AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: miconazole
Target: Melanocortin receptor 3 (GPCR)
Gene: MC3R
UniProt: P41968 (MC3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.792
Assay: DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug: miconazole
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.692
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: miconazole
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 5.711
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: miconazole
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.94
Drug: miconazole
Target: Acetylcholinesterase (Enzyme)
Gene: ache
UniProt: O42275 (ACES_ELEEL)
Organism: Electrophorus electricus
Activity: IC50 = 4.67
Assay: Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by modified Ellman assay
Drug: miconazole
Target: Aromatase (Enzyme)
Gene: Cyp19a1
UniProt: P22443 (CP19A_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 6.4
Assay: In vitro inhibition of cytochrome P450 19A1 by rat ovarian microsomes incubated with [3H]androstenedione and NADPH-generating system.
Drug: miconazole
Target: Cholinesterase (Enzyme)
Gene: BCHE
UniProt: P81908 (CHLE_HORSE)
Organism: Equus caballus
Activity: IC50 = 5.17
Assay: Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by modified Ellman assay
Drug: miconazole
Target: Lanosterol 14-alpha demethylase (Enzyme)
Gene: cyp51
UniProt: P9WPP9 (CP51_MYCTU)
Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)
Activity: Kd = 6.7
Assay: Binding affinity to Mycobacterium tuberculosis CYP51
Drug: miconazole
Target: Indoleamine 2,3-dioxygenase 2 (Enzyme)
Gene: Ido2
UniProt: Q8R0V5 (I23O2_MOUSE)
Organism: Mus musculus
Activity: IC50 = 5.17
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: miconazole
Target: Mycocyclosin synthase (Enzyme)
Gene: cyp121
UniProt: P9WPP7 (CP121_MYCTU)
Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)
Activity: Kd = 7.14
Assay: Binding affinity to Mycobacterium tuberculosis H37Rv wild type CYP121 by titration assay
Drug: miconazole
Target: Malate dehydrogenase cytoplasmic  (Enzyme)
Gene: MDH1
UniProt: P40925 (MDHC_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.6
Assay: Inhibition of malate dehydrogenase (MDH)
Drug: miconazole
Target: Indoleamine 2,3-dioxygenase 1 (Enzyme)
Gene: Ido1
UniProt: P28776 (I23O1_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4.75
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: miconazole
Target: Calcium release-activated calcium channel protein 1 (Ion channel)
Gene: ORAI1
UniProt: Q96D31 (CRCM1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.57
Assay: Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction in BAPTA-induced Ca2+ depletion-stimulated SOCE activity preincubated for 15 mins followed by BAPTA addition in presence of extracellular Ca2+ by PBX-based FLIPR assay
Drug: miconazole
Target: Fatty acid hydroperoxide lyase, chloroplastic (Enzyme)
Gene: HPL
UniProt: K4CF70 (HPL_SOLLC)
Organism: Solanum lycopersicum
Activity: IC50 = 4.19
Assay: Inhibition of recombinant Solanum lycopersicum (tomato) fatty acid 13-hydroperoxide lyase using (13S)-HPOT substrate by spectrophotometry
Drug: miconazole
Target: 7-alpha-hydroxycholest-4-en-3-one 12-alpha-hydroxylase (Enzyme)
Gene: CYP8B1
UniProt: Q9UNU6 (CP8B1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.82
Assay: Inhibition of CYP8B1 in human liver microsomes using D7-7alpha-hydroxy-4-cholesten-3-one as substrate preincubated for 20 mins followed by substrate addition in presence of NADPH by UPLC-ESI-MS/MS analysis
Drug: midazolam
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: Km = 6
Drug: midazolam
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: Km = 4.353
Drug: midazolam
Target: Translocator protein (Membrane receptor)
Gene: Tspo
UniProt: P16257 (TSPO_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.7
Assay: Binding affinity against rat benzodiazepine (BZD) receptor
Drug: midazolam
Target: Thyrotropin-releasing hormone receptor (GPCR)
Gene: Trhr
UniProt: Q01717 (TRFR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.49
Action type: ANTAGONIST
Drug: midazolam
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
Activity: Ki = 8.745
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: midazolam
Target: GABA-A receptor alpha-5/beta-3/gamma-2 (Ion channel)
