AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: mianserin
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 10.15
Assay: Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug: mianserin
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P31389 (HRH1_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 9.07
Drug: mianserin
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.08
Assay: Binding affinity towards Dopamine receptor D2 at 1.0 uM concentration
Drug: mianserin
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: Slc6a4
UniProt: P31652 (SC6A4_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.54
Assay: The binding affinity at the 5-HT reuptake sites determined using competition binding assay
Drug: mianserin
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: Htr2a
UniProt: P14842 (5HT2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.82
Assay: The binding affinity at 5-hydroxytryptamine 2A receptor was determined using [3H]ketanserin
Drug: mianserin
Target: Transporter (Transporter)
Gene: Slc6a2
UniProt: Q9WTR4 (Q9WTR4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.59
Assay: Inhibition of uptake of tritiated norepinephrine (NE) in rat synaptosomes
Drug: mianserin
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32305 (5HT7R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.2
Assay: Binding affinity towards 5-hydroxytryptamine 7 receptor
Drug: mianserin
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32304 (5HT7R_MOUSE)
Organism: Mus musculus
Activity: Ki = 7
Action type: ANTAGONIST
Drug: mianserin
Target: D(1A) dopamine receptor (GPCR)
Gene: Drd1
UniProt: P18901 (DRD1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.85
Assay: Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
Drug: mianserin
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: Htr2c
UniProt: P08909 (5HT2C_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.85
Assay: The binding affinity at 5-hydroxytryptamine 2C receptor was determined using [3H]mesulergine
Drug: mianserin
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P18130 (ADA1A_BOVIN)
Organism: Bos taurus
Activity: Ki = 7.37
Assay: Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
Drug: mianserin
Target: D(3) dopamine receptor (GPCR)
Gene: Drd3
UniProt: P19020 (DRD3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.82
Assay: Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells.
Drug: mianserin
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: Q28838 (ADA2A_BOVIN)
Organism: Bos taurus
Activity: Ki = 7.77
Assay: Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
Drug: mianserin
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: Chrm5
UniProt: P08911 (ACM5_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.72
Assay: Binding affinity towards muscarinic acetylcholine receptor by inhibiting specific binding of [3H]quinuclidinyl benzilate (0.8 nM) in vitro to membranes of rat brain without cerebellum
Drug: mianserin
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: Htr6
UniProt: P31388 (5HT6R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.4
Action type: ANTAGONIST
Drug: mianserin
Target: Serotonin 3 (5-HT3) receptor (Ion channel)
Gene: Htr3a|Htr3b
UniProt: P35563|Q9JJ16 (5HT3A_RAT|5HT3B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.15
Assay: The binding affinity at 5-hydroxytryptamine 3 receptor was determined using [3H]LY-278584
Drug: mianserin
Target: Serotonin 1 (5-HT1) receptor (GPCR)
Gene: Htr1a|Htr1b|Htr1d|Htr1f
UniProt: P19327|P28564|P28565|P30940 (5HT1A_RAT|5HT1B_RAT|5HT1D_RAT|5HT1F_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.24
Assay: Binding affinity towards serotonin S1 receptor at 1.0 uM concentration
Drug: mianserin
Target: Adrenergic receptor alpha-2 (GPCR)
Gene: Adra2b|Adra2c|Adra2a
UniProt: P19328|P22086|P22909 (ADA2B_RAT|ADA2C_RAT|ADA2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.21
Assay: Binding affinity towards alpha-2 adrenergic receptor at 1.0 uM concentration
Drug: mianserin
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 = 5.26
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: mianserin
Target: Cerebral cortex alpha adrenergic receptor (GPCR)
Gene: ADRA1A|ADRA2A
UniProt: P18130|Q28838 (ADA1A_BOVIN|ADA2A_BOVIN)
