AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: famotidine
Target: Carbonic anhydrase 12 (Enzyme)
Gene: CA12
UniProt: O43570 (CAH12_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.34
Assay: Inhibition of recombinant human CA12 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay
Drug: famotidine
Target: Carbonic anhydrase 5A, mitochondrial (Enzyme)
Gene: CA5A
UniProt: P35218 (CAH5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.84
Assay: Inhibition of recombinant human CA5a preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay
Drug: famotidine
Target: Carbonic anhydrase 5B, mitochondrial (Enzyme)
Gene: CA5B
UniProt: Q9Y2D0 (CAH5B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.27
Assay: Inhibition of recombinant human CA5b preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay
Drug: famotidine
Target: Carbonic anhydrase 7 (Enzyme)
Gene: CA7
UniProt: P43166 (CAH7_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.52
Assay: Inhibition of recombinant human CA7 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay
Drug: famotidine
Target: Carbonic anhydrase 6 (Enzyme)
Gene: CA6
UniProt: P23280 (CAH6_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.01
Assay: Inhibition of recombinant human CA6 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay
Drug: famotidine
Target: Carbonic anhydrase 14 (Enzyme)
Gene: CA14
UniProt: Q9ULX7 (CAH14_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.17
Assay: Inhibition of recombinant human CA14 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay
Drug: famotidine
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P47747 (HRH2_CAVPO)
Organism: Cavia porcellus
Activity: Kd = 7
Assay: In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
Drug: famotidine
Target: Carbonic anhydrase 13 (Enzyme)
Gene: CA13
UniProt: Q8N1Q1 (CAH13_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.77
Assay: Inhibition of recombinant human CA13 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay
Drug: famotidine
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.44
Assay: Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Drug: famotidine
Target: Multidrug and toxin extrusion protein 1 (Transporter)
Gene: SLC47A1
UniProt: Q96FL8 (S47A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.12
Assay: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Drug: famotidine
Target: Multidrug and toxin extrusion protein 2 (Transporter)
Gene: SLC47A2
UniProt: Q86VL8 (S47A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.44
Assay: Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Drug: famotidine
Target: Heat shock protein HSP 90-alpha (Cytosolic other)
Gene: HSP90AA1
UniProt: P07900 (HS90A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.304
Drug: famotidine
Target: Solute carrier family 22 member 3 (Transporter)
Gene: SLC22A3
UniProt: O75751 (S22A3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.97
Assay: Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Drug: famprofazone
Target: Nuclear receptor subfamily 2 group E member 1 (Nuclear hormone receptor)
Gene: NR2E1
UniProt: Q9Y466 (NR2E1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.18
Assay: orthogonal direct binding assay
Drug: fasudil
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.6
Assay: Displacement of [3H]dofetilide from human ERG
Drug: fasudil
Target: Myosin light chain kinase, smooth muscle (Kinase)
Gene: MYLK
UniProt: Q15746 (MYLK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.44
Assay: Inhibition of MLCK by HTRF assay
Drug: fasudil
Target: Protein kinase C epsilon type (Kinase)
Gene: PRKCE
UniProt: Q02156 (KPCE_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.52
Assay: Inhibition of PKCepsilon
Drug: fasudil
Target: Serine/threonine-protein kinase N1 (Kinase)
Gene: PKN1
UniProt: Q16512 (PKN1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.77
Assay: Inhibition of Protein kinase C related kinase 1 (PRK1)
Drug: fasudil
Target: Ribosomal protein S6 kinase alpha-5 (Kinase)
Gene: RPS6KA5
UniProt: O75582 (KS6A5_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.3
Assay: Inhibition of His-tagged human MSK1 expressed in Sf9 cells
Drug: fasudil
Target: C-C motif chemokine 2 (Cytokine)
Gene: CCL2
UniProt: P13500 (CCL2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.16
Assay: Inhibition of MCP1-mediated human THP cell migration
Drug: fasudil
Target: Serine/threonine-protein kinase N2 (Kinase)
Gene: PKN2
UniProt: Q16513 (PKN2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.11
Assay: Inhibition of PKN2
Drug: fasudil
Target: cAMP-dependent protein kinase catalytic subunit alpha (Kinase)
Gene: PRKACA
UniProt: P17612 (KAPCA_HUMAN)
Organism: Homo sapiens
Activity: AC50 = 5.81
Assay: PUBCHEM_BIOASSAY: Protein Kinase A Activity Assay Measured in Biochemical System Using Plate Reader - 2052-04_Inhibitor_Dose_DryPowder_Activity. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID2689]
