AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: trifluoperazine
Target: DNA-dependent protein kinase catalytic subunit (Kinase)
Gene: PRKDC
UniProt: P78527 (PRKDC_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4
Assay: Inhibition of DNA-PK in human U1810 cells after 30 mins
Drug: trifluoperazine
Target: NS3 (Enzyme)
Gene: NS3
UniProt: A3EZI9 (A3EZI9_9HEPC)
Organism: Hepatitis C virus
Activity: IC50 = 6.15
Assay: Inhibitory concentration against hepatitis C virus helicase; range 0.6-0.7
Drug: trifluoperazine
Target: Beta-glucuronidase (Enzyme)
Gene: Gusb
UniProt: P06760 (BGLR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.11
Assay: Inhibitory effect of compound on the release of Beta-glucuronidase in rat neutrophils stimulated with fMLP/CB
Drug: trifluoperazine
Target: Lysozyme C-1 (Enzyme)
Gene: Lyz1
UniProt: P00697 (LYSC1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.05
Assay: Inhibitory effect of compound on the release of lysozyme in rat neutrophils stimulated with fMLP/CB
Drug: trifluoperazine
Target: C-8 sterol isomerase (Enzyme)
Gene: ERG2
UniProt: P32352 (ERG2_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: Ki = 6.3
Assay: Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand
Drug: trifluoperazine
Target: Pleiotropic ABC efflux transporter of multiple drugs (Transporter)
Gene: PDR5
UniProt: P33302 (PDR5_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: IC50 = 5.85
Assay: Inhibition of Pdr5p-mediated rhodamine 6G transport in Saccharomyces cerevisiae MKPDR5h plasma membrane by spectrofluorometric assay
Drug: trifluoperazine
Target: Emopamil-binding protein-like (Enzyme)
Gene: EBPL
UniProt: Q9BY08 (EBPL_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.41
Assay: Binding affinity to emopamil binding protein (unknown origin)
Drug: trifluoperazine
Target: Adrenergic receptor alpha-1 (GPCR)
Gene: Adra1b|Adra1d|Adra1a
UniProt: P15823|P23944|P43140 (ADA1B_RAT|ADA1D_RAT|ADA1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.53
Assay: The compound was tested for its binding affinity towards Alpha-1 adrenergic receptor by displacing [3H]WB-4101 radioligand in rat cerebral cortex
Drug: trifluoperazine
Target: Sodium channel alpha subunits; brain (Types I, II, III) (Ion channel)
Gene: SCN1A|SCN2A|SCN3A
UniProt: P35498|Q99250|Q9NY46 (SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.3
Assay: Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex
Drug: trifluoperazine
Target: Serotonin 2 (5-HT2) receptor (GPCR)
Gene: Htr2c|Htr2a|Htr2b
UniProt: P08909|P14842|P30994 (5HT2C_RAT|5HT2A_RAT|5HT2B_RAT)
Organism: Rattus norvegicus
Activity: Kd = 8.98
Assay: Compound was tested for its effect on 5-hydroxytryptamine 2 receptor saturation analysis
Drug: trifluoperazine
Target: Calmodulin (Cytosolic other)
Gene: CALM
UniProt: P62157 (CALM_BOVIN)
Organism: Bos taurus
Activity: Kd = 5.47
Assay: Binding affinity to bovine brain CaM by FTPFACE analysis
Drug: trifluperidol
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki  9.699
Drug: trifluperidol
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.08
Assay: Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand
Drug: trifluperidol
Target: 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase (Enzyme)
Gene: EBP
UniProt: Q15125 (EBP_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.78
Assay: Affinity for human EMP expressed in ERG2 deficient strain of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine as radioligand
Drug: trifluperidol
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki  8.456
Drug: trifluperidol
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki  9.456
Drug: trifluperidol
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: Sigmar1
UniProt: Q9R0C9 (SGMR1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.1
Assay: Displacement of [3H](+)-pentazocine from sigma1 receptor in rat liver membrane by liquid scintillation counting
Drug: trifluperidol
Target: C-8 sterol isomerase (Enzyme)
Gene: ERG2
UniProt: P32352 (ERG2_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: Ki = 9.82
Assay: Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand
Drug: triflupromazine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.553
Action type: ANTAGONIST
Drug: triflupromazine
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.8
Assay: 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
Drug: triflupromazine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.398
Drug: triflupromazine
Target: Trypanothione reductase (Enzyme)
Gene: TPR
UniProt: P28593 (TYTR_TRYCR)
Organism: Trypanosoma cruzi
Activity: Ki = 4.52
Assay: Inhibitory activity against recombinant Trypanosoma cruzi (Trypanosoma cruzi) Trypanothione reductase (linear competitive type)
Drug: triflupromazine