Gene: GABRG2|GABRB3|GABRA5
UniProt: P18507|P28472|P31644 (GBRG2_HUMAN|GBRB3_HUMAN|GBRA5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.125
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: midazolam
Target: GABA-A receptor alpha-1/beta-2/gamma-3 (Ion channel)
Gene: GABRA1|GABRB2|GABRG3
UniProt: P14867|P47870|Q99928 (GBRA1_HUMAN|GBRB2_HUMAN|GBRG3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.75
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: midazolam
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: Ki = 8.7
Assay: Binding affinity to rat benzodiazepine receptor
Drug: midazolam
Target: GABA A receptor alpha-3/beta-2/gamma-2 (Ion channel)
Gene: GABRG2|GABRA3|GABRB2
UniProt: P18507|P34903|P47870 (GBRG2_HUMAN|GBRA3_HUMAN|GBRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.444
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: midazolam
Target: GABA A receptor alpha-3/beta-2/gamma-3 (Ion channel)
Gene: GABRA3|GABRB2|GABRG3
UniProt: P34903|P47870|Q99928 (GBRA3_HUMAN|GBRB2_HUMAN|GBRG3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.613
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: midazolam
Target: GABA A receptor alpha-5/beta-3/gamma-3 (Ion channel)
Gene: GABRB3|GABRA5|GABRG3
UniProt: P28472|P31644|Q99928 (GBRB3_HUMAN|GBRA5_HUMAN|GBRG3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.26
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: midazolam
Target: GABA A receptor alpha-5/beta-2/gamma-2 (Ion channel)
Gene: GABRG2|GABRA5|GABRB2
UniProt: P18507|P31644|P47870 (GBRG2_HUMAN|GBRA5_HUMAN|GBRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.125
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: midazolam
Target: GABA A receptor alpha-5/beta-2/gamma-3 (Ion channel)
Gene: GABRA5|GABRB2|GABRG3
UniProt: P31644|P47870|Q99928 (GBRA5_HUMAN|GBRB2_HUMAN|GBRG3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.26
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: midodrine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Drug: midodrine
Target: Heat shock protein HSP 90-alpha (Cytosolic other)
Gene: HSP90AA1
UniProt: P07900 (HS90A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.699
Drug: mifepristone
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.001
Assay: DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine)
Drug: mifepristone
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.957
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: mifepristone
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.64
Drug: mifepristone
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.918
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: mifepristone
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9
Action type: ANTAGONIST
Drug: mifepristone
Target: Nuclear receptor subfamily 1 group I member 2 (Nuclear hormone receptor)
Gene: NR1I2
UniProt: O75469 (NR1I2_HUMAN)
Organism: Homo sapiens
Activity: EC50 ~ 5
Action type: AGONIST
Drug: mifepristone
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.095
Assay: DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine)
Drug: mifepristone
Target: Mineralocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C2
UniProt: P08235 (MCR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.68
Drug: mifepristone
Target: Estrogen receptor (Nuclear hormone receptor)
Gene: ESR1
UniProt: P03372 (ESR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.3
Assay: Antagonist activity at estrogen receptor by Gal4-DNA binding domain-hormone receptor LBD one-hybrid assay
Drug: mifepristone
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.33
Drug: mifepristone
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.74
Action type: ANTAGONIST
Drug: mifepristone
Target: Estrogen receptor beta (Nuclear hormone receptor)
Gene: ESR2
UniProt: Q92731 (ESR2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.54
Assay: Displacement of [3H]E2 from human ERbeta after 16 hrs by scintillation counting
Drug: mifepristone
Target: Tyrosine-protein kinase Fyn (Kinase)
Gene: FYN
UniProt: P06241 (FYN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.67
Assay: DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: mifepristone
Target: Mitogen-activated protein kinase 14 (Kinase)
Gene: MAPK14
UniProt: Q16539 (MK14_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.081