Drug: fasudil
Target: Rho-associated protein kinase 2 (Kinase)
Gene: Rock2
UniProt: Q62868 (ROCK2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.72
Assay: Inhibition of rat ROCK2 expressed in Sf9 cells
Drug: fasudil
Target: Rho-associated protein kinase 1 (Kinase)
Gene: ROCK1
UniProt: Q13464 (ROCK1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7
Action type: INHIBITOR
Assay: Inhibition of ROCK-1
Drug: fasudil
Target: Rho-associated protein kinase 2 (Kinase)
Gene: ROCK2
UniProt: O75116 (ROCK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.11
Action type: INHIBITOR
Assay: Displacement of fluorescent-ARC-1063 from His6-tagged recombinant human ROCK2 by luminescence intensity assay
Drug: febuxostat
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.44
Drug: febuxostat
Target: Xanthine dehydrogenase/oxidase (Enzyme)
Gene: XDH
UniProt: P47989 (XDH_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.22
Action type: INHIBITOR
Drug: febuxostat
Target: Xanthine dehydrogenase/oxidase (Enzyme)
Gene: XDH
UniProt: P80457 (XDH_BOVIN)
Organism: Bos taurus
Activity: IC50 = 8.52
Assay: Inhibition of bovine xanthine oxidase by spectrophotometry
Drug: febuxostat
Target: Xanthine dehydrogenase/oxidase (Enzyme)
Gene: Xdh
UniProt: P22985 (XDH_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.4
Assay: Inhibition of rat xanthine oxidase
Drug: felbamate
Target: Glutamate receptor ionotropic, NMDA 2A (Ion channel)
Gene: GRIN2A
UniProt: Q12879 (NMDE1_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Drug: felbamate
Target: Glutamate receptor ionotropic, NMDA 2B (Ion channel)
Gene: GRIN2B
UniProt: Q13224 (NMDE2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.284
Action type: ANTAGONIST
Drug: felbinac
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action
Drug: felbinac
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.049
Action type: INHIBITOR
Assay: DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid)
Drug: felodipine
Target: Aldehyde oxidase (Enzyme)
Gene: AOX1
UniProt: Q06278 (AOXA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.523
Drug: felodipine
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.224
Assay: DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
Drug: felodipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: CACNA1C
UniProt: Q13936 (CAC1C_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: felodipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1D (Ion channel)
Gene: CACNA1D
UniProt: Q01668 (CAC1D_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: felodipine
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.339
Assay: DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: felodipine
Target: Voltage-dependent T-type calcium channel subunit alpha-1H (Ion channel)
Gene: CACNA1H
UniProt: O95180 (CAC1H_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.168
Drug: felodipine
Target: Bile acid receptor (Nuclear hormone receptor)
Gene: NR1H4
UniProt: Q96RI1 (NR1H4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.3
Assay: Antagonist activity at human GTS-tagged FXR after 20 mins by TR-FRET assay
Drug: felodipine
Target: Cystic fibrosis transmembrane conductance regulator (Ion channel)
Gene: CFTR
UniProt: P13569 (CFTR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.4
Action type: ACTIVATOR
Drug: felodipine
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 = 4.43
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: fenbufen
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P05979 (PGH1_SHEEP)
Organism: Ovis aries
Activity: IC50 = 5.41
Assay: Inhibition of ovine COX1 by enzyme-immuno assay
Drug: fenbufen
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P79208 (PGH2_SHEEP)
Organism: Ovis aries
Activity: IC50 = 5.09
Assay: Inhibition of ovine COX2 by enzyme-immuno assay
Drug: fenbufen
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Drug: fenbufen
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Drug: fendiline
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.49
Assay: Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug: fendiline
Target: Extracellular calcium-sensing receptor (GPCR)
Gene: CASR
UniProt: P41180 (CASR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6
Assay: Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
Drug: fendiline
Target: Transcriptional activator protein luxR (Unclassified)
Gene: luxR
UniProt: P12746 (LUXR_ALIFS)
Organism: Aliivibrio fischeri
Activity: IC50 = 4.04
Assay: Inhibition of LuxR-dependent quorum sensing in Vibrio fischeri assessed as reduction of 3-oxo-C6-HSL-induced bioluminescence intensity
Drug: fendiline
Target: Calmodulin (Cytosolic other)
Gene: CALM
UniProt: P62157 (CALM_BOVIN)
Organism: Bos taurus
Activity: Kd = 6.3
Assay: Binding affinity to dansylated bovine testes CaM by fluorescence analysis in presence of calcium2+
Drug: fendiline
Target: Extracellular calcium-sensing receptor (GPCR)
Gene: CASR
