AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: tetroxoprim
Target: Dihydrofolate reductase (Enzyme)
Gene: folA
UniProt: Q8Z9J9 (Q8Z9J9_SALTI)
Organism: Salmonella typhi
Activity: Ki = 8.35
Drug: thalidomide
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.301
Drug: thalidomide
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.432
Drug: thalidomide
Target: Tumor necrosis factor (Cytokine)
Gene: TNF
UniProt: P01375 (TNFA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8
Drug: thalidomide
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P05979 (PGH1_SHEEP)
Organism: Ovis aries
Activity: IC50 = 6.43
Assay: Inhibitory activity (RA1) against Prostaglandin G/H synthase 1 was calculated relative to aspirin
Drug: thalidomide
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P79208 (PGH2_SHEEP)
Organism: Ovis aries
Activity: IC50 = 6.3
Assay: Inhibitory activity (RA2) against Prostaglandin G/H synthase 2 was calculated relative to aspirin
Drug: thalidomide
Target: Cereblon isoform 4 (Unclassified)
UniProt: A4TVL0 (A4TVL0_9PROT)
Organism: Magnetospirillum gryphiswaldense
Activity: Ki = 5.36
Assay: Inhibition of MANT-uracil binding to wild type Magnetospirillum gryphiswaldense cereblon isoform 4 by Cheng-Prusoff equation analysis
Drug: thalidomide
Target: Protein cereblon (Cytosolic other)
Gene: CRBN
UniProt: Q96SW2 (CRBN_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.393
Action type: MODULATOR
Assay: competitive titration of thalidomide with human DDB1-human CRBN (50 nM) and Cy5-thalidomide (20 nM)
Drug: theophylline
Target: Adenosine receptor A2a (GPCR)
Gene: ADORA2A
UniProt: P29274 (AA2AR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.22
Action type: ANTAGONIST
Assay: Binding affinity for adenosine A2a receptor by using as [3H]ZM-241385 radioligand in membranes from HEK-A2A cells
Drug: theophylline
Target: cGMP-inhibited 3',5'-cyclic phosphodiesterase A (Enzyme)
Gene: PDE3A
UniProt: Q14432 (PDE3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 3.85
Action type: INHIBITOR
Drug: theophylline
Target: Adenosine receptor A1 (GPCR)
Gene: ADORA1
UniProt: P30542 (AA1R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.22
Action type: ANTAGONIST
Assay: Binding affinity for adenosine A1 receptor by using as [3H]CPX iradioligand n membranes from Chinese hamster ovary cells
Drug: theophylline
Target: Adenosine receptor A2b (GPCR)
Gene: ADORA2B
UniProt: P29275 (AA2BR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.57
Action type: ANTAGONIST
Assay: Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membrane
Drug: theophylline
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.85
Action type: ANTAGONIST
Assay: Binding affinity for adenosine A3 receptor by displacement of specific binding of [125I]AB-MECA in membranes from CHO-A3 cells
Drug: theophylline
Target: cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Enzyme)
Gene: PDE4A
UniProt: P27815 (PDE4A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.11
Action type: INHIBITOR
Drug: theophylline
Target: Alkaline phosphatase, tissue-nonspecific isozyme (Enzyme)
Gene: ALPL
UniProt: P05186 (PPBT_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.09
Assay: Inhibition of TNSALP
Drug: theophylline
Target: Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (Kinase)
Gene: PIK3CD
UniProt: O00329 (PK3CD_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.12
Assay: Inhibition of PI3Kdelta (unknown origin)
Drug: theophylline
Target: Adenosine receptor A1 (GPCR)
Gene: Adora1
UniProt: P25099 (AA1R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.15
Assay: Inhibition of [3H]-CHA binding to rat brain membrane Adenosine A1 receptor
Drug: theophylline
Target: Adenosine receptor A2a (GPCR)
Gene: Adora2a
UniProt: P30543 (AA2AR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.17
Assay: Binding affinity at rat Adenosine A2A receptor by [3H]-CGS- 21680 displacement.