Assay: DRUGMATRIX: Protein Serine/Threonine Kinase, p38alpha enzyme inhibition (substrate: Myelin Basic Protein)
Drug: mifepristone
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.255
Assay: DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
Drug: mifepristone
Target: Arachidonate 15-lipoxygenase (Enzyme)
Gene: ALOX15
UniProt: P12530 (LOX15_RABIT)
Organism: Oryctolagus cuniculus
Activity: IC50 = 6.256
Assay: DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid)
Drug: mifepristone
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 9.374
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: mifepristone
Target: Glucocorticoid receptor (Transcription factor)
Gene: Nr3c1
UniProt: P06536 (GCR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.85
Assay: Inhibition of [3H]dexamethasone binding to rat glucocorticoid receptor
Drug: mifepristone
Target: Progesterone receptor (Transcription factor)
Gene: Pgr
UniProt: Q63449 (PRGR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.46
Assay: Inhibition of [3H]R5020 binding to cytosolic progesterone receptor (PRc) of rat uterus
Drug: mifepristone
Target: P-glycoprotein 3 (Transporter)
Gene: Abcb1a
UniProt: P21447 (MDR1A_MOUSE)
Organism: Mus musculus
Activity: Kd = 4.7
Assay: Compound was tested for the binding affinity towards recombinant NBD2 C-terminal cytotoxic nucleotide-binding domain of mouse P-Glycoprotein
Drug: mifepristone
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: F1Q298 (F1Q298_CANLF)
Organism: Canis lupus familiaris
Activity: IC50 = 7.7
Assay: Antagonist activity at GR in dog PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 6 hrs by RT-qPCR method
Drug: mifepristone
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: Q9N1U3 (GCR_PIG)
Organism: Sus scrofa
Activity: IC50 = 7.96
Assay: Antagonist activity at GR in mini pig PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 24 hrs by RT-qPCR method
Drug: miglitol
Target: Maltase-glucoamylase, intestinal (Enzyme)
Gene: MGAM
UniProt: O43451 (MGA_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6
Action type: INHIBITOR
Assay: Inhibition of human recombinant N-terminal subunit of maltase-glucoamylase after 60 mins by glucose oxidase assay
Drug: miglitol
Target: Pancreatic alpha-amylase (Enzyme)
Gene: AMY2A
UniProt: P04746 (AMYP_HUMAN)
Organism: Homo sapiens
Drug: miglitol
Target: Glucosylceramidase (Enzyme)
Gene: GBA
UniProt: P04062 (GLCM_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.08
Assay: Inhibition of human lysosomal beta-glucosidase
Drug: miglitol
Target: Lysosomal alpha-glucosidase (Enzyme)
Gene: GAA
UniProt: P10253 (LYAG_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.46
Action type: INHIBITOR
Assay: Inhibition of human lysosomal alpha-glucosidase
Drug: miglitol
Target: Sucrase-isomaltase, intestinal (Enzyme)
Gene: Si
UniProt: P23739 (SUIS_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.96
Assay: Inhibition of rat intestinal brush border membrane sucrase
Drug: miglitol
Target: Lysosomal alpha-glucosidase (Enzyme)
Gene: Gaa
UniProt: Q6P7A9 (LYAG_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.34
Assay: Competitive inhibition of rat intestinal maltase by Lineweaver-Burk plot analysis
Drug: miglitol
Target: Glycogen debranching enzyme (Enzyme)
Gene: AGL
UniProt: P35574 (GDE_RABIT)
Organism: Oryctolagus cuniculus
Activity: IC50 = 6.41
Assay: Inhibition of rabbit muscle amylo-1,6-glucosidase
Drug: miglitol
Target: Sucrase-isomaltase, intestinal (Enzyme)
Gene: SI
UniProt: P14410 (SUIS_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.3
Assay: Inhibition of sucrase by HPLC
Drug: miglitol
Target: Lactase-phlorizin hydrolase (Enzyme)
Gene: LCT
UniProt: P09848 (LPH_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.3
Assay: Inhibition of lactase by HPLC
Drug: miglitol
Target: Beta-galactosidase (Enzyme)
Gene: GLB1
UniProt: Q58D55 (BGAL_BOVIN)
Organism: Bos taurus
Activity: Ki = 4
Drug: miglitol
Target: Alpha-mannosidase (Enzyme)
UniProt: C0HJB3 (MANULL_CANEN)
Organism: Canavalia ensiformis
Activity: IC50 = 4.12
Assay: Inhibition of Canavalia ensiformis alpha-mannosidase using p-nitrophenyl-alpha-D-mannopyranoside as substrate preincubated for 1 hr followed by substrate addition measured after 10 mins by spectrophotometric method
Drug: miglitol
Target: Alpha-glucosidase (Enzyme)
