phencyclidine [Ligand Id: 4282] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL275528 (Angel dust, Fenciclidina, J4.441E, Phencyclidine, Phencycline, Phenylcyclidine, Tic tac) |
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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 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]
