trifluoperazine [Ligand Id: 214] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL422 (Stelazine Fte, Stelazine, Amylozine, Trifluoperazine)
  • 3-beta-hydroxysteroid-delta(8),delta(7)-isomerase in Human [ChEMBL: CHEMBL4931] [UniProtKB: Q15125]
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  • C-8 sterol isomerase in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL3224] [UniProtKB: P32352]
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  • protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
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  • D2 receptor in Human [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • Hepatitis C virus NS3 protease/helicase in Hepatitis C virus [ChEMBL: CHEMBL4893] [UniProtKB: A3EZI9]
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  • Pleiotropic ABC efflux transporter of multiple drugs in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL1697658] [UniProtKB: P33302]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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  • Trypanothione reductase in Trypanosoma cruzi [ChEMBL: CHEMBL5131] [UniProtKB: P28593]
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  • ubiquitin specific peptidase 1/Ubiquitin carboxyl-terminal hydrolase 1/WD repeat-containing protein 48 in Human [ChEMBL: CHEMBL3430885] [GtoPdb: 2428] [UniProtKB: O94782Q8TAF3]
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  • 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335]
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  • D4 receptor in Human [GtoPdb: 217] [UniProtKB: P21917]
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  • H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
3-beta-hydroxysteroid-delta(8),delta(7)-isomerase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4931] [UniProtKB: Q15125]
ChEMBL Affinity for human EMP expressed in ERG2 deficient strain of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine as radioligand B 8.1 pKi 8 nM Ki J. Med. Chem. (2005) 48: 4754-4764 [PMID:16033255]
Beta-glucuronidase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4814] [UniProtKB: P06760]
ChEMBL Inhibitory effect of compound on the release of Beta-glucuronidase in rat neutrophils stimulated with fMLP/CB B 5.11 pIC50 7800 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 1011-1014 [PMID:15013012]
C-8 sterol isomerase in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3224] [UniProtKB: P32352]
ChEMBL Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand B 6.3 pKi 500 nM Ki J. Med. Chem. (2005) 48: 4754-4764 [PMID:16033255]
Calmodulin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6093] [UniProtKB: P0DP23]
ChEMBL Binding affinity to calmodulin B 6 pKd 1000 nM Kd J. Med. Chem. (2008) 51: 3081-3093 [PMID:18459732]
Calmodulin in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6092] [UniProtKB: P62157]
ChEMBL Binding affinity to dansylated bovine testes CaM by fluorescence analysis in presence of calcium2+ B 5.3 pKd 5000 nM Kd Eur. J. Med. Chem. (2016) 116: 36-45 [PMID:27043269]
ChEMBL Binding affinity to bovine brain CaM by FTPFACE analysis B 5.47 pKd 3400 nM Kd Eur. J. Med. Chem. (2016) 116: 36-45 [PMID:27043269]
protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
ChEMBL Inhibition of DNA-PK in human U1810 cells after 30 mins B 4 pIC50 100000 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 5352-5359 [PMID:22835870]
D2 receptor in Human [GtoPdb: 215] [UniProtKB: P14416]
GtoPdb - - 9.02 pKi 0.96 nM Ki Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531];
Neuropsychopharmacology (1997) 16: 93-110; discussion 111-35 [PMID:9015795]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Compound was tested for its effect on dopamine saturation analysis B 9.27 pKd 0.53 nM Kd J. Med. Chem. (1986) 29: 359-369 [PMID:2869146]
ChEMBL Binding affinity towards dopamine receptor D2 by displacing [3H]spiperone radioligand in rat striatum B 8.66 pKi 2.2 nM Ki J. Med. Chem. (1992) 35: 552-558 [PMID:1346653]
