AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: ketanserin
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.7
Action type: ANTAGONIST
Drug: ketanserin
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.62
Assay: Binding affinity for Dopamine receptor D2 by displacement of [3H]-spiperone
Drug: ketanserin
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki
Drug: ketanserin
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9
Assay: The compound was tested for affinity towards sigma-3 receptor
Drug: ketanserin
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.97
Drug: ketanserin
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5
Action type: ANTAGONIST
Drug: ketanserin
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.7
Assay: GRAC: human 5-HT2A selective antagonist
Drug: ketanserin
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.7
Action type: ANTAGONIST
Drug: ketanserin
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.5
Action type: ANTAGONIST
Drug: ketanserin
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.55
Assay: Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
Drug: ketanserin
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.5
Action type: ANTAGONIST
Drug: ketanserin
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.2
Action type: ANTAGONIST
Drug: ketanserin
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.701
Drug: ketanserin
Target: D(1B) dopamine receptor (GPCR)
Gene: DRD5
UniProt: P21918 (DRD5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.6
Action type: ANTAGONIST
Drug: ketanserin
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.747
Drug: ketanserin
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.19
Assay: Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
Drug: ketanserin
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.59
Assay: Binding affinity by displacement to human cloned 5-hydroxytryptamine 1D receptor in CHO cells by [3H]5-HT displacement.
Drug: ketanserin
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.57
Assay: Inhibitory concentration against human Adenosine A3 receptor expressed in HEK293 cells using 0.1 nM [3H]AB-MECA
Drug: ketanserin
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.46
Assay: Binding affinity towards human dopamine receptor D4
Drug: ketanserin
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.8
Action type: ANTAGONIST
Drug: ketanserin
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.2
Action type: ANTAGONIST
Drug: ketanserin
Target: 5-hydroxytryptamine receptor 5A (GPCR)
Gene: HTR5A
UniProt: P47898 (5HT5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.7
Action type: ANTAGONIST
Drug: ketanserin
Target: 5-hydroxytryptamine receptor 1F (GPCR)
Gene: HTR1F
UniProt: P30939 (5HT1F_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.903
Drug: ketanserin
Target: Synaptic vesicular amine transporter (Transporter)
Gene: SLC18A2
UniProt: Q05940 (VMAT2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.155
Drug: ketanserin
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.72
Assay: Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug: ketanserin
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.44
Assay: Inhibitory constant against binding of [125I]- IBZM to rat striatal membrane
Drug: ketanserin
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.74
Assay: Binding affinity towards 5-hydroxytryptamine 1A receptor by the displacement of [125I]trans-8-OH-PIPAT in membrane homogenates of hippocampal tissue of rat brain
Drug: ketanserin
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: Htr2a
UniProt: P14842 (5HT2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.33
Assay: Displacement of [3H]ketanserin from 5-HT2A receptor in Sprague-Dawley rat frontal cortex after 15 mins
Drug: ketanserin
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32305 (5HT7R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.7
Action type: ANTAGONIST
Drug: ketanserin
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32304 (5HT7R_MOUSE)
Organism: Mus musculus
Activity: Ki = 6.4
Action type: ANTAGONIST
Drug: ketanserin
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: Htr2c
UniProt: P08909 (5HT2C_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.3
Assay: Binding affinity against 5-hydroxytryptamine 1C receptor in rat using [3H]mesulergine as radioligand
Drug: ketanserin
Target: Chromaffin granule amine transporter (Transporter)
Gene: SLC18A1
UniProt: P54219 (VMAT1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.8
Action type: INHIBITOR
Drug: ketanserin
Target: Adrenergic receptor alpha-1 (GPCR)
Gene: Adra1b|Adra1d|Adra1a
UniProt: P15823|P23944|P43140 (ADA1B_RAT|ADA1D_RAT|ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.82
Assay: Inhibition of [3H]prazosin binding to alpha-1 adrenergic receptor from rat cortical membranes
Drug: ketanserin
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 = 9.4
Assay: Evaluated for the binding affinity to rat cortical membranes at 5-hydroxytryptamine 2 receptor binding site by using [3H]- KET as a radioligand.