Target: Cholinesterase (Enzyme)
Gene: BCHE
UniProt: P81908 (CHLE_HORSE)
Organism: Equus caballus
Activity: IC50 = 5.13
Assay: Inhibition of Equine serum BChE using butyrylthiocholine iodide as a substrate after 20 mins by Ellman's assay
Drug: triflupromazine
Target: Pleiotropic ABC efflux transporter of multiple drugs (Transporter)
Gene: PDR5
UniProt: P33302 (PDR5_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: IC50 = 5.31
Assay: Inhibition of Pdr5p-mediated rhodamine 6G transport in Saccharomyces cerevisiae MKPDR5h plasma membrane by spectrofluorometric assay
Drug: trifluridine
Target: Thymidine kinase (Kinase)
Gene: UL23
UniProt: A3RLP8 (A3RLP8_CHV1)
Organism: Cercopithecine herpesvirus 1
Activity: IC50 = 5.7
Assay: Inhibition of Herpes B virus recombinant thymidine kinase-mediated [3H]TdR phosphorylation
Drug: trifluridine
Target: Thymidylate kinase (Kinase)
Gene: tmk
UniProt: P9WKE1 (KTHY_MYCTU)
Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)
Activity: Ki = 4.01
Assay: Inhibitory activity against thymidine monophosphate kinase (TMPK) in Mycobacterium tuberculosis
Drug: trihexyphenidyl
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.347
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: trihexyphenidyl
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.89
Action type: ANTAGONIST
Assay: Evaluated for its binding affinity at human muscarinic receptor m1 by displacement of [3H]NMS binding using membranes in transfected chinese hamster ovarian cell
Drug: trihexyphenidyl
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.73
Assay: Evaluated for its binding affinity at human muscarinic receptor m2 by displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug: trihexyphenidyl
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.58
Assay: Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug: trihexyphenidyl
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.17
Assay: Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug: trihexyphenidyl
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.99
Assay: Evaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug: trihexyphenidyl
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.611
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: trilostane
Target: 3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 2 (Enzyme)
Gene: HSD3B2
UniProt: P26439 (3BHS2_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Drug: alimemazine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Assay: Mechanism of Action; CHEMBL231; SINGLE PROTEIN
Drug: alimemazine
Target: FAD-linked sulfhydryl oxidase ALR (Enzyme)
Gene: GFER
UniProt: P55789 (ALR_HUMAN)
Organism: Homo sapiens
Activity: AC50 = 5.9
Assay: PUBCHEM_BIOASSAY: HTS-Luminescent assay for inhibitors of ALR by detection of hydrogen peroxide production Measured in Biochemical System Using Plate Reader - 2036-02_Inhibitor_Dose_CherryPick_Activity. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID488787]
Drug: trimetazidine
Target: Carnitine O-palmitoyltransferase 1, muscle isoform (Enzyme)
Gene: Cpt1b
UniProt: Q63704 (CPT1B_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.89
Assay: Inhibition of CPT1A in rat myocardium
Drug: trimethadione
Target: Voltage-dependent T-type calcium channel subunit alpha-1G (Ion channel)
Gene: CACNA1G
UniProt: O43497 (CAC1G_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: trimetaphan
Target: Neuronal acetylcholine receptor subunit alpha-10 (Ion channel)
Gene: CHRNA10
UniProt: Q9GZZ6 (ACH10_HUMAN)
Organism: Homo sapiens
Drug: trimetaphan
Target: Neuronal acetylcholine receptor subunit alpha-7 (Ion channel)
Gene: CHRNA7
UniProt: P36544 (ACHA7_HUMAN)
Organism: Homo sapiens
Drug: trimetaphan
Target: Acetylcholine receptor subunit alpha (Ion channel)
Gene: CHRNA1
UniProt: P02710 (ACHA_TORCA)
Organism: Torpedo californica
Activity: IC50 = 5.15
Assay: Displacement of [3H]PCP from nAChR in Torpedo nobiliana electric organs membranes in presence of 100 uM carbachol by scintillation counting method
Drug: trimetaphan
Target: Nicotinic acetylcholine receptor alpha 5 subunit (Ion channel)
Gene: nAChRalpha5
UniProt: A9XFY4 (A9XFY4_MUSDO)
Organism: Musca domestica
Activity: Ki = 5.56
Assay: Displacement of [3H]alpha-bungarotoxin from nAChR in Musca domestica (house fly) head membrane after 60 min by scintillation counting
Drug: trimetaphan
Target: Neuronal acetylcholine receptor; alpha3/beta4 (Ion channel)
Gene: CHRNB4|CHRNA3
UniProt: P30926|P32297 (ACHB4_HUMAN|ACHA3_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Drug: trimethoprim
Target: Dihydrofolate reductase (Enzyme)
Gene: DHFR
UniProt: P00374 (DYR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8
Assay: Inhibition of recombinant Dihydrofolate reductase from humans.
