AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: troglitazone
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.531
Assay: DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
Drug: troglitazone
Target: Carbonic anhydrase 2 (Enzyme)
Gene: CA2
UniProt: P00918 (CAH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.013
Assay: DRUGMATRIX: Carbonic Anhydrase II enzyme inhibition (substrate: 4-Nitrophenyl acetate (4-NPA))
Drug: troglitazone
Target: Bile salt export pump (Transporter)
Gene: ABCB11
UniProt: O95342 (ABCBB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.57
Drug: troglitazone
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.398
Assay: DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: troglitazone
Target: Amine oxidase [flavin-containing] B (Enzyme)
Gene: MAOB
UniProt: P27338 (AOFB_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.02
Assay: Uncompetitive inhibition of human MAOB expressed in Pichia pastoris
Drug: troglitazone
Target: Amine oxidase [flavin-containing] A (Enzyme)
Gene: MAOA
UniProt: P21397 (AOFA_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.98
Assay: Uncompetitive inhibition of human MAOA expressed in Pichia pastoris
Drug: troglitazone
Target: Aldose reductase (Enzyme)
Gene: AKR1B1
UniProt: P15121 (ALDR_HUMAN)
Organism: Homo sapiens
Drug: troglitazone
Target: Peroxisome proliferator-activated receptor gamma (Nuclear hormone receptor)
Gene: PPARG
UniProt: P37231 (PPARG_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.27
Action type: AGONIST
Drug: troglitazone
Target: Tyrosine-protein phosphatase non-receptor type 1 (Enzyme)
Gene: PTPN1
UniProt: P18031 (PTN1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.26
Assay: Inhibition of PTP1B
Drug: troglitazone
Target: Glycogen [starch] synthase, liver (Enzyme)
Gene: GYS2
UniProt: P54840 (GYS2_HUMAN)
Organism: Homo sapiens
Drug: troglitazone
Target: Thromboxane-A synthase (Enzyme)
Gene: TBXAS1
UniProt: P24557 (THAS_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.528
Assay: DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2)
Drug: troglitazone
Target: Aldose reductase (Enzyme)
Gene: Akr1b1
UniProt: P07943 (ALDR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.691
Assay: DRUGMATRIX: Aldose Reductase enzyme inhibition (substrate: DL-Glyceraldehyde)
Drug: troglitazone
Target: Mitogen-activated protein kinase 1 (Kinase)
Gene: MAPK1
UniProt: P28482 (MK01_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.907
Assay: DRUGMATRIX: Protein Serine/Threonine Kinase, ERK2 enzyme inhibition (substrate: Myelin Basic Protein)
Drug: troglitazone
Target: Amine oxidase [flavin-containing] B (Enzyme)
Gene: Maob
UniProt: P19643 (AOFB_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.96
Assay: Uncompetitive inhibition of rat MAOB expressed in Pichia pastoris
Drug: troglitazone
Target: Amine oxidase [flavin-containing] A (Enzyme)
Gene: Maoa
UniProt: P21396 (AOFA_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.32
Assay: Uncompetitive inhibition of rat MAOA expressed in Pichia pastoris
Drug: troglitazone
Target: Indoleamine 2,3-dioxygenase 2 (Enzyme)
Gene: Ido2
UniProt: Q8R0V5 (I23O2_MOUSE)
Organism: Mus musculus
Activity: IC50 = 5.35
Assay: Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
Drug: troglitazone
Target: UDP-glucuronosyltransferase 1-6 (Enzyme)
Gene: UGT1A6
UniProt: P19224 (UD16_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.7
Assay: Inhibition of AZT glucuronidation by human recombinant UGT1A6
Drug: troglitazone
Target: Indoleamine 2,3-dioxygenase 1 (Enzyme)
Gene: Ido1
UniProt: P28776 (I23O1_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4.21
Assay: Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
Drug: troglitazone
Target: Bile salt export pump (Transporter)
Gene: Abcb11
UniProt: O70127 (ABCBB_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.97
Drug: troglitazone
Target: Polyunsaturated fatty acid lipoxygenase ALOX15 (Enzyme)
Gene: Alox15
UniProt: P39654 (LOX15_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4.7
Assay: Inhibition of 15-LOX-mediated lipid oxidation in 10% C57BL/6J mouse plasma
Drug: troleandomycin
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.8
Action type: INHIBITOR
Drug: tropicamide
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.167
Assay: DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: tropicamide