Organism: Bos taurus
Activity: IC50 = 8.22
Assay: In vitro binding affinity towards alpha-adrenoceptor of calf cortex membrane Site B using [3H]-clonidine
Drug: mianserin
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: Ki = 8.96
Assay: Binding affinity towards 5-hydroxytryptamine 2 receptor at 1.0 uM concentration
Drug: mianserin
Target: Serotonin 3 receptor (5HT3) (Ion channel)
Gene: Htr3a|Htr3b
UniProt: P23979|Q9JHJ5 (5HT3A_MOUSE|5HT3B_MOUSE)
Organism: Mus musculus
Activity: Ki = 6.6
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: mianserin
Target: G-protein coupled receptor (GPCR)
Gene: tyr1
UniProt: Q9NG02 (Q9NG02_APIME)
Organism: Apis mellifera
Activity: IC50 = 4.14
Assay: Antagonist activity at Apis mellifera tyramine receptor TyR1
Drug: mianserin
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28334 (5HT1B_MOUSE)
Organism: Mus musculus
Activity: Ki = 8.3
Action type: ANTAGONIST
Drug: mibefradil
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.3
Assay: Inhibition of human heart Nav1.5 expressed in HEK293 cells by whole cell voltage clamp method
Drug: mibefradil
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.72
Assay: Binding affinity at hERG expressed in HEK293 cells by fluorescence polarization assay
Drug: mibefradil
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.22
Drug: mibefradil
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.8
Drug: mibefradil
Target: Sodium channel protein type 9 subunit alpha (Ion channel)
Gene: SCN9A
UniProt: Q15858 (SCN9A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.3
Assay: Inhibition of human Nav1.7 expressed in HEK293 cells by whole cell voltage clamp method
Drug: mibefradil
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: CACNA1C
UniProt: Q13936 (CAC1C_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.9
Action type: BLOCKER
Drug: mibefradil
Target: Voltage-dependent T-type calcium channel subunit alpha-1G (Ion channel)
Gene: CACNA1G
UniProt: O43497 (CAC1G_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.7
Assay: Inhibition of human Cav3.1 alpha1G expressed in HEK293 cells assessed as inhibition of calcium influx by FLIPR assay
Drug: mibefradil
Target: Voltage-dependent T-type calcium channel subunit alpha-1I (Ion channel)
Gene: CACNA1I
UniProt: Q9P0X4 (CAC1I_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.9
Assay: Inhibition of T-type calcium channel alpha1I by FLIPR
Drug: mibefradil
Target: Potassium channel subfamily K member 9 (Ion channel)
Gene: KCNK9
UniProt: Q9NPC2 (KCNK9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.61
Assay: Inhibition of human TASK3 expressed in HEK293 cells by Ti+ flux assay
Drug: mibefradil
Target: Voltage-dependent N-type calcium channel subunit alpha-1B (Ion channel)
Gene: CACNA1B
UniProt: Q00975 (CAC1B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.87
Assay: Inhibition of N-type calcium channel Alpha-1B
Drug: mibefradil
Target: Sodium channel protein type 2 subunit alpha (Ion channel)
Gene: Scn2a
UniProt: P04775 (SCN2A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.3
Assay: Inhibition of rat brain Nav1.2 expressed in HEK293 cells by whole cell voltage clamp method
Drug: mibefradil
Target: Cation channel sperm-associated protein 1 (Ion channel)
Gene: CATSPER1
UniProt: Q8NEC5 (CTSR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.5
Action type: BLOCKER
Assay: Patch clamp electrophysiology, kinetic rapid mixing fluometry
Drug: mibefradil
Target: Cation channel sperm-associated protein 2 (Ion channel)
Gene: CATSPER2
UniProt: Q96P56 (CTSR2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.5
Action type: BLOCKER
Assay: Patch clamp electrophysiology and kinetic rapid mixing fluometry.
Drug: mibefradil
Target: Cation channel sperm-associated protein 3 (Ion channel)
Gene: CATSPER3
UniProt: Q86XQ3 (CTSR3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.5
Action type: BLOCKER
Assay: Patch clamp electrophysiology, kinetic rapid mixing fluometry.
Drug: mibefradil
Target: Cation channel sperm-associated protein 4 (Ion channel)
Gene: CATSPER4
UniProt: Q7RTX7 (CTSR4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.5
Action type: BLOCKER
Assay: Patch clamp electrophysiology, kinetic rapid mixing fluometry.