Gene: aglA
UniProt: P56526 (AGLU_ASPNG)
Organism: Aspergillus niger
Activity: IC50 = 4.24
Assay: Inhibition of Aspergillus niger alpha-glucosidase using p-nitrophenyl-alpha-D-glucopyranoside as substrate preincubated for 1 hr followed by substrate addition measured after 10 mins by spectrophotometric method
Drug: miglustat
Target: Maltase-glucoamylase, intestinal (Enzyme)
Gene: MGAM
UniProt: O43451 (MGA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.68
Assay: Inhibition of Glycosidases (maltase) in rat intestinal brush border membranes by D-glucose oxidase-peroxidase method maltase
Drug: miglustat
Target: Ceramide glucosyltransferase (Enzyme)
Gene: UGCG
UniProt: Q16739 (CEGT_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.13
Action type: INHIBITOR
Drug: miglustat
Target: Lysosomal alpha-glucosidase (Enzyme)
Gene: GAA
UniProt: P10253 (LYAG_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7
Assay: Inhibition of human lysosomal alpha glucosidase
Drug: miglustat
Target: Sucrase-isomaltase, intestinal (Enzyme)
Gene: Si
UniProt: P23739 (SUIS_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.24
Assay: Inhibition of Sucrase in rat intestinal brush border membranes by D-glucose oxidase-peroxidase method
Drug: miglustat
Target: Non-lysosomal glucosylceramidase (Enzyme)
Gene: Gba2
UniProt: Q69ZF3 (GBA2_MOUSE)
Organism: Mus musculus
Activity: IC50 = 6.85
Assay: Inhibition of conduritol beta-epoxide-sensitive mouse glucosylceramidase
Drug: miglustat
Target: Lysosomal alpha-glucosidase (Enzyme)
Gene: Gaa
UniProt: Q6P7A9 (LYAG_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.68
Assay: Inhibition of rat intestinal maltase using moltose as substrate
Drug: miglustat
Target: Non-lysosomal glucosylceramidase (Enzyme)
Gene: GBA2
UniProt: Q9HCG7 (GBA2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.64
Assay: Inhibition of human GBA2
Drug: miglustat
Target: Sucrase-isomaltase, intestinal (Enzyme)
Gene: SI
UniProt: P14410 (SUIS_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.3
Assay: Inhibition of sucrase by HPLC
Drug: miglustat
Target: Glycogen debranching enzyme (Enzyme)
Gene: AGL
UniProt: P35573 (GDE_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5
Assay: Inhibition of glycogen glycogen de-branching enzyme by HPLC
Drug: miglustat
Target: Lysosomal alpha-glucosidase (Enzyme)
Gene: Gaa
UniProt: P70699 (LYAG_MOUSE)
Organism: Mus musculus
Activity: IC50 = 5.05
Assay: Inhibition of maltase in mouse intestinal input by glucose release assay
Drug: miglustat
Target: Sucrase-isomaltase (Enzyme)
Gene: Sis
UniProt: B5THE3 (B5THE3_MOUSE)
Organism: Mus musculus
Activity: IC50 = 6.22
Assay: Inhibition of sucrase in mouse intestinal input by glucose release assay
Drug: miglustat
Target: Putative alpha-glucosidase (Enzyme)
Gene: P0504H10.9
UniProt: Q9LGC6 (Q9LGC6_ORYSJ)
Organism: Oryza sativa subsp. japonica
Activity: IC50 = 6.38
Assay: Inhibitory activity against alpha-Glucosidase from rice
Drug: miglustat
Target: Trehalase (Enzyme)
Gene: Treh
UniProt: O70282 (O70282_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.89
Assay: Inhibition of Glycosidases (trehalase)in rat intestinal brush border membranes by D-glucose oxidase-peroxidase method
Drug: miglustat
Target: Uncharacterized protein (Enzyme)
Gene: TREH
UniProt: I3LIR5 (I3LIR5_PIG)
Organism: Sus scrofa
Activity: IC50 = 4.44
Assay: Inhibition of porcine kidney trehalase
Drug: miglustat
Target: Ceramide glucosyltransferase (Enzyme)
Gene: Ugcg
UniProt: O88693 (CEGT_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4.64
Assay: Inhibition mouse glucosylceramide synthase
Drug: milnacipran
Target: Glutamate receptor ionotropic, NMDA 2A (Ion channel)
Gene: GRIN2A
UniProt: Q12879 (NMDE1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.2
Drug: milnacipran
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.29
Action type: INHIBITOR
Drug: milnacipran
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.6
Action type: INHIBITOR
Drug: milnacipran
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.21
Assay: Inhibition of human DAT
Drug: milnacipran
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: Slc6a4
UniProt: P31652 (SC6A4_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.33
Assay: Displacement of [alpha,beta-3H(N)]-5-hydroxytryptamine from rat synaptosomal SERT expressed in HEK293 cells by microplate scintillation counter