UniProt: P35384 (CASR_BOVIN)
Organism: Bos taurus
Activity: EC50 = 4.921
Action type: POSITIVE ALLOSTERIC MODULATOR
Assay: increase in intracellular Ca2+ in bovine parathyroid cells
Drug: fenfluramine
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.004
Drug: fenfluramine
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.111
Drug: fenfluramine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.428
Drug: fenfluramine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.176
Drug: fenfluramine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.172
Drug: fenfluramine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.845
Drug: fenfluramine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.398
Drug: fenfluramine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.79
Drug: fenfluramine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.042
Drug: fenfluramine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.378
Drug: fenfluramine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.57
Drug: fenfluramine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.717
Drug: fenfluramine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.016
Drug: fenfluramine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.726
Drug: fenfluramine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.489
Drug: fenfluramine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.167
Drug: fenfluramine
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.736
Drug: fenfluramine
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.195
Drug: fenfluramine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.735
Drug: fenfluramine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.848
Drug: fenfluramine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: Slc6a4
UniProt: P31652 (SC6A4_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 6.97
Assay: Activity at SERT in rat synaptosomes assessed as release of [3H]HT after 5 mins by liquid scintillation counting method
Drug: fenofibrate
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.673
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: fenofibrate
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.218
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: fenofibrate
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.906
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: fenofibrate
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.331
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: fenofibrate
Target: Beta-3 adrenergic receptor (GPCR)
Gene: ADRB3
UniProt: P13945 (ADRB3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.032
Assay: DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug: fenofibrate
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.164
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: fenofibrate
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.492
Assay: DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
Drug: fenofibrate
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P22303 (ACES_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.808
Assay: DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine)
Drug: fenofibrate
Target: Peroxisome proliferator-activated receptor alpha (Nuclear hormone receptor)
Gene: PPARA
UniProt: Q07869 (PPARA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Action type: AGONIST
Assay: Inhibition of human PPARalpha receptor by scintillation proximity assay
Drug: fenofibrate
Target: Peroxisome proliferator-activated receptor gamma (Nuclear hormone receptor)
Gene: PPARG
UniProt: P37231 (PPARG_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.24
Assay: In vitro activation of human peroxisome proliferator activated receptor gamma (PPAR gamma)
Drug: fenofibrate
Target: Fatty acid-binding protein, liver (Unclassified)
Gene: Fabp1
UniProt: P02692 (FABPL_RAT)
Organism: Rattus norvegicus
Activity: Kd = 7.74
Assay: Binding affinity to rat recombinant L-FABP high affinity site expressed in Escherichia coli BL21(DE3) at 5 deg C by fluorimetric assay
Drug: fenofibrate
Target: Cruzipain (Enzyme)
UniProt: P25779 (CYSP_TRYCR)
Organism: Trypanosoma cruzi
Activity: IC50 = 4.21
Assay: Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-100
Drug: fenoldopam
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.55
Action type: AGONIST
Assay: Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug: fenoldopam
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.09
Assay: Affinity towards Dopamine receptor D2
Drug: fenoldopam
Target: D(1B) dopamine receptor (GPCR)
Gene: DRD5
UniProt: P21918 (DRD5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.96
Drug: fenoldopam
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.5
Action type: AGONIST
Drug: fenoldopam
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Kd = 5.89
Assay: In vitro affinity at wild type Dopamine receptor D2 on C6 (glioma) cell membranes.