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.432
Assay: DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: tropicamide
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.523
Action type: ANTAGONIST
Assay: DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: tropicamide
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.46
Drug: tropicamide
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.194
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: tropicamide
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Assay: DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: tropicamide
Target: Cytochrome P450 2C19 (Enzyme)
Gene: CYP2C19
UniProt: P33261 (CP2CJ_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Assay: DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: tropisetron
Target: 5-hydroxytryptamine receptor 4 (GPCR)
Gene: HTR4
UniProt: O70528 (5HT4R_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 6.9
Assay: Binding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluated
Drug: tropisetron
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.587
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: tropisetron
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.28
Assay: Inhibition constant against 5-hydroxytryptamine 1A receptor
Drug: tropisetron
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.606
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: tropisetron
Target: 5-hydroxytryptamine receptor 3A (Ion channel)
Gene: HTR3A
UniProt: P46098 (5HT3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.8
Action type: ANTAGONIST
Drug: tropisetron
Target: Glycine receptor subunit alpha-1 (Ion channel)
Gene: GLRA1
UniProt: P23415 (GLRA1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.1
Action type: ANTAGONIST
Drug: tropisetron
Target: Glycine receptor subunit alpha-2 (Ion channel)
Gene: GLRA2
UniProt: P23416 (GLRA2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.9
Action type: ANTAGONIST
Drug: tropisetron
Target: 5-hydroxytryptamine receptor 4 (GPCR)
Gene: HTR4
UniProt: Q13639 (5HT4R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.85
Drug: tropisetron
Target: Neuronal acetylcholine receptor subunit alpha-7 (Ion channel)
Gene: CHRNA7
UniProt: P36544 (ACHA7_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.16
Assay: Inhibition constant against nicotinic acetylcholine receptor alpha7
Drug: tropisetron
Target: Glycine receptor subunit beta (Ion channel)
Gene: GLRB
UniProt: P48167 (GLRB_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.3
Action type: ANTAGONIST
Drug: tropisetron
Target: Neuronal acetylcholine receptor subunit alpha-7 (Ion channel)
Gene: Chrna7
UniProt: Q05941 (ACHA7_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 8
Assay: Activation responses to that evoked by ACh at human Nicotinic acetylcholine receptor alpha-7 expressed in xenopus oocytes
Drug: tropisetron
Target: 5-hydroxytryptamine receptor 4 (GPCR)
Gene: Htr4
UniProt: Q62758 (5HT4R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.2
Assay: Displacement of [3H]GR-113808 from rat striatum 5-hydroxytryptamine 4 receptor
Drug: tropisetron
Target: Neuronal acetylcholine receptor subunit alpha-7 (Ion channel)
Gene: Chrna7
UniProt: P49582 (ACHA7_MOUSE)
Organism: Mus musculus
Activity: Ki = 8.16
Assay: In vitro Binding affinity towards alpha-7 nAChR was determined
Drug: tropisetron
Target: 5-hydroxytryptamine receptor 3A (Ion channel)
Gene: HTR3A
UniProt: O70212 (5HT3A_CAVPO)
Organism: Cavia porcellus
Activity: Kd = 7.52
Assay: Antagonist activity at 5HT3 receptor in spontaneously beating guinea pig right atrium assessed as inhibition of serotonin-induced maximum response by competitive binding assay
Drug: tropisetron
Target: Serotonin 3 (5-HT3) receptor (Ion channel)
Gene: Htr3a|Htr3b
UniProt: P35563|Q9JJ16 (5HT3A_RAT|5HT3B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.89
Assay: Inhibitory activity against 5-hydroxytryptamine 3 receptor in rat cortical membranes using [3H]- 1-Methyl-1H-indazole-3-carboxylic acid (8-methyl-8-aza-bicyclo[3.2.1]oct-3-yl)-amide as a radioligand
Drug: tropisetron
Target: Neuronal acetylcholine receptor; alpha4/beta2 (Ion channel)
Gene: CHRNB2|CHRNA4
UniProt: P17787|P43681 (ACHB2_HUMAN|ACHA4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.26