Drug: ketanserin
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28334 (5HT1B_MOUSE)
Organism: Mus musculus
Activity: Ki = 8.3
Action type: ANTAGONIST
Drug: ketanserin
Target: Synaptic vesicular amine transporter (Transporter)
Gene: Slc18a2
UniProt: Q8BRU6 (VMAT2_MOUSE)
Organism: Mus musculus
Activity: IC50 = 7
Assay: Inhibition of VMAT2 in C57Bl/6J mouse striatal membranes assessed as reduction in [3H[-5HT uptake pre-incubated for 10 mins before [3H[-5HT addition and measured after 8 mins
Drug: ketobemidone
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 9
Drug: ketobemidone
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.223
Drug: ketobemidone
Target: Glutamate receptor ionotropic, NMDA 3A (Ion channel)
Gene: GRIN3A
UniProt: Q8TCU5 (NMD3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.585
Drug: ketobemidone
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.845
Drug: ketobemidone
Target: Opioid receptor (GPCR)
Gene: Oprd1|Oprm1|Oprk1|Sigmar1
UniProt: P33533|P33535|P34975|Q9R0C9 (OPRD_RAT|OPRM_RAT|OPRK_RAT|SGMR1_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 8.7
Assay: Displacement of radiolabeled dihydromorphine from opioid receptor in rat brain homogenates
Drug: ketobemidone
Target: Opioid receptor (GPCR)
Gene: Sigmar1|Oprd1|Oprk1|Oprm1
UniProt: O55242|P32300|P33534|P42866 (SGMR1_MOUSE|OPRD_MOUSE|OPRK_MOUSE|OPRM_MOUSE)
Organism: Mus musculus
Activity: IC50 = 5.15
Assay: Tested for displacement of radioligand [3H]-Naloxone from opiate receptor; value ranges from 7-10 uM
Drug: ketoconazole
Target: Sodium/nucleoside cotransporter 1 (Transporter)
Gene: SLC28A1
UniProt: O00337 (S28A1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.821
Assay: DRUGMATRIX: Sodium/nucleoside co-transporter radioligand binding (ligand: nitrobenzylthioinosine)
Drug: ketoconazole
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.13
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: ketoconazole
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.72
Drug: ketoconazole
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7
Drug: ketoconazole
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6
Drug: ketoconazole
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.55
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: ketoconazole
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.62
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: ketoconazole
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.084
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: ketoconazole
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.667
Assay: DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug: ketoconazole
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.028
Assay: DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: ketoconazole
Target: Aldehyde oxidase (Enzyme)
Gene: AOX1
UniProt: Q06278 (AOXA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.456
Drug: ketoconazole
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.729
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: ketoconazole
Target: Nuclear receptor subfamily 1 group I member 2 (Nuclear hormone receptor)
Gene: NR1I2
UniProt: O75469 (NR1I2_HUMAN)
Organism: Homo sapiens
Drug: ketoconazole
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.84
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: ketoconazole
Target: Lanosterol 14-alpha demethylase (Enzyme)
Gene: ERG11
UniProt: P10613 (CP51_CANAL)
Organism: Candida albicans (strain SC5314 / ATCC MYA-2876)
Activity: IC50 = 7
Action type: INHIBITOR
Drug: ketoconazole
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.346
Assay: DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole)
Drug: ketoconazole
Target: Bile salt export pump (Transporter)
Gene: ABCB11
UniProt: O95342 (ABCBB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.54
Assay: Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Drug: ketoconazole
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.4
Assay: Inhibition Assay: Solutions of each test compound were separately prepared at concentrations of 20000, 6000, 2000, 600, 200, and 60 uM by serial dilution with DMSO:MeCN (50:50 v/v). The individual test compound solutions were then diluted 20-fold with DMSO:MeCN:deionized water (5:5:180 v/v/v) to concentrations of 1000, 300, 100, 30, 10, and 3 uM. Mixtures of isozyme inhibitors (sulfaphenazole, tranylcypromine, and ketoconazole as specific inhibitors of isozymes 2C9, 2C19, and 3A4, respectively) were prepared containing each inhibitor at concentrations of 6000, 2000, 600, 200, 60, 20, 6, and 2 uM by serial dilution with DMSO:ACN (50:50 v/v). The mixed inhibitor solutions were then diluted 20-fold with DMSO:MeCN:deionized water (5:5:180 v/v/v) to concentrations of 300, 100, 30, 10, 3, 1, 0.3, and 0.1 uM. The percent of organic solvent attributable to the test compound or inhibitor mixture in the final reaction mixture was 2% v/v.Pooled human liver microsome suspension (20 mg/mL