Drug: trimethoprim
Target: Bifunctional dihydrofolate reductase-thymidylate synthase (Enzyme)
UniProt: Q07422 (DRTS_TOXGO)
Organism: Toxoplasma gondii
Activity: IC50 = 8.14
Assay: Inhibitory activity against recombinant Dihydrofolate reductase from Toxoplasma gondii (tgDHFR)
Drug: trimethoprim
Target: Dihydrofolate reductase (Enzyme)
UniProt: P16184 (DYR_PNECA)
Organism: Pneumocystis carinii
Activity: Ki = 6.82
Assay: Inhibition of dihydrofolate reductase (DHFR) from Pneumocystis carinii.
Drug: trimethoprim
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.25
Assay: Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Drug: trimethoprim
Target: Bifunctional dihydrofolate reductase-thymidylate synthase (Enzyme)
UniProt: Q27713 (DRTS_PLABA)
Organism: Plasmodium berghei (strain Anka)
Activity: IC50 = 6.92
Assay: In vitro inhibition of dihydrofolate reductase of Plasmodium berghei
Drug: trimethoprim
Target: Bifunctional dihydrofolate reductase-thymidylate synthase (Enzyme)
UniProt: P13922 (DRTS_PLAFK)
Organism: Plasmodium falciparum
Activity: Ki = 7.99
Assay: Inhibitory activity against wild-type dihydrofolate reductase (S108N DHFR)
Drug: trimethoprim
Target: Dihydrofolate reductase (Enzyme)
Gene: Dhfr
UniProt: P00375 (DYR_MOUSE)
Organism: Mus musculus
Activity: Ki = 6.3
Assay: Competitive inhibition of mouse DHFR by enzyme kinetics assay in presence of variable DHFA level
Drug: trimethoprim
Target: Dihydrofolate reductase (Enzyme)
Gene: Dhfr
UniProt: Q920D2 (DYR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.84
Assay: Inhibition of rat liver DHFR by enzyme kinetics assay in presence of variable DHFA level
Drug: trimethoprim
Target: Dihydrofolate reductase (Enzyme)
Gene: folA
UniProt: P0ABQ4 (DYR_ECOLI)
Organism: Escherichia coli (strain K12)
Activity: IC50 = 5.57
Action type: INHIBITOR
Assay: Inhibition of dihydrofolate reductase from Toxoplasma gondii.
Drug: trimethoprim
Target: Dihydrofolate reductase (Enzyme)
Gene: folA
UniProt: P00381 (DYR_LACCA)
Organism: Lactobacillus casei
Activity: Ki = 6.88
Assay: Inhibitory activity against Lactobacillus casei dihydrofolate reductase
Drug: trimethoprim
Target: Dihydrofolate reductase (Enzyme)
Gene: DFR1
UniProt: P07807 (DYR_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: IC50 = 4.92
Assay: Inhibitory activity against Pneumocystis carinii dihydrofolate reductase.
