perphenazine [Ligand Id: 209] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL567 (Perphenazine maleate, NSC-150866, Trilafon-La, Perphenazine, Decentan, Trilafon, Chlorpiprazine, Fentazin, Perphenazine Fendizoate, Perphenazine fendizoate, Etaperazine)
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • This target only has 1 pki data point
  • 9.59
1 CHEMBL567_lig_chart_1 Dopamine D2 receptor Human
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  • Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
  • This target only has 1 pki data point
  • 5.46
2 CHEMBL567_lig_chart_2 HERG Human
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  • Plasmodium falciparum [ChEMBL: CHEMBL364]
  • This target only has 0 pki data point
  • 0
3 CHEMBL567_lig_chart_3 Plasmodium falciparum Plasmodium falciparum
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  • Pleiotropic ABC efflux transporter of multiple drugs in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL1697658] [UniProtKB: P33302]
  • This target only has 0 pki data point
  • 0
4 CHEMBL567_lig_chart_4 Pleiotropic ABC efflux transporter of multiple drugs Saccharomyces cerevisiae S288c
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
  • 7.6
5 CHEMBL567_lig_chart_5 Serotonin 7 (5-HT7) receptor HumanRat
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  • 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
  • This target only has 1 pki data point
  • 8.2
6 CHEMBL567_lig_chart_6 5-HT2A receptor Human
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  • 5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335]
  • This target only has 1 pki data point
  • 6.9
7 CHEMBL567_lig_chart_7 5-HT2C receptor Human
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  • 5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406]
  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
  • 7.8
8 CHEMBL567_lig_chart_8 5-HT6 receptor HumanRat
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  • H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
  • This target only has 1 pki data point
  • 8.1
9 CHEMBL567_lig_chart_9 H1 receptor Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
GtoPdb - - 9.59 pKi 0.26 nM Ki Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531];
Clinical Neuroscience Research (2001) 1: 53-60
ChEMBL Antagonist activity at dopamine D2 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 assessed as inhibition of agonist-induced response incubated for 60 mins in incubator followed by 15 mins at room temperature by FLIPR assay B 9.52 pIC50 0.3 nM IC50 J. Med. Chem. (2013) 56: 4671-4690 [PMID:23675993]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 5.46 pKi 3454.1 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 5.38 pIC50 4216 nM IC50 DrugMatrix in vitro pharmacology data
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 5.2 pIC50 6309.57 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 5.4 pIC50 3981.07 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 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 7G8 after 72 hrs by SYBR green assay F 5.5 pIC50 3162.28 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 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 5.6 pIC50 2511.89 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
Pleiotropic ABC efflux transporter of multiple drugs in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697658] [UniProtKB: P33302]
ChEMBL Inhibition of Pdr5p-mediated rhodamine 6G transport in Saccharomyces cerevisiae MKPDR5h plasma membrane by spectrofluorometric assay B 5.85 pIC50 1400 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 1516-1527 [PMID:19188399]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
GtoPdb - - 7.2 pKi - - - Psychopharmacology (Berl.) (2005) 179: 461-9 [PMID:15821958]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 7 receptor B 7.64 pKi 23 nM Ki J. Med. Chem. (2003) 46: 2795-2812 [PMID:12825922]
5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
GtoPdb - - 7.6 pKi - - - J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]
5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 8.2 pKi - - - Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]
5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335]
GtoPdb - - 6.9 pKi - - - Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]
5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406]
GtoPdb - - 7.1 pKi - - - Psychopharmacology (Berl.) (2005) 179: 461-9 [PMID:15821958]
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 7.8 pKi - - - J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]
H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb - - 8.1 pKi - - - Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]

ChEMBL data shown on this page come from version 28:

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]