Drug: mibefradil
Target: Voltage-dependent R-type calcium channel subunit alpha-1E (Ion channel)
Gene: Cacna1e
UniProt: Q07652 (CAC1E_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.4
Action type: GATING INHIBITOR
Drug: mibefradil
Target: Voltage-dependent P/Q-type calcium channel subunit alpha-1A (Ion channel)
Gene: Cacna1a
UniProt: P54282 (CAC1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.5
Action type: GATING INHIBITOR
Drug: mibefradil
Target: Calcium release-activated calcium channel protein 1 (Ion channel)
Gene: ORAI1
UniProt: Q96D31 (CRCM1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.28
Assay: Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction of SERCA inhibition-induced ER release preincubated for 15 mins followed by CPA addition by PBX-based FLIPR assay
Drug: mibefradil
Target: Sodium channel protein type 4 subunit alpha (Ion channel)
Gene: Scn4a
UniProt: P15390 (SCN4A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.3
Assay: Inhibition of rat skeletal muscle Nav1.4 expressed in HEK293 cells by whole cell voltage clamp method
Drug: mibefradil
Target: Voltage-dependent T-type calcium channel subunit alpha-1H (Ion channel)
Gene: CACNA1H
UniProt: O95180 (CAC1H_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.602
Action type: BLOCKER
Drug: micafungin
Target: Beta-1,3-glucan synthase (Unclassified)
Gene: GSC1
UniProt: Q5AIC4 (Q5AIC4_CANAL)
Organism: Candida albicans (strain SC5314 / ATCC MYA-2876)
Drug: micafungin
Target: Beta-1,3-glucan synthase catalytic subunit 1 (Enzyme)
Gene: GSC1
UniProt: O13428 (O13428_CANAX)
Organism: Candida albicans
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2364673; SINGLE PROTEIN
Drug: miconazole
Target: Sodium/potassium-transporting ATPase subunit alpha-2 (Ion channel)
Gene: ATP1A2
UniProt: D2WKD8 (AT1A2_PIG)
Organism: Sus scrofa
Activity: IC50 = 4.715
Assay: DRUGMATRIX: ATPase, Na+/K+ enzyme inhibition (substrate: ATP)
Drug: miconazole
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.137
Assay: DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug: miconazole
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.588
Assay: DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid)
Drug: miconazole
Target: Cannabinoid receptor 1 (GPCR)
Gene: CNR1
UniProt: P21554 (CNR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.78
Assay: DRUGMATRIX: Cannabinoid CB1 radioligand binding (ligand: [3H] SR141716A)
Drug: miconazole
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.609
Assay: DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine)
Drug: miconazole
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.505
Assay: DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug: miconazole
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.38
Assay: DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
Drug: miconazole
Target: Adenosine receptor A2a (GPCR)
Gene: ADORA2A
UniProt: P29274 (AA2AR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.097
Assay: DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA)
Drug: miconazole
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.828
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: miconazole
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Drug: miconazole
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7
Assay: DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin)
Drug: miconazole
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.383
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: miconazole
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.535
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: miconazole
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.183
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
Drug: miconazole
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.952
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: miconazole
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.452
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: miconazole
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.555
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: miconazole
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.296
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: miconazole
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.785
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: miconazole
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.964
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: miconazole
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.178
Assay: DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug: miconazole
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.02
Assay: DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: miconazole
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.812
Assay: DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: miconazole
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.175
Assay: DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: miconazole
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.351
Assay: DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: miconazole
Target: Beta-3 adrenergic receptor (GPCR)
Gene: ADRB3
UniProt: P13945 (ADRB3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.386
Assay: DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug: miconazole
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.869