Drug: trimethoprim
Target: Bifunctional dihydrofolate reductase-thymidylate synthase (Enzyme)
UniProt: P07382 (DRTS_LEIMA)
Organism: Leishmania major
Activity: Ki = 6.921
Drug: trimethoprim
Target: Dihydrofolate reductase (Enzyme)
Gene: DFR1
UniProt: P22906 (DYR_CANAX)
Organism: Candida albicans
Activity: IC50 = 8.66
Assay: Inhibitory activity against cell free dihydrofolate reductase (DHFR) from Escherichia coli
Drug: trimethoprim
Target: Dihydrofolate reductase (Enzyme)
Gene: folA
UniProt: O30463 (O30463_MYCAV)
Organism: Mycobacterium avium
Activity: IC50 = 6.72
Assay: Inhibitory activity against DHFR (Dihydrofolate reductase) from Mycobacterium avium
Drug: trimethoprim
Target: Dihydrofolate reductase (Enzyme)
Gene: dfrA17
UniProt: B0BL08 (B0BL08_ECOLX)
Organism: Escherichia coli
Activity: Ki = 8.89
Assay: Binding affinity for Escherichia coli Dihydrofolate reductase
Drug: trimethoprim
Target: Bifunctional dihydrofolate reductase-thymidylate synthase (Enzyme)
UniProt: Q27793 (DRTS_TRYCR)
Organism: Trypanosoma cruzi
Activity: Ki = 6
Drug: trimethoprim
Target: Dihydrofolate reductase (Enzyme)
Gene: folA
UniProt: P0A017 (DYR_STAAU)
Organism: Staphylococcus aureus
Activity: Ki = 8.92
Assay: Inhibition of Staphylococcus aureus DHFR using dihydrofolate as substrate preincubated for 10 mins followed by substrate addition by spectrophotometric analysis in presence of NADPH
Drug: trimethoprim
Target: Bifunctional dihydrofolate reductase-thymidylate synthase (Enzyme)
UniProt: Q27783 (DRTS_TRYBB)
Organism: Trypanosoma brucei brucei
Activity: Ki = 8
Drug: trimethoprim
Target: Dihydrofolate reductase (Enzyme)
Gene: folA
UniProt: P04174 (DYR_NEIGO)
Organism: Neisseria gonorrhoeae
Activity: IC50 = 6.35
Assay: Inhibitory activity against dihydrofolate reductase (DHFR) of Neisseria gonorrhoea
Drug: trimethoprim
Target: Dihydrofolate reductase (Enzyme)
Gene: folA
UniProt: Q59487 (DYR_LACLA)
Organism: Lactococcus lactis subsp. lactis (strain IL1403)
Activity: IC50 = 6.35
Assay: In vitro inhibition of dihydrofolate reductase enzymes in Neisseria gonorrhoeae
Drug: trimethoprim
Target: Dihydrofolate reductase (Enzyme)
Gene: dfrA
UniProt: Q81R22 (Q81R22_BACAN)
Organism: Bacillus anthracis
Activity: Ki = 4.62
Assay: Inhibition of wild type Bacillus anthracis recombinant DHFR
Drug: trimethoprim
Target: Bifunctional dihydrofolate reductase-thymidylate synthase (Enzyme)
Gene: DHFR-TS
UniProt: Q27552 (Q27552_CRYPV)
Organism: Cryptosporidium parvum
Activity: IC50 = 5.4
Assay: Inhibition of Cryptosporidium parvum recombinant DHFR using dihydrofolate as substrate incubated for 5 min prior to substrate addition by spectrophotometric assay
Drug: trimethoprim
Target: Dihydrofolate reductase type 1 (Enzyme)
Gene: dhfrI
UniProt: P00382 (DYR1_ECOLX)
Organism: Escherichia coli
Activity: IC50 = 6.3
Assay: Inhibitory activity to dihydrofolate reductase in Escherichia coli
Drug: trimethoprim
Target: Dihydrofolate reductase (Enzyme)
Gene: folA
UniProt: Q8Z9J9 (Q8Z9J9_SALTI)
Organism: Salmonella typhi
Activity: Ki = 8.08
Drug: trimethoprim
Target: Dihydrofolate reductase (Enzyme)
Gene: dhfR
UniProt: Q54801 (DYR_STRPN)
Organism: Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4)
Activity: IC50 = 4.38
Assay: Inhibition of trimethoprim-resistant Streptococcus pneumoniae DHFR I100L mutant
Drug: trimethoprim
Target: Dihydrofolate reductase (Enzyme)
Gene: DHFR
UniProt: Q9UUP5 (Q9UUP5_PNEJI)
Organism: Pneumocystis jirovecii
Activity: IC50 = 7.04
Assay: Inhibition of Pneumocystis jirovecii recombinant DHFR expressed in Escherichia coli Rosetta Gami B (DE3) competent cells using DHFA as substrate and NADPH
Drug: trimetrexate
Target: Dihydrofolate reductase (Enzyme)
Gene: DHFR
UniProt: P00374 (DYR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.85
Assay: Inhibition of human recombinant Dihydrofolate reductase enzyme
Drug: trimetrexate
Target: Folylpolyglutamate synthase, mitochondrial (Enzyme)
Gene: FPGS
UniProt: Q05932 (FOLC_HUMAN)
Organism: Homo sapiens
Drug: trimetrexate
Target: Bifunctional dihydrofolate reductase-thymidylate synthase (Enzyme)
UniProt: Q07422 (DRTS_TOXGO)
Organism: Toxoplasma gondii
Activity: IC50 = 8.29
Assay: Inhibitory activity against Toxoplasma gondii (tg) Dihydrofolate reductase (DHFR)
Drug: trimetrexate
Target: Dihydrofolate reductase (Enzyme)
UniProt: P16184 (DYR_PNECA)
Organism: Pneumocystis carinii
Activity: Ki = 9.15
Action type: INHIBITOR
Assay: Binding affinity was reported with purified recombinant Pneumocystis carinii Dihydrofolate reductase
Drug: trimetrexate
Target: Dihydrofolate reductase (Enzyme)
Gene: Dhfr
UniProt: P00375 (DYR_MOUSE)
Organism: Mus musculus
Activity: Ki = 10.22
Assay: Inhibitory constant for murine Wild-type dihydrofolate reductase (DHFR)
Drug: trimetrexate
Target: Dihydrofolate reductase (Enzyme)
Gene: Dhfr
UniProt: Q920D2 (DYR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.52
Assay: Inhibitory activity against Dihydrofolate reductase from rat liver
Drug: trimetrexate
Target: Dihydrofolate reductase (Enzyme)
Gene: folA
UniProt: P0ABQ4 (DYR_ECOLI)
Organism: Escherichia coli (strain K12)
Activity: IC50 = 8
Assay: Inhibition of dihydrofolate reductase in Toxoplasma gondii.