ChEMBL Compound was tested in vitro for its affinity towards rat striatal Dopamine receptor D2 labeled with [3H]- spiperone B 7.8 pIC50 16 nM IC50 J. Med. Chem. (1986) 29: 359-369 [PMID:2869146]
Emopamil-binding protein-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2311238] [UniProtKB: Q9BY08]
ChEMBL Binding affinity to emopamil binding protein (unknown origin) B 8.41 pKi 3.9 nM Ki Bioorg. Med. Chem. (2013) 21: 215-222 [PMID:23199475]
Hepatitis C virus NS3 protease/helicase in Hepatitis C virus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4893] [UniProtKB: A3EZI9]
ChEMBL Inhibitory concentration against hepatitis C virus helicase; range 0.6-0.7 B 6.15 pIC50 700 nM IC50 J. Med. Chem. (2005) 48: 1-20 [PMID:15633995]
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 5.29 pKi 5100.8 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 5.21 pIC50 6226 nM IC50 DrugMatrix in vitro pharmacology data
Lysozyme C in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2297] [UniProtKB: P00697]
ChEMBL Inhibitory effect of compound on the release of lysozyme in rat neutrophils stimulated with fMLP/CB B 5.05 pIC50 9000 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 1011-1014 [PMID:15013012]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL Concentration giving half of the maximal ATPase activity calculated for the high-affinity binding site of the CHO P-Glycoprotein (P-gp) in two-affinity model B 5.19 pKi 6500 nM Ki J. Med. Chem. (2002) 45: 5671-5686 [PMID:12477351]
ChEMBL TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells F 4.96 pIC50 10900 nM IC50 Biochem. Biophys. Res. Commun. (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells F 5.14 pIC50 7200 nM IC50 Biochem. Biophys. Res. Commun. (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells F 5.2 pIC50 6300 nM IC50 Biochem. Biophys. Res. Commun. (2001) 289: 580-585 [PMID:11716514]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimicrobial activity against Plasmodium falciparum F 5.22 pIC50 6000 nM IC50 Bioorg. Med. Chem. (2010) 18: 2225-2231 [PMID:20185316]
ChEMBL DNDI: Malaria in Vitro, 72 hour F 5.83 pIC50 1480 nM IC50 Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning
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-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 from rat hippocampus B 6.39 pKi 411 nM Ki J. Med. Chem. (1992) 35: 552-558 [PMID:1346653]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand B 7.82 pKi 15 nM Ki J. Med. Chem. (2005) 48: 4754-4764 [PMID:16033255]
Trypanothione reductase in Trypanosoma cruzi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5131] [UniProtKB: P28593]
ChEMBL Inhibitory activity against recombinant Trypanosoma cruzi (Trypanosoma cruzi) Trypanothione reductase (linear competitive type) B 4.64 pKi 23000 nM Ki J. Med. Chem. (1998) 41: 148-156 [PMID:9457238]
ChEMBL Inhibitory activity against recombinant Trypanosoma cruzi (Trypanosoma cruzi) Trypanothione reductase B 4.14 pIC50 72000 nM IC50 J. Med. Chem. (1998) 41: 148-156 [PMID:9457238]
ubiquitin specific peptidase 1/Ubiquitin carboxyl-terminal hydrolase 1/WD repeat-containing protein 48 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3430885] [GtoPdb: 2428] [UniProtKB: O94782Q8TAF3]
ChEMBL Inhibition of human USP1/UAF1 complex using Ub-Rho as substrate by qHTS assay B 5.1 pIC50 8000 nM IC50 J Med Chem (2016) 59: 9321-9336 [PMID:27362876]
5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 7.9 pKi - - - Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]
5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335]
GtoPdb - - 6.4 pKi - - - Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]
D4 receptor in Human [GtoPdb: 217] [UniProtKB: P21917]
GtoPdb - - 7.36 pKi 44 nM Ki Neuropsychopharmacology (1997) 16: 93-110; discussion 111-35 [PMID:9015795]
H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb - - 7.2 pKi - - - Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]

ChEMBL data shown on this page come from version 25:

A.P. Bento, A. Gaulton, A. Hersey, et al. (2014). The ChEMBL bioactivity database: an update. Nucl. Acids Res. Database Issue. 42 D1083-D1090. [PMID:24214965]