Drug: theophylline
Target: Uncharacterized protein (Enzyme)
Gene: PDE3B
UniProt: E1BN64 (E1BN64_BOVIN)
Organism: Bos taurus
Activity: Ki = 4.11
Assay: Inhibition of bovine heart phosphodiesterase
Drug: theophylline
Target: Adenosine receptor A3 (GPCR)
Gene: Adora3
UniProt: P28647 (AA3R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.07
Assay: Binding affinity to rat adenosine A3 receptor
Drug: theophylline
Target: Adenosine receptor A1 (GPCR)
Gene: ADORA1
UniProt: P28190 (AA1R_BOVIN)
Organism: Bos taurus
Activity: Ki = 5.42
Assay: Binding affinity towards adenosine A1 receptor of bovine brain membrane using [3H]-CHA at 20 uM
Drug: theophylline
Target: Adenosine receptor A1 (GPCR)
Gene: ADORA1
UniProt: P47745 (AA1R_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 5.01
Assay: Affinity against adenosine A1 receptor in the brain membranes by the displacement of [3H]CPX.
Drug: theophylline
Target: Adenosine A2 receptor (GPCR)
Gene: Adora2b|Adora2a
UniProt: P29276|P30543 (AA2BR_RAT|AA2AR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.88
Assay: Binding of Adenosine A2 receptor in whole rat brain membrane using [3H]CHA as a Radioligand
Drug: theophylline
Target: Adenosine A2b receptor (GPCR)
Gene: Adora2b
UniProt: P29276 (AA2BR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.82
Assay: Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
Drug: theophylline
Target: Adenosine receptor (GPCR)
Gene: Adora1|Adora3|Adora2b|Adora2a
UniProt: P25099|P28647|P29276|P30543 (AA1R_RAT|AA3R_RAT|AA2BR_RAT|AA2AR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.7
Assay: Antagonist binding of N6-cyclohexyl-[3H]-adenosine to rat testes
Drug: theophylline
Target: Heart phosphodiesterase (Enzyme)
Gene: PDE3B|PDE1A|PDE1B
UniProt: E1BN64|P14100|Q01061 (E1BN64_BOVIN|PDE1A_BOVIN|PDE1B_BOVIN)
Organism: Bos taurus
Activity: IC50 = 4.04
Assay: Inhibition of bovine heart phosphodiesterase
Drug: theophylline
Target: Adenosine A2a receptor (GPCR)
Gene: ADORA2A
UniProt: P46616 (AA2AR_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 4.89
Assay: Antagonist binding of N6-cyclohexyl-[3H]-adenosine to guinea pig brain
Drug: theophylline
Target: Adenosine receptor A2b (GPCR)
Gene: Adora2b
UniProt: Q60614 (AA2BR_MOUSE)
Organism: Mus musculus
Activity: Ki = 5.25
Action type: ANTAGONIST
Drug: theophylline
Target: Transmembrane domain-containing protein TMIGD3 (Unclassified)
Gene: TMIGD3
UniProt: P0DMS9 (TMIG3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.06
Assay: Displacement of [3H]HEMADO from human A3 adenosine receptor expressed in CHO cells
Drug: thiabendazole
Target: Peptidyl-prolyl cis-trans isomerase FKBP1A (Enzyme)
Gene: FKBP1A
UniProt: P62942 (FKB1A_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.22
Assay: Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
Drug: thiabendazole
Target: Cytochrome P450 1A2 (Enzyme)
Gene: CYP1A2
UniProt: P05177 (CP1A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.097
Assay: DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: thiabendazole
Target: Succinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrial (Enzyme)
Gene: sdha-1
UniProt: Q09508 (SDHA_CAEEL)
Organism: Caenorhabditis elegans
Drug: thiabendazole
Target: Methionine aminopeptidase 2 (Enzyme)
Gene: METAP2
UniProt: P50579 (MAP2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.35
Assay: Inhibition of human MetAP2 expressed in baculovirus infected Sf9 cells
Drug: thiabendazole
Target: Reverse transcriptase/RNaseH (Enzyme)
Gene: pol
UniProt: Q72547 (Q72547_9HIV1)