Drug: trimetrexate
Target: Dihydrofolate reductase (Enzyme)
Gene: folA
UniProt: P00381 (DYR_LACCA)
Organism: Lactobacillus casei
Activity: IC50 = 7.57
Assay: Inhibitory activity against Dihydrofolate reductase from Lactobacillus casei
Drug: trimetrexate
Target: Dihydrofolate reductase (Enzyme)
Gene: DFR1
UniProt: P07807 (DYR_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: IC50 = 7.38
Assay: Inhibitory activity against Pneumocystis carinii dihydrofolate reductase.
Drug: trimetrexate
Target: Dihydrofolate reductase (Enzyme)
Gene: DFR1
UniProt: P22906 (DYR_CANAX)
Organism: Candida albicans
Activity: Ki = 8.72
Assay: Inhibition of Dihydrofolate reductase enzyme from Candida albicans
Drug: trimetrexate
Target: Dihydrofolate reductase (Enzyme)
Gene: folA
UniProt: O30463 (O30463_MYCAV)
Organism: Mycobacterium avium
Activity: IC50 = 8.82
Assay: Inhibitory concentration against Mycobacterium avium dihydrofolate reductase
Drug: trimetrexate
Target: Dihydrofolate reductase (Enzyme)
Gene: dfrA17
UniProt: B0BL08 (B0BL08_ECOLX)
Organism: Escherichia coli
Activity: IC50 = 8.15
Assay: Inhibitory activity against Escherichia coli (ec) Dihydrofolate reductase
Drug: trimetrexate
Target: Bifunctional dihydrofolate reductase-thymidylate synthase (Enzyme)
UniProt: Q27793 (DRTS_TRYCR)
Organism: Trypanosoma cruzi
Activity: Ki = 8.18
Assay: Inhibition of Trypanosoma cruzi DHFR by spectrophotometric assay
Drug: trimipramine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.827
Action type: INHIBITOR
Drug: trimipramine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.61
Action type: INHIBITOR
Drug: trimipramine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.854
Action type: ANTAGONIST
Drug: trimipramine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.423
Action type: INHIBITOR
Drug: trimipramine
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.56
Assay: Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Drug: trioxsalen
Target: Adenosine receptor A2a (GPCR)
Gene: ADORA2A
UniProt: P29274 (AA2AR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.133
Assay: DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA)
Drug: trioxsalen
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.909
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: trioxsalen
Target: Amine oxidase [flavin-containing] A (Enzyme)
Gene: MAOA
UniProt: P21397 (AOFA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.08
Assay: DRUGMATRIX: Monoamine Oxidase MAO-A enzyme inhibition (substrate: Kynuramine)
Drug: triparanol
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.1
Assay: Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand
Drug: triparanol
Target: 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase (Enzyme)
Gene: EBP
UniProt: Q15125 (EBP_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.96
Assay: Affinity for human EMP expressed in ERG2 deficient strain of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine as radioligand
Drug: triparanol
Target: C-8 sterol isomerase (Enzyme)
Gene: ERG2
UniProt: P32352 (ERG2_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: Ki = 8.7
Assay: Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand
Drug: tripelennamine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.4
Action type: ANTAGONIST
Assay: Inhibitory activity against human Histamine H1 receptor
Drug: triprolidine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.9
Action type: ANTAGONIST
Assay: GRAC: human H1 selective antagonist
Drug: triprolidine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P31389 (HRH1_CAVPO)
Organism: Cavia porcellus
Activity: Kd = 9.9
Assay: Potency against histamine H1 receptor on guinea pig ileum
Drug: troglitazone
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: Km = 3.208
Drug: troglitazone
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.078
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)