Drug: ketoconazole
Target: Aromatase (Enzyme)
Gene: CYP19A1
UniProt: P11511 (CP19A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.4
Assay: Inhibition of human recombinant aromatase assessed as conversion of O-dibenzylfluorescein benzyl ester substrate to fluorescein byproduct by fluorometric assay
Drug: ketoconazole
Target: 25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial (Enzyme)
Gene: CYP27B1
UniProt: O15528 (CP27B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.47
Assay: Inhibition of human CYP27B1 expressed in Escherichia coli assessed as reduction in hydrolase activity incubated for 25 mins using Adx, AdR and 1,25(OH)2D3
Drug: ketoconazole
Target: Potassium voltage-gated channel subfamily A member 10 (Ion channel)
Gene: KCNA10
UniProt: Q16322 (KCA10_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.3
Action type: BLOCKER
Drug: ketoconazole
Target: Cytochrome P450 2C19 (Enzyme)
Gene: CYP2C19
UniProt: P33261 (CP2CJ_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.72
Assay: Inhibition Assay: Solutions of each test compound were separately prepared at concentrations of 20000, 6000, 2000, 600, 200, and 60 uM by serial dilution with DMSO:MeCN (50:50 v/v). The individual test compound solutions were then diluted 20-fold with DMSO:MeCN:deionized water (5:5:180 v/v/v) to concentrations of 1000, 300, 100, 30, 10, and 3 uM. Mixtures of isozyme inhibitors (sulfaphenazole, tranylcypromine, and ketoconazole as specific inhibitors of isozymes 2C9, 2C19, and 3A4, respectively) were prepared containing each inhibitor at concentrations of 6000, 2000, 600, 200, 60, 20, 6, and 2 uM by serial dilution with DMSO:ACN (50:50 v/v). The mixed inhibitor solutions were then diluted 20-fold with DMSO:MeCN:deionized water (5:5:180 v/v/v) to concentrations of 300, 100, 30, 10, 3, 1, 0.3, and 0.1 uM. The percent of organic solvent attributable to the test compound or inhibitor mixture in the final reaction mixture was 2% v/v.Pooled human liver microsome suspension (20 mg/mL
Drug: ketoconazole
Target: Thromboxane-A synthase (Enzyme)
Gene: TBXAS1
UniProt: P24557 (THAS_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.665
Assay: DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2)
Drug: ketoconazole
Target: Lanosterol 14-alpha demethylase (Enzyme)
Gene: CYP51A1
UniProt: Q16850 (CP51A_HUMAN)
Organism: Homo sapiens
Activity: app Ki = 7.197
Drug: ketoconazole
Target: Indoleamine 2,3-dioxygenase 1 (Enzyme)
Gene: IDO1
UniProt: P14902 (I23O1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.6
Drug: ketoconazole
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.58
Assay: Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
Drug: ketoconazole
Target: Substance-K receptor (GPCR)
Gene: TACR2
UniProt: P21452 (NK2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.24
Assay: DRUGMATRIX: Tachykinin NK2  radioligand binding (ligand: [3H] SR-48968)
Drug: ketoconazole
Target: Cytochrome P450 3A5 (Enzyme)
Gene: CYP3A5
UniProt: P20815 (CP3A5_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.92
Assay: Fluorescent High Throughput P450 Assay: The interaction of SC12 with cytochrome P450 enzymes was tested using Fluorescent High Throughput P450 assays (Gentest) The IC50s of the compounds was calculated on isoenzymes (CYP1A2, CYP2C9, CYP2C19, CYP2C8, CYP2B6, CYP2D6, CYP2E1, CYP3A4 and CYP3A5). Inhibition of the P450 isoforms was measured in specific assays using specific substrates that become fluorescent upon CYP metabolism. Compounds, dissolved in ACN (acetonitrile) (CYP2E1, CYP2C8, CYP2B6, CYP3A5) or DMSO (all remaining isoforms), were tested in duplicate (n=2) in concentration-response curves (eight concentrations) in a 96-well plate containing incubation/NADPH regenerating buffer. Specific isoenzymes and substrates were added and incubated at 37° C. Reactions were terminated at different times, depending on the assays, and plates read on a Fluoroskan Ascent at the appropriate emission/excitation wavelengths. Concentration-response curves performed in duplicate for known i
Drug: ketoconazole
Target: Arachidonate 15-lipoxygenase (Enzyme)
Gene: ALOX15
UniProt: P12530 (LOX15_RABIT)
Organism: Oryctolagus cuniculus
Activity: IC50 = 5.266
Assay: DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid)
Drug: ketoconazole
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.897
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: ketoconazole
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.211
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug: ketoconazole
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.009