Organism: Human immunodeficiency virus 1
Activity: IC50 = 4.84
Assay: HIV-1 reverse transcriptase (RT) activity using Poly (rC)/oligo (dG) as template/primer and [3H]dGTP
Drug: thiabendazole
Target: Methionine aminopeptidase (Enzyme)
Gene: map
UniProt: P0AE18 (MAP1_ECOLI)
Organism: Escherichia coli (strain K12)
Activity: IC50 = 6.33
Assay: Inhibition of Co2+ loaded MetAP expressed in Escherichia coli
Drug: thiabendazole
Target: Methionine aminopeptidase 1 (Enzyme)
Gene: METAP1
UniProt: P53582 (MAP11_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.47
Assay: Inhibition of human methionine aminopeptidase 1 in presence of Co2+
Drug: thiabendazole
Target: Tubulin (Structural)
UniProt: C4PKY4|C4PKZ2|C4PKZ6 (C4PKY4_ECHGR|C4PKZ2_ECHGR|C4PKZ6_ECHGR)
Organism: Echinococcus granulosus
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2364704; PROTEIN COMPLEX GROUP
Drug: thiabendazole
Target: Tubulin (Structural)
UniProt: F1L005|F1L4P8|F1L5G6|F1L7U3|F1L7Y0|F1L8A5|F1LCS0 (F1L005_ASCSU|F1L4P8_ASCSU|F1L5G6_ASCSU|F1L7U3_ASCSU|F1L7Y0_ASCSU|F1L8A5_ASCSU|F1LCS0_ASCSU)
Organism: Ascaris suum
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2364705; PROTEIN COMPLEX GROUP
Drug: thiamphenicol
Target: 50S ribosomal protein L10 (Ribosomal protein)
Gene: rpl10
UniProt: P15825 (RL10_HALMA)
Organism: Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
Drug: thiamphenicol
Target: Cytochrome P450 2C19 (Enzyme)
Gene: CYP2C19
UniProt: P33261 (CP2CJ_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.12
Drug: thiamphenicol
Target: Streptokinase A (Enzyme)
Gene: ska
UniProt: P10520 (STRP_STRP1)
Organism: Streptococcus pyogenes serotype M1
Activity: EC50 = 5.77
Drug: thiamylal
Target: GABA-A receptor; anion channel (Ion channel)
Gene: GABRP|GABRD|GABRA1|GABRB1|GABRG2|GABRB3|GABRA5|GABRA3|GABRA2|GABRB2|GABRA4|GABRE|GABRA6|GABRG1|GABRG3|GABRQ
UniProt: O00591|O14764|P14867|P18505|P18507|P28472|P31644|P34903|P47869|P47870|P48169|P78334|Q16445|Q8N1C3|Q99928|Q9UN88 (GBRP_HUMAN|GBRD_HUMAN|GBRA1_HUMAN|GBRB1_HUMAN|GBRG2_HUMAN|GBRB3_HUMAN|GBRA5_HUMAN|GBRA3_HUMAN|GBRA2_HUMAN|GBRB2_HUMAN|GBRA4_HUMAN|GBRE_HUMAN|GBRA6_HUMAN|GBRG1_HUMAN|GBRG3_HUMAN|GBRT_HUMAN)
Organism: Homo sapiens
Action type: POSITIVE ALLOSTERIC MODULATOR
Assay: Mechanism of Action; CHEMBL2093872; PROTEIN COMPLEX GROUP
Drug: thiethylperazine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.301
Drug: thiethylperazine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.699
Action type: ANTAGONIST
Drug: thiethylperazine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.155
Drug: thiethylperazine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.155
Drug: thiethylperazine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7
Drug: thiethylperazine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7
Drug: thiethylperazine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7
Drug: thiethylperazine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.699
Drug: thiethylperazine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.699
Drug: thiethylperazine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.602
Drug: thiethylperazine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Drug: thiethylperazine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Drug: thiethylperazine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Drug: thiethylperazine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Drug: thiethylperazine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Drug: thiethylperazine