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: miconazole
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: miconazole
Target: Adenosine receptor A1 (GPCR)
Gene: ADORA1
UniProt: P30542 (AA1R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.136
Assay: DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX)
Drug: miconazole
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.799
Assay: DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
Drug: miconazole
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.271
Assay: DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug: miconazole
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.825
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: miconazole
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.579
Assay: DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine)
Drug: miconazole
Target: Lanosterol 14-alpha demethylase (Enzyme)
Gene: ERG11
UniProt: P10613 (CP51_CANAL)
Organism: Candida albicans (strain SC5314 / ATCC MYA-2876)
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL1780; SINGLE PROTEIN
Drug: miconazole
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.923
Assay: DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole)
Drug: miconazole
Target: Beta-lactamase (Enzyme)
Gene: ampC
UniProt: P00811 (AMPC_ECOLI)
Organism: Escherichia coli (strain K12)
Activity: IC50 = 4.4
Assay: Compound was tested for the inhibition of beta-lactamase
Drug: miconazole
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P22303 (ACES_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.729
Assay: DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine)
Drug: miconazole
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.699
Assay: DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: miconazole
Target: Aromatase (Enzyme)
Gene: CYP19A1
UniProt: P11511 (CP19A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.22
Assay: Inhibition of human placental microsome CYP19
Drug: miconazole
Target: Epidermal growth factor receptor (Kinase)
Gene: EGFR
UniProt: P00533 (EGFR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.534
Assay: DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: miconazole
Target: Substance-P receptor (GPCR)
Gene: TACR1
UniProt: P25103 (NK1R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.43
Assay: DRUGMATRIX: Tachykinin NK1 radioligand binding (ligand: [3H] Substance P)
Drug: miconazole
Target: Steroid 17-alpha-hydroxylase/17,20 lyase (Enzyme)
Gene: CYP17A1
UniProt: P05093 (CP17A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.61
Assay: In vitro inhibition of human Cytochrome P450 17A1 activity
Drug: miconazole
Target: Cytochrome P450 2C19 (Enzyme)
Gene: CYP2C19
UniProt: P33261 (CP2CJ_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.796
Assay: DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: miconazole
Target: Alkaline phosphatase, tissue-nonspecific isozyme (Enzyme)
Gene: ALPL
UniProt: P05186 (PPBT_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.15
Assay: PUBCHEM_BIOASSAY: uHTS identification of compounds activating TNAP in the absence of phosphate acceptor performed in luminescent assay. (Class of assay: confirmatory) [Related pubchem assays: 813, 518, 1548, 1450 ]
Drug: miconazole
Target: Tyrosine-protein kinase Fyn (Kinase)
Gene: FYN
UniProt: P06241 (FYN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.381
Assay: DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: miconazole
Target: Receptor tyrosine-protein kinase erbB-2 (Kinase)
Gene: ERBB2
UniProt: P04626 (ERBB2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.562
Assay: DRUGMATRIX: Protein Tyrosine Kinase, ERBB2 (HER2) enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: miconazole
Target: Thromboxane-A synthase (Enzyme)
Gene: TBXAS1
UniProt: P24557 (THAS_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.58
Assay: DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2)
Drug: miconazole
Target: Lanosterol 14-alpha demethylase (Enzyme)
Gene: CYP51A1
UniProt: Q16850 (CP51A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.7
Assay: Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay
Drug: miconazole
Target: Indoleamine 2,3-dioxygenase 1 (Enzyme)
Gene: IDO1
UniProt: P14902 (I23O1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.42
Drug: miconazole
Target: Type-2 angiotensin II receptor (GPCR)
Gene: AGTR2
UniProt: P50052 (AGTR2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.109
Assay: DRUGMATRIX: Angiotensin AT2 radioligand binding (ligand: [125I] CGP-42112A)
Drug: miconazole
Target: Substance-K receptor (GPCR)
Gene: TACR2
UniProt: P21452 (NK2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.792
Assay: DRUGMATRIX: Tachykinin NK2  radioligand binding (ligand: [3H] SR-48968)
Drug: miconazole
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.326
Assay: DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
Drug: miconazole
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.029
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug: miconazole
Target: Melanocortin receptor 4 (GPCR)
Gene: MC4R
UniProt: P32245 (MC4R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.922
Assay: DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug: miconazole
Target: Melanocortin receptor 5 (GPCR)
Gene: MC5R
UniProt: P33032 (MC5R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.674
Assay: DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)