phencyclidine [Ligand Id: 4282] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL275528 (Angel dust, J4.441E, Phencyclidine, Phencycline, Phenylcyclidine) |
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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 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 | 6.66 | pIC50 | 217 | nM | IC50 | J Pestic 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: 459, 461, 455, 456, 457, 458, 460] [UniProtKB: O15399, O60391, Q05586, Q12879, Q13224, Q14957, Q8TCU5] | ||||||||
| ChEMBL | Binding affinity to NMDAR (unknown origin) | B | 7.23 | pKi | 59 | nM | Ki | Eur J Med Chem (2020) 194: 112242-112242 [PMID:32248004] |
| 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: 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 | - | 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: 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 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: 455, 456] [UniProtKB: Q05586, Q12879] | ||||||||
| 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: 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 | 5.9 | 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 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]