Drug: milnacipran
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: Slc6a3
UniProt: P23977 (SC6A3_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.43
Assay: Displacement of 3,4-[ring-2,5,6-3H]dihydroxyphenylethylamine from rat synaptosomal DAT expressed in HEK293 cells by microplate scintillation counter
Drug: milnacipran
Target: Transporter (Transporter)
Gene: NET
UniProt: Q63380 (Q63380_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.52
Assay: Displacement of Levo[ring-2,5,6-3H]norepinephrine from rat synaptosomal NET expressed in HEK293 cells by microplate scintillation counter
Drug: milrinone
Target: cGMP-inhibited 3',5'-cyclic phosphodiesterase A (Enzyme)
Gene: PDE3A
UniProt: Q14432 (PDE3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.36
Action type: INHIBITOR
Assay: Inhibitory concentration required to inhibit human phosphodiesterase 3A expressed in Escherichia coli
Drug: milrinone
Target: cGMP-specific 3',5'-cyclic phosphodiesterase (Enzyme)
Gene: PDE5A
UniProt: O76074 (PDE5A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.13
Assay: Inhibitory activity against cGMP-phosphodiesterase from porcine aorta
Drug: milrinone
Target: cGMP-inhibited 3',5'-cyclic phosphodiesterase B (Enzyme)
Gene: PDE3B
UniProt: Q13370 (PDE3B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.55
Assay: Inhibitory concentration required to inhibit human phosphodiesterase 3B expressed in Escherichia coli
Drug: milrinone
Target: Cyclic nucleotide phosphodiesterase PDE3A (Enzyme)
UniProt: Q9XSW7 (Q9XSW7_PIG)
Organism: Sus scrofa
Activity: IC50 = 6.07
Assay: Inhibition of phosphodiesterase 3 (PDE3) from porcine platelets, range 0.581-1.23
Drug: milrinone
Target: Cyclic AMP-specific phosphodiesterase SSPDE4A1A (Enzyme)
Gene: PDE4A
UniProt: O77823 (O77823_PIG)
Organism: Sus scrofa
Activity: IC50 = 4.89
Assay: Inhibition of phosphodiesterase 4 (PDE4) from porcine liver, range 10.4-16.3
Drug: milrinone
Target: Uncharacterized protein (Enzyme)
Gene: PDE3B
UniProt: E1BN64 (E1BN64_BOVIN)
Organism: Bos taurus
Activity: IC50 = 6
Assay: Inhibition of bovine arterial Phosphodiesterase 3
Drug: milrinone
Target: cGMP-specific 3',5'-cyclic phosphodiesterase (Enzyme)
Gene: PDE5A
UniProt: Q28156 (PDE5A_BOVIN)
Organism: Bos taurus
Activity: IC50 = 5.3
Assay: Inhibition of bovine arterial Phosphodiesterase 5
Drug: milrinone
Target: cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Enzyme)
Gene: PDE4A
UniProt: O89085 (PDE4A_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 5.33
Assay: Inhibition of Cavia porcellus (guinea pig) PDE3 isolated from heart using [3H]cAMP as substrate by two-step method
Drug: milrinone
Target: Phosphodiesterase 3 (Enzyme)
Gene: PDE3B|PDE3A
UniProt: Q13370|Q14432 (PDE3B_HUMAN|PDE3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.82
Assay: Inhibition of human phosphodiesterase 3
Drug: milrinone
Target: Phosphodiesterase 4 (Enzyme)
Gene: PDE4A|PDE4B|PDE4C|PDE4D
UniProt: P27815|Q07343|Q08493|Q08499 (PDE4A_HUMAN|PDE4B_HUMAN|PDE4C_HUMAN|PDE4D_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.22
Assay: Inhibition of canine cardiac cAMP phosphodiesterase (cAMP-PDE)
Drug: miltefosine
Target: RAC-alpha serine/threonine-protein kinase (Kinase)
Gene: AKT1
UniProt: P31749 (AKT1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.02
Assay: Inhibition of Akt phosphorylation in human insulin-stimulated A549 cells incubated for 2 hrs prior to insulin-induction measured after 30 mins by ELISA
Drug: miltefosine
Target: Dual specificity phosphatase Cdc25A (Enzyme)
Gene: CDC25A
UniProt: P30304 (MPIP1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.6
Assay: Inhibition of Cell division cycle 25 (Cdc25) phosphatase
Drug: mimosine
Target: Serine hydroxymethyltransferase, cytosolic (Enzyme)
Gene: SHMT1
UniProt: P34896 (GLYC_HUMAN)
Organism: Homo sapiens
Drug: mimosine
Target: Tyrosinase (Enzyme)
Gene: TYR
UniProt: P14679 (TYRO_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.43
Drug: mimosine
Target: Ribonucleoside-diphosphate reductase large subunit (Enzyme)
UniProt: P08543 (RIR1_HHV11)
Organism: Human herpesvirus 1 (strain 17)
Activity: IC50 = 4.39
Drug: mimosine
Target: Polyphenol oxidase 2 (Enzyme)
Gene: PPO2
UniProt: O42713 (PPO2_AGABI)
Organism: Agaricus bisporus
Activity: IC50 = 5.43