Target: Pleiotropic ABC efflux transporter of multiple drugs (Transporter)
Gene: PDR5
UniProt: P33302 (PDR5_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: IC50 = 5.64
Assay: Inhibition of Pdr5p-mediated rhodamine 6G transport in Saccharomyces cerevisiae MKPDR5h plasma membrane by spectrofluorometric assay
Drug: thiethylperazine
Target: FAD-linked sulfhydryl oxidase ALR (Enzyme)
Gene: GFER
UniProt: P55789 (ALR_HUMAN)
Organism: Homo sapiens
Activity: AC50 = 5.96
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: thioguanine
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.221
Assay: DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid)
Drug: thioguanine
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.912
Assay: DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
Drug: thioguanine
Target: Multidrug resistance-associated protein 5 (Transporter)
Gene: ABCC5
UniProt: O15440 (MRP5_HUMAN)
Organism: Homo sapiens
Drug: thioguanine
Target: Multidrug resistance-associated protein 4 (Transporter)
Gene: ABCC4
UniProt: O15439 (MRP4_HUMAN)
Organism: Homo sapiens
Drug: thioguanine
Target: Inosine-5'-monophosphate dehydrogenase 1 (Enzyme)
Gene: IMPDH1
UniProt: P20839 (IMDH1_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Drug: thioguanine
Target: Xanthine dehydrogenase/oxidase (Enzyme)
Gene: XDH
UniProt: P47989 (XDH_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.03
Assay: Inhibition of human xanthine oxidase
Drug: thioguanine
Target: Inosine-5'-monophosphate dehydrogenase 2 (Enzyme)
Gene: IMPDH2
UniProt: P12268 (IMDH2_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Drug: thioguanine
Target: Hypoxanthine-guanine phosphoribosyltransferase (Enzyme)
Gene: HPRT1
UniProt: P00492 (HPRT_HUMAN)
Organism: Homo sapiens
Drug: thioguanine
Target: Mitogen-activated protein kinase 3 (Kinase)
Gene: MAPK3
UniProt: P27361 (MK03_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.258
Assay: DRUGMATRIX: Protein Serine/Threonine Kinase, ERK1 enzyme inhibition (substrate: Myelin Basic Protein)
Drug: thioguanine
Target: Arachidonate 15-lipoxygenase (Enzyme)
Gene: ALOX15
UniProt: P12530 (LOX15_RABIT)
Organism: Oryctolagus cuniculus
Activity: IC50 = 4.792
Assay: DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid)
Drug: thioguanine
Target: 2-amino-4-hydroxy-6-hydroxymethyldihydropteridine pyrophosphokinase (Kinase)
Gene: folK
UniProt: P26281 (HPPK_ECOLI)
Organism: Escherichia coli (strain K12)
Activity: Kd = 4.75
Assay: Binding affinity to GST-tagged Escherichia coli HPPK expressed in Escherichia coli by SPR assay based alternative equilibrium affinity method in presence of AMP-CPP
Drug: thiopental
Target: GABA-A receptor alpha-1/beta-2/gamma-2 (Ion channel)
Gene: GABRA1|GABRG2|GABRB2
UniProt: P14867|P18507|P47870 (GBRA1_HUMAN|GBRG2_HUMAN|GBRB2_HUMAN)
Organism: Homo sapiens
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: thiopental
Target: GABA-A receptor; anion channel (Ion channel)
Gene: Gabrp|Gabrb1|Gabrd|Gabrg2|Gabra5|Gabra3|Gabrg1|Gabra2|Gabra4|Gabrg3|Gabra6|Gabra1|Gabrb3|Gabrb2|Gabrq|Gabre
UniProt: O09028|P15431|P18506|P18508|P19969|P20236|P23574|P23576|P28471|P28473|P30191|P62813|P63079|P63138|Q91ZM7|Q9ES14 (GBRP_RAT|GBRB1_RAT|GBRD_RAT|GBRG2_RAT|GBRA5_RAT|GBRA3_RAT|GBRG1_RAT|GBRA2_RAT|GBRA4_RAT|GBRG3_RAT|GBRA6_RAT|GBRA1_RAT|GBRB3_RAT|GBRB2_RAT|Q91ZM7_RAT|GBRE_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.53
Assay: The concentration required to inhibit 50% of binding of [35S]TBPS to Gamma-aminobutyric acid A receptor to rat whole brain membranes.