Assay: In vitro Binding affinity towards Nicotinic acetylcholine receptor alpha4-beta2 was determined
Drug: tropisetron
Target: Acetylcholine receptor; alpha1/beta1/delta/gamma (Ion channel)
Gene: CHRNA1|CHRNG|CHRNB1|CHRND
UniProt: P02708|P07510|P11230|Q07001 (ACHA_HUMAN|ACHG_HUMAN|ACHB_HUMAN|ACHD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.57
Assay: In vitro Binding affinity towards alpha-1-beta-1-gamma-delta nAChR was determined
Drug: tropisetron
Target: Serotonin 3 receptor (5HT3) (Ion channel)
Gene: Htr3a|Htr3b
UniProt: P23979|Q9JHJ5 (5HT3A_MOUSE|5HT3B_MOUSE)
Organism: Mus musculus
Activity: Ki = 8.42
Assay: The binding affinity was measured for 5-hydroxytryptamine 3 receptor on NG 108-15 cell line of mouse neuroblastoma-glioma cells in presence of [3H]5 radioligand (in vitro)
Drug: tropisetron
Target: 5-hydroxytryptamine receptor 3B (Ion channel)
Gene: HTR3B
UniProt: O95264 (5HT3B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.8
Assay: GRAC: human 5-HT3B selective antagonist
Drug: tropisetron
Target: Neuronal acetylcholine receptor subunit alpha-3 (Ion channel)
Gene: CHRNA3
UniProt: P32297 (ACHA3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.8
Assay: In vitro Binding affinity towards alpha-3 (PC12) nAChR was determined
Drug: tropisetron
Target: 5-hydroxytryptamine receptor 4 (GPCR)
Gene: Htr4
UniProt: P97288 (5HT4R_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.1
Action type: ANTAGONIST
Drug: trospium
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Drug: trospium
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Assay: Mechanism of Action; CHEMBL211; SINGLE PROTEIN
Drug: trospium
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Drug: trospium
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Drug: trovafloxacin
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.306
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: trovafloxacin
Target: Thromboxane-A synthase (Enzyme)
Gene: TBXAS1
UniProt: P24557 (THAS_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.395
Assay: DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2)
Drug: trovafloxacin
Target: Topoisomerase IV (Enzyme)
Gene: parC|parE
UniProt: P0AFI2|P20083 (PARC_ECOLI|PARE_ECOLI)
Organism: Escherichia coli (strain K12)
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2363076; PROTEIN COMPLEX
Drug: trovafloxacin
Target: DNA gyrase (Enzyme)
Gene: gyrA|gyrB
UniProt: P0AES4|P0AES6 (GYRA_ECOLI|GYRB_ECOLI)
Organism: Escherichia coli (strain K12)
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2311224; PROTEIN COMPLEX
Drug: tryptophan
Target: Extracellular calcium-sensing receptor (GPCR)
Gene: CASR
UniProt: P41180 (CASR_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.4
Action type: ALLOSTERIC MODULATOR
Drug: tryptophan
Target: Myeloperoxidase (Enzyme)
Gene: MPO
UniProt: P05164 (PERM_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.65
Assay: Inhibition of MPO (unknown origin) using H2O2 as substrate
Drug: tryptophan
Target: Probable G-protein coupled receptor 139 (GPCR)
Gene: GPR139
UniProt: Q6DWJ6 (GP139_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.59
Action type: AGONIST
Assay: Measured using a GTP&gamma;S assay in transfected COS7 cells.
Drug: tubocurarine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.013
Drug: tubocurarine
Target: 5-hydroxytryptamine receptor 3A (Ion channel)
Gene: HTR3A
UniProt: P46098 (5HT3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.06
Drug: tubocurarine
Target: Neuronal acetylcholine receptor subunit alpha-7 (Ion channel)
Gene: CHRNA7
UniProt: P36544 (ACHA7_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.51
Assay: GRAC: human AChR-alpha7 commonly used antagonist
Drug: tubocurarine
Target: Small conductance calcium-activated potassium channel protein 3 (Ion channel)
Gene: KCNN3
UniProt: Q9UGI6 (KCNN3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.5
Action type: BLOCKER
Drug: tubocurarine
Target: Small conductance calcium-activated potassium channel protein 2 (Ion channel)
Gene: KCNN2
UniProt: Q9H2S1 (KCNN2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.7
Action type: BLOCKER
Drug: tubocurarine
Target: Neuronal acetylcholine receptor subunit alpha-7 (Ion channel)
Gene: Chrna7
UniProt: Q05941 (ACHA7_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.32
