binding of [125I]-PIPAG to sigma binding site in Guinea pig brain membranes B 6.06 pIC50 868 nM IC50 J. Med. Chem. (1992) 35: 4683-4689 [PMID:1469697]
ChEMBL Inhibition of specific binding of [3H]NANM of sigma binding site in Guinea pig brain membranes B 6.25 pIC50 560 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 Inhibition of [3H]NANM binding to sigma receptor obtained from tissue homogenate preparation of fresh whole rat brain minus cerebellum B 6.28 pIC50 530 nM IC50 J. Med. Chem. (1998) 41: 468-477 [PMID:9484497]
ChEMBL Inhibition of [3H]- N-allylnormetazocine ([3H]NANM) binding to sigma receptor B 6.28 pIC50 530 nM IC50 J. Med. Chem. (1989) 32: 1242-1248 [PMID:2542555]

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]