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: ketoconazole
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.45
Drug: ketoconazole
Target: Gonadotropin-releasing hormone receptor (GPCR)
Gene: Gnrhr
UniProt: P30969 (GNRHR_RAT)
Organism: Rattus norvegicus
Activity: Kd = 9.66
Assay: Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M
Drug: ketoconazole
Target: 1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial (Enzyme)
Gene: CYP24A1
UniProt: Q07973 (CP24A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.506
Drug: ketoconazole
Target: Cytochrome P450 21 (Enzyme)
Gene: CYP21A2
UniProt: P08686 (CP21A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.05
Assay: Inhibition of Progesterone 21-hydroxylase cytochrome P450 21
Drug: ketoconazole
Target: Cytochrome P450 11B1 (Enzyme)
Gene: CYP11B1
UniProt: P15150 (C11B1_BOVIN)
Organism: Bos taurus
Activity: IC50 = 6.82
Assay: Inhibition of Corticoid 11-beta-hydroxylase cytochrome P450
Drug: ketoconazole
Target: Cytochrome P450 11A1 (Enzyme)
Gene: Cyp11a1
UniProt: P14137 (CP11A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.91
Assay: Inhibition of cholesterol side chain cleavage cytochrome P450
Drug: ketoconazole
Target: Cytochrome P450 24A1 (Enzyme)
Gene: Cyp24a1
UniProt: Q09128 (CP24A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.7
Assay: Inhibitory activity against 25-hydroxyvitamin D3 24-hydroxylase of rat kidney mitochondria
Drug: ketoconazole
Target: Cytochrome P450 7A1 (Enzyme)
Gene: Cyp7a1
UniProt: P18125 (CP7A1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.71
Assay: Inhibition of cytochrome P450 Cholesterol 7-alpha-hydroxylase
Drug: ketoconazole
Target: Cytochrome P450 51 (Enzyme)
Gene: Cyp51a1
UniProt: Q64654 (CP51A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.19
Assay: Inhibition of lanosterol 14-alpha-demethylase of rat hepatic microsomes
Drug: ketoconazole
Target: Cytochrome P450 17A1 (Enzyme)
Gene: Cyp17a1
UniProt: P11715 (CP17A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.69
Assay: Inhibition of 17,20-lyase activity of rat testicular microsomal P450-17alpha
Drug: ketoconazole
Target: Bile salt export pump (Transporter)
Gene: Abcb11
UniProt: O70127 (ABCBB_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.81
Assay: Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Drug: ketoconazole
Target: 25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial (Enzyme)
Gene: Cyp27b1
UniProt: O35084 (CP27B_MOUSE)
Organism: Mus musculus
Activity: IC50 = 6.44
Drug: ketoconazole
Target: Cytochrome P450 11B2, mitochondrial (Enzyme)
Gene: CYP11B2
UniProt: P19099 (C11B2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.174
Action type: INHIBITOR
Drug: ketoconazole
Target: Steroid 17-alpha-hydroxylase/17,20 lyase (Enzyme)
Gene: CYP17A1
UniProt: P05093 (CP17A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.28
Action type: INHIBITOR
Drug: ketoconazole
Target: Cytochrome P450 11B1, mitochondrial (Enzyme)
Gene: CYP11B1
UniProt: P15538 (C11B1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.896
Action type: INHIBITOR
Drug: ketoprofen
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.62
Action type: INHIBITOR
Drug: ketoprofen
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.33
Action type: INHIBITOR
Drug: ketoprofen
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P05979 (PGH1_SHEEP)
Organism: Ovis aries
Activity: IC50 = 6.1
Drug: ketoprofen
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P79208 (PGH2_SHEEP)
Organism: Ovis aries
Activity: IC50 = 6.75
Assay: Inhibition of ovine COX2 assessed as reduction in PGH2 production by enzyme immunoassay
Drug: ketoprofen
Target: Cyclooxygenase (Enzyme)
Gene: PTGS1|PTGS2
UniProt: O62664|O62698 (PGH1_BOVIN|PGH2_BOVIN)
Organism: Bos taurus
Activity: IC50 = 5.47
Assay: Evaluated for the inhibition of Prostaglandin synthetase obtained from bovine seminal vesicles at the dose of 4 mg/kg p.o.
Drug: ketorolac
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.9
Action type: INHIBITOR
Drug: ketorolac
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.72
Action type: INHIBITOR
Drug: ketorolac
Target: Fatty acid-binding protein, liver (Unclassified)
Gene: Fabp1
UniProt: P02692 (FABPL_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.94
Assay: Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay
Drug: ketorolac
Target: Aldose reductase (Enzyme)
Gene: Akr1b1
UniProt: P07943 (ALDR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.214
Assay: DRUGMATRIX: Aldose Reductase enzyme inhibition (substrate: DL-Glyceraldehyde)
Drug: ketorolac
Target: Prostaglandin-H2 D-isomerase (Enzyme)
Gene: Ptgds
UniProt: O09114 (PTGDS_MOUSE)
Organism: Mus musculus
Activity: IC50 = 6.64
Assay: Concentration required to inhibit 50% activity of prostaglandin synthetase was determined in vitro in mouse brain microsomes