Drug: fenoldopam
Target: D(1A) dopamine receptor (GPCR)
Gene: Drd1
UniProt: P18901 (DRD1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.52
Assay: Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug: fenoldopam
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P20288 (DRD2_BOVIN)
Organism: Bos taurus
Activity: Ki = 6.1
Assay: Compound was tested for inhibition of [3H]spiroperidol binding against Dopamine receptor D2
Drug: fenoldopam
Target: Lysine-specific demethylase 4E (Enzyme)
Gene: KDM4E
UniProt: B2RXH2 (KDM4E_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.72
Assay: Non-competitive inhibition of JMJD2E relative to alpha-ketoglutarate
Drug: fenoldopam
Target: Adrenergic receptor alpha-1 (GPCR)
Gene: ADRA1D|ADRA1A|ADRA1B
UniProt: P25100|P35348|P35368 (ADA1D_HUMAN|ADA1A_HUMAN|ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.3
Assay: Activity at alpha-1 adrenergic receptor in rabbit aorta rings
Drug: fenoldopam
Target: Adenosine A2b receptor (GPCR)
Gene: Adora2b
UniProt: P29276 (AA2BR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.45
Drug: fenoldopam
Target: FAD-linked sulfhydryl oxidase ALR (Enzyme)
Gene: GFER
UniProt: P55789 (ALR_HUMAN)
Organism: Homo sapiens
Activity: AC50 = 5.86
Assay: PUBCHEM_BIOASSAY: HTS-Luminescent assay for inhibitors of ALR by detection of hydrogen peroxide production Measured in Biochemical System Using Plate Reader - 2036-02_Inhibitor_Dose_CherryPick_Activity. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID488787]
Drug: fenoprofen
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.23
Action type: INHIBITOR
Drug: fenoprofen
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.36
Action type: INHIBITOR
Drug: fenoprofen
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P79208 (PGH2_SHEEP)
Organism: Ovis aries
Activity: IC50 = 4.58
Assay: Inhibition of ovine COX2 assessed as reduction in PGH2 production by enzyme immunoassay
Drug: fenoprofen
Target: Cyclooxygenase (Enzyme)
Gene: PTGS1|PTGS2
UniProt: O62664|O62698 (PGH1_BOVIN|PGH2_BOVIN)
Organism: Bos taurus
Activity: IC50 = 4.01
Assay: Evaluated for the inhibition of Prostaglandin synthetase obtained from bovine seminal vesicles at the dose of 20 mg/kg (p.o.)
Drug: fenoprofen
Target: Sodium-coupled monocarboxylate transporter 1 (Transporter)
Gene: SLC5A8
UniProt: Q8N695 (SC5A8_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.57
Action type: INHIBITOR
Drug: fenoterol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.9
Action type: AGONIST
Drug: fenoterol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: Adrb2
UniProt: Q8K4Z4 (ADRB2_CAVPO)
Organism: Cavia porcellus
Activity: IC50 = 7.22
Assay: In vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig trachea
Drug: fentanyl
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 9.001
Action type: AGONIST
Drug: fentanyl
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.45
Assay: Displacement of [3H]PPP from sigma1 receptor (unknown origin)
Drug: fentanyl
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.74
Assay: Inhibitory concentration against potassium channel HERG
Drug: fentanyl
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.71
Assay: Binding affinity against Opioid receptor kappa 1
Drug: fentanyl
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.17
Assay: Binding affinity against Opioid receptor delta 1 in guinea pig brain membranes
Drug: fentanyl
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.34
Assay: Inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis
Drug: fentanyl
Target: Mu-type opioid receptor (GPCR)
Gene: Oprm1
UniProt: P33535 (OPRM_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.82
Assay: Inhibition of [3H]DAMGO binding to mu opioid receptor of rat brain membranes
Drug: fentanyl
Target: Mu-type opioid receptor (GPCR)
Gene: Oprm1
UniProt: P42866 (OPRM_MOUSE)
Organism: Mus musculus
Activity: Ki = 8.23
Drug: fentanyl
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P97266 (OPRM_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 8.07
Assay: Binding affinity against mu opioid receptor in guinea pig brain membranes