Assay: Binding affinity nicotinic acetylcholine receptor alpha-7 was evaluated by its ability to inhibit [3H]methyllycaconitine ([3H]-MLA) binding to rat brain membranes
Drug: tubocurarine
Target: Small conductance calcium-activated potassium channel protein 3 (Ion channel)
Gene: Kcnn3
UniProt: P70605 (KCNN3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.04
Assay: Displacement of [I125]apamine from Wistar rat recombinant SK3 channel expressed in HEK293 cells
Drug: tubocurarine
Target: Zinc-activated ligand-gated ion channel (Ion channel)
Gene: ZACN
UniProt: Q401N2 (ZACN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.2
Assay: GRAC: human ZAC selective agonist
Drug: tubocurarine
Target: 5-hydroxytryptamine receptor 3A (Ion channel)
Gene: Htr3a
UniProt: P23979 (5HT3A_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.1
Action type: ANTAGONIST
Drug: tubocurarine
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.1
Assay: Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Drug: tubocurarine
Target: Multidrug and toxin extrusion protein 1 (Transporter)
Gene: SLC47A1
UniProt: Q96FL8 (S47A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.03
Assay: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Drug: tubocurarine
Target: Multidrug and toxin extrusion protein 2 (Transporter)
Gene: SLC47A2
UniProt: Q86VL8 (S47A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.26
Assay: Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Drug: tubocurarine
Target: Acetylcholine receptor subunit alpha (Ion channel)
Gene: CHRNA1
UniProt: P02710 (ACHA_TORCA)
Organism: Torpedo californica
Activity: IC50 = 5.22
Assay: Displacement of [3H]PCP from nAChR in Torpedo nobiliana electric organs membranes in presence of 100 uM carbachol by scintillation counting method
Drug: tubocurarine
Target: Nicotinic acetylcholine receptor alpha 5 subunit (Ion channel)
Gene: nAChRalpha5
UniProt: A9XFY4 (A9XFY4_MUSDO)
Organism: Musca domestica
Activity: Ki = 5.73
Assay: Displacement of [3H]alpha-bungarotoxin from nAChR in Musca domestica (house fly) head membrane after 60 min by scintillation counting
Drug: tubocurarine
Target: Neuronal acetylcholine receptor; alpha4/beta2 (Ion channel)
Gene: Chrna4|Chrnb2
UniProt: P09483|P12390 (ACHA4_RAT|ACHB2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.01
Assay: Binding affinity for nicotinic acetylcholine receptor alpha4-beta2 was evaluated by its ability to inhibit [3H]NIC binding to rat brain membranes
Drug: tubocurarine
Target: Acetylcholine receptor (Ion channel)
Gene: CHRNA1|CHRNB1|CHRND
UniProt: P02708|P11230|Q07001 (ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.62
Action type: ANTAGONIST
Drug: tubocurarine
Target: Neuronal acetylcholine receptor; alpha2/beta2 (Ion channel)
Gene: CHRNB2|CHRNA2
UniProt: P17787|Q15822 (ACHB2_HUMAN|ACHA2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.38
Drug: tubocurarine
Target: Neuronal acetylcholine receptor; alpha4/beta2 (Ion channel)
Gene: CHRNB2|CHRNA4
UniProt: P17787|P43681 (ACHB2_HUMAN|ACHA4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.579
Drug: tubocurarine
Target: Neuronal acetylcholine receptor; alpha3/beta4 (Ion channel)
Gene: CHRNB4|CHRNA3
UniProt: P30926|P32297 (ACHB4_HUMAN|ACHA3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.7
Assay: Inhibitory activity against nicotinic acetylcholine receptor alpha3-beta4
Drug: tubocurarine
Target: Neuronal acetylcholine receptor; alpha4/beta4 (Ion channel)
Gene: CHRNB4|CHRNA4
UniProt: P30926|P43681 (ACHB4_HUMAN|ACHA4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.066
Drug: tubocurarine
Target: Acetylcholine receptor; alpha1/beta1/delta/gamma (Ion channel)
Gene: CHRNA1|CHRNG|CHRNB1|CHRND
UniProt: P02708|P07510|P11230|Q07001 (ACHA_HUMAN|ACHG_HUMAN|ACHB_HUMAN|ACHD_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.09
Assay: GRAC: human AChR-alpha1 commonly used antagonist
Drug: tubocurarine
Target: Serotonin 3 receptor (5HT3) (Ion channel)
Gene: HTR3B|HTR3A
UniProt: O95264|P46098 (5HT3B_HUMAN|5HT3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.5
Action type: ANTAGONIST
Drug: tubocurarine
Target: Small conductance calcium-activated potassium channel protein 1 (Ion channel)
Gene: KCNN1
UniProt: Q92952 (KCNN1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.6
Action type: BLOCKER
Drug: tubocurarine
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