Drug: thiopental
Target: Potassium voltage-gated channel subfamily C member 4 (Ion channel)
Gene: Kcnc4
UniProt: Q63734 (KCNC4_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4
Action type: GATING INHIBITOR
Drug: thioproperazine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.347
Drug: thioproperazine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.921
Drug: thioridazine
Target: Nuclear receptor subfamily 1 group I member 3 (Nuclear hormone receptor)
Gene: NR1I3
UniProt: Q14994 (NR1I3_HUMAN)
Organism: Homo sapiens
Drug: thioridazine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.1
Drug: thioridazine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.4
Action type: ANTAGONIST
Drug: thioridazine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.872
Drug: thioridazine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.815
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: thioridazine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7
Drug: thioridazine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.9
Drug: thioridazine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.813
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: thioridazine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.1
Action type: ANTAGONIST
Drug: thioridazine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8
Action type: ANTAGONIST
Drug: thioridazine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.086
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: thioridazine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.3
Action type: ANTAGONIST
Drug: thioridazine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.2
Action type: ANTAGONIST
Drug: thioridazine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.15
Assay: Binding affinity towards human 5-hydroxytryptamine 7 receptor
Drug: thioridazine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.9
Drug: thioridazine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.466
Drug: thioridazine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.3
Action type: ANTAGONIST
Drug: thioridazine
Target: D(1B) dopamine receptor (GPCR)
Gene: DRD5
UniProt: P21918 (DRD5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.6
Action type: ANTAGONIST
Drug: thioridazine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.7
Action type: ANTAGONIST
Drug: thioridazine
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.866
Drug: thioridazine
Target: Histamine H4 receptor (GPCR)
Gene: HRH4
UniProt: Q9H3N8 (HRH4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.62
Drug: thioridazine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.569
Drug: thioridazine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.854
Drug: thioridazine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.595
Drug: thioridazine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.046
Drug: thioridazine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.886
Drug: thioridazine
Target: Aldehyde oxidase (Enzyme)
Gene: AOX1
UniProt: Q06278 (AOXA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.796
Drug: thioridazine
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.963
Drug: thioridazine
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.237
Drug: thioridazine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.126
Drug: thioridazine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.774
Drug: thioridazine
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.751
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: thioridazine
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.979
Action type: ANTAGONIST
Drug: thioridazine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.686
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: thioridazine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.62
Drug: thioridazine
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.002
Assay: DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine)
Drug: thioridazine
Target: 5-hydroxytryptamine receptor 5A (GPCR)
Gene: HTR5A
UniProt: P47898 (5HT5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.439
Drug: thioridazine
Target: Cytochrome P450 1A2 (Enzyme)
Gene: CYP1A2
UniProt: P05177 (CP1A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.03
Assay: DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: thioridazine
Target: 5-hydroxytryptamine receptor 1E (GPCR)
Gene: HTR1E
UniProt: P28566 (5HT1E_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.712
Drug: thioridazine
Target: Epidermal growth factor receptor (Kinase)
Gene: EGFR
UniProt: P00533 (EGFR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.531
Assay: DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: thioridazine
Target: Cytochrome P450 2C19 (Enzyme)
Gene: CYP2C19
UniProt: P33261 (CP2CJ_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.195
Assay: DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: thioridazine
Target: Tyrosine-protein kinase Fyn (Kinase)
Gene: FYN
UniProt: P06241 (FYN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.297
Assay: DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr))