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

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ChEMBL ligand: CHEMBL422 (Amylozine, Apo-trifluoperazine, Flurazine, NSC-17474, NSC-46061, RP-7623, Stelazine, Stelazine fte, Trifluoperazina, Trifluoperazine)
  • 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase in Human [ChEMBL: CHEMBL4931] [UniProtKB: Q15125]
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  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • ABCB1/ATP-dependent translocase ABCB1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
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  • C-8 sterol isomerase ERG2 in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL3224] [UniProtKB: P32352]
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  • D2 receptor in Human [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/D(2) dopamine receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase catalytic subunit in Human [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
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  • FPR2/N-formyl peptide receptor 2 in Human [ChEMBL: CHEMBL4227] [GtoPdb: 223] [UniProtKB: P25090]
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  • Pleiotropic ABC efflux transporter of multiple drugs in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL1697658] [UniProtKB: P33302]
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  • Sarcoplasmic/endoplasmic reticulum calcium ATPase 1 in Rabbit [ChEMBL: CHEMBL4693] [UniProtKB: P04191]
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  • sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 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: O94782, Q8TAF3]
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  • Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
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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]
5-HT1A receptor/5-hydroxytryptamine receptor 1A 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]
ABCB1/ATP-dependent translocase ABCB1 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]
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 ERG2 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 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]
Calmodulin-1 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]
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/D(2) dopamine 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]
protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase catalytic subunit 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]
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]
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]
FPR2/N-formyl peptide receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4227] [GtoPdb: 223] [UniProtKB: P25090]
ChEMBL Fluorescence Polarization Assay: The competition binding assay was performed in a 384-well plate format and in 20 ÎĽl reactions. Serial dilutions (0.001-100 ÎĽM) of a test compound were incubated with CaM in the presence of 16B05 at room temperature for 30 min. The final binding reagent contained 50 nM of CaM and 5 nM of 16B05 in the assay buffer (50 mM HEPES pH 7.5, 0.01% (w/v) Triton X-100 and 100 ÎĽM CaCl2). Each plate contained two types of control wells, containing either 5 nM fluorescent probe bound to 50 nM CaM (bound state, maximum read) or 5 nM unbound probe alone (free state, minimum read) in the assay buffer. Reference compounds Trifluoperazine (CP-Chengdu, Barcode 20008599), A-3 hydrochloride (Sigma, Cat. No. A1980), and A-7 (Tocris Bioscience, Cat. No. 0378) were also included. Upon completion of the incubation, fluorescence polarization degrees (excitation at 531 nm, emission at 595 nm) were measured on the EnVision Microplate Reader (PerkinElmer). Data analysis was performed according to Audran et al., Biochim Biophys Acta. 1833 (2013) 1720-1731. Fluorescence decay was plotted against log concentration of the compound and half maximal inhibitory concentration (IC50) was calculated by XLfit version 4.3.1 (ID Business Solutions) with a 4-parameter logistic model or sigmoidal dose-response model. B 5.95 pIC50 1110 nM IC50 US-11542290-B2. Phenothiazine derivatives and uses thereof (2023)
ChEMBL Fluorescence Polarization Assay: The competition binding assay was performed in a 384-well plate format and in 20 ÎĽl reactions. Serial dilutions (0.001-100 ÎĽM) of a test compound were incubated with CaM in the presence of 16B05 at room temperature for 30 min. The final binding reagent contained 50 nM of CaM and 5 nM of 16B05 in the assay buffer (50 mM HEPES pH 7.5, 0.01% (w/v) Triton X-100 and 100 ÎĽM CaCl2). Each plate contained two types of control wells, containing either 5 nM fluorescent probe bound to 50 nM CaM (bound state, maximum read) or 5 nM unbound probe alone (free state, minimum read) in the assay buffer. Reference compounds Trifluoperazine (CP-Chengdu, Barcode 20008599), A-3 hydrochloride (Sigma, Cat. No. A1980), and A-7 (Tocris Bioscience, Cat. No. 0378) were also included. Upon completion of the incubation, fluorescence polarization degrees (excitation at 531 nm, emission at 595 nm) were measured on the EnVision Microplate Reader (PerkinElmer). Data analysis was performed according to Audran et al., Biochim Biophys Acta. 1833 (2013) 1720-1731. Fluorescence decay was plotted against log concentration of the compound and half maximal inhibitory concentration (IC50) was calculated by XLfit version 4.3.1 (ID Business Solutions) with a 4-parameter logistic model or sigmoidal dose-response model. B 5.97 pIC50 1060 nM IC50 US-11542290-B2. Phenothiazine derivatives and uses thereof (2023)
ChEMBL Fluorescence Polarization Assay: The competition binding assay was performed in a 384-well plate format and in 20 ÎĽl reactions. Serial dilutions (0.001-100 ÎĽM) of a test compound were incubated with CaM in the presence of 16B05 at room temperature for 30 min. The final binding reagent contained 50 nM of CaM and 5 nM of 16B05 in the assay buffer (50 mM HEPES pH 7.5, 0.01% (w/v) Triton X-100 and 100 ÎĽM CaCl2). Each plate contained two types of control wells, containing either 5 nM fluorescent probe bound to 50 nM CaM (bound state, maximum read) or 5 nM unbound probe alone (free state, minimum read) in the assay buffer. Reference compounds Trifluoperazine (CP-Chengdu, Barcode 20008599), A-3 hydrochloride (Sigma, Cat. No. A1980), and A-7 (Tocris Bioscience, Cat. No. 0378) were also included. Upon completion of the incubation, fluorescence polarization degrees (excitation at 531 nm, emission at 595 nm) were measured on the EnVision Microplate Reader (PerkinElmer). Data analysis was performed according to Audran et al., Biochim Biophys Acta. 1833 (2013) 1720-1731. Fluorescence decay was plotted against log concentration of the compound and half maximal inhibitory concentration (IC50) was calculated by XLfit version 4.3.1 (ID Business Solutions) with a 4-parameter logistic model or sigmoidal dose-response model. B 5.97 pIC50 1060 nM IC50 US-11542290-B2. Phenothiazine derivatives and uses thereof (2023)
NS3 in Hepatitis C virus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293269] [UniProtKB: A3EZJ3]
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]
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
ChEMBL Antiplasmodial activity against Plasmodium falciparum FCB infected in human erythrocytes after 30 mins by FACS analysis F 5.72 pEC50 1900 nM EC50 J Med Chem (2018) 61: 8061-8077 [PMID:29771541]
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]
Sarcoplasmic/endoplasmic reticulum calcium ATPase 1 in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4693] [UniProtKB: P04191]
ChEMBL Inhibition of rabbit skeletal muscle microsomes SERCA1a incubated for 10 mins by enzyme-coupled method B 4.35 pIC50 45000 nM IC50 J Med Chem (2020) 63: 1937-1963 [PMID:32030976]
sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 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: O94782, Q8TAF3]
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]
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 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
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 36:

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]