Activity: IC50 = 4.24
Assay: Displacement of [3H]GABA from gamma-aminobutyric-acid A (GABA-A) receptor
Drug: tubocurarine
Target: Small conductance calcium-activated potassium channel protein 2 (Ion channel)
Gene: Kcnn2
UniProt: P70604 (KCNN2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.6
Action type: BLOCKER
Drug: tulobuterol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: Q28044 (ADRB2_BOVIN)
Organism: Bos taurus
Activity: Kd = 6.89
Assay: Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug: tulobuterol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action
Drug: tyramine
Target: 5-hydroxytryptamine receptor 3A (Ion channel)
Gene: HTR3A
UniProt: P46098 (5HT3A_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.59
Assay: Activity at SER3 receptor expressed in HEK293 cells assessed as increase in calcium by calcium imaging assay
Drug: tyramine
Target: Beta-secretase 1 (Enzyme)
Gene: BACE1
UniProt: P56817 (BACE1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 2.7
Assay: Binding affinity to BACE1 by surface plasmon resonance method
Drug: tyramine
Target: Trace amine-associated receptor 1 (GPCR)
Gene: Taar1
UniProt: Q923Y9 (TAAR1_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 7.2
Action type: AGONIST
Drug: tyramine
Target: Trace amine-associated receptor 1 (GPCR)
Gene: Taar1
UniProt: Q923Y8 (TAAR1_MOUSE)
Organism: Mus musculus
Activity: EC50 = 7.1
Action type: AGONIST
Drug: tyramine
Target: TyR1 (GPCR)
UniProt: H9TVJ1 (H9TVJ1_9NEOP)
Organism: Chilo suppressalis
Activity: EC50 = 6.43
Assay: Agonist activity at Chilo suppressalis (rice stem borer) tyramine receptor TyR1 expressed in HEK293 cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 20 min
Drug: tyramine
Target: Serotonin (5-HT) receptor (GPCR)
Gene: Htr2c|Htr2a|Htr1a|Htr1b|Htr1d|Htr1f|Htr2b|Htr6|Htr7|Htr5a|Htr5b|Htr3a|Htr4|Htr3b
UniProt: P08909|P14842|P19327|P28564|P28565|P30940|P30994|P31388|P32305|P35364|P35365|P35563|Q62758|Q9JJ16 (5HT2C_RAT|5HT2A_RAT|5HT1A_RAT|5HT1B_RAT|5HT1D_RAT|5HT1F_RAT|5HT2B_RAT|5HT6R_RAT|5HT7R_RAT|5HT5A_RAT|5HT5B_RAT|5HT3A_RAT|5HT4R_RAT|5HT3B_RAT)
Organism: Rattus norvegicus
Activity: Kd = 5.07
Assay: Affinity against 5-hydroxytryptamine receptors in rat fundus model
Drug: tyramine
Target: Trace amine-associated receptor 1 (GPCR)
Gene: TAAR1
UniProt: Q96RJ0 (TAAR1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.16
Action type: AGONIST
Drug: tyrosine
Target: Large neutral amino acids transporter small subunit 1 (Transporter)
Gene: SLC7A5
UniProt: Q01650 (LAT1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.17
Assay: Cis-inhibition of human LAT1 expressed in TREx HEK293 cells at 200 uM assessed as inhibition of [3H]-gabapentin uptake preincubated for 3 mins at 37 degC followed by washing with choline buffer and measured after 3 hrs by scintillation counting analysis relative to BCH
Drug: ubenimex
Target: 72 kDa type IV collagenase (Enzyme)
Gene: MMP2
UniProt: P08253 (MMP2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.47
Assay: Inhibition of MMP2 after 30 mins
Drug: ubenimex
Target: Aminopeptidase N (Enzyme)
Gene: ANPEP
UniProt: P15144 (AMPN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.62
Assay: Inhibition of aminopeptidase N
Drug: ubenimex
Target: Cytosol aminopeptidase (Enzyme)
Gene: LAP3
UniProt: P28838 (AMPL_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.22
Assay: Binding affinity for cytosolic leucine aminopeptidase (LAP) from porcine kidney
Drug: ubenimex
Target: Leukotriene A-4 hydrolase (Enzyme)
Gene: LTA4H
UniProt: P09960 (LKHA4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.3
Assay: Inhibition of aminopeptidase activity of human leukotriene A4 hydrolase by Dixon plot analysis
Drug: ubenimex
Target: Aminopeptidase N (Enzyme)
Gene: ANPEP
UniProt: P15145 (AMPN_PIG)
Organism: Sus scrofa
Activity: Ki = 9.3
Assay: Competitive inhibition of pig APN using L-leucine-p-nitroanilide as substrate by Dixon-plot analysis
Drug: ubenimex
Target: M1 family aminopeptidase (Enzyme)
UniProt: O96935 (AMP1_PLAFQ)
Organism: Plasmodium falciparum (isolate FcB1 / Columbia)
Activity: Ki = 6.72
Assay: Inhibition of Plasmodium falciparum recombinant M1-aminopeptidase expressed in Escherichia coli after 40 mins uisng fluorogenic substrate L-Leucyl-7-amido-40-methylcoumarin by fluorescence spectrophotometry