AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: loperamide
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.685
Assay: DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug: loperamide
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.62
Assay: Inhibition of human Nav1.5 channel expressed in HEK293 cells at holding potential of -70 mV by whole cell patch clamp assay
Drug: loperamide
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.824
Action type: AGONIST
Drug: loperamide
Target: Glutamate receptor ionotropic, NMDA 2A (Ion channel)
Gene: GRIN2A
UniProt: Q12879 (NMDE1_HUMAN)
Organism: Homo sapiens
Drug: loperamide
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.578
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: loperamide
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.932
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: loperamide
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.583
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: loperamide
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.343
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: loperamide
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.699
Drug: loperamide
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.519
Assay: DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug: loperamide
Target: Aldehyde oxidase (Enzyme)
Gene: AOX1
UniProt: Q06278 (AOXA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5
Drug: loperamide
Target: Voltage-dependent P/Q-type calcium channel subunit alpha-1A (Ion channel)
Gene: CACNA1A
UniProt: O00555 (CAC1A_HUMAN)
Organism: Homo sapiens
Drug: loperamide
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.699
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: loperamide
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.599
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: loperamide
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.81
Drug: loperamide
Target: Calmodulin (Cytosolic other)
Gene: CALM1|CALM2|CALM3
UniProt: P0DP23|P0DP24|P0DP25 (CALM1_HUMAN|CALM2_HUMAN|CALM3_HUMAN)
Organism: Homo sapiens
Drug: loperamide
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.91
Drug: loperamide
Target: Somatostatin receptor type 5 (GPCR)
Gene: SSTR5
UniProt: P35346 (SSR5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.345
Drug: loperamide
Target: Glutamate receptor ionotropic, NMDA 2B (Ion channel)
Gene: GRIN2B
UniProt: Q13224 (NMDE2_HUMAN)
Organism: Homo sapiens
Drug: loperamide
Target: Glutamate receptor ionotropic, NMDA 2C (Ion channel)
Gene: GRIN2C
UniProt: Q14957 (NMDE3_HUMAN)
Organism: Homo sapiens
Drug: loperamide
Target: Glutamate receptor ionotropic, NMDA 2D (Ion channel)
Gene: GRIN2D
UniProt: O15399 (NMDE4_HUMAN)
Organism: Homo sapiens
Drug: loperamide
Target: Angiopoietin-1 receptor (Kinase)
Gene: TEK
UniProt: Q02763 (TIE2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.23
Assay: Binding affinity to human recombinant Tie2 by SPR assay
Drug: loperamide
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.63
Assay: Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Drug: loperamide
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.272
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: loperamide
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.072
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: loperamide
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.21
Drug: loperamide
Target: Mu-type opioid receptor (GPCR)
Gene: Oprm1
UniProt: P33535 (OPRM_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.8
Assay: Binding affinity for Mu opioid receptor of rat brain
Drug: loperamide
Target: Delta-type opioid receptor (GPCR)
Gene: Oprd1
UniProt: P33533 (OPRD_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.3
Assay: Binding affinity for delta opioid receptor of rat brain
Drug: loperamide
Target: Cocaine esterase (Enzyme)
Gene: CES2
UniProt: O00748 (EST2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.39
Assay: Inhibition of CE2 in human liver microsomes using fluorescein diacetate as substrate preincubated for 10 mins followed by substrate addition measured after 20 mins by luminescence assay
Drug: loperamide
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 = 6.57
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: loperamide
Target: Menin (Unclassified)
Gene: MEN1
UniProt: O00255 (MEN1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.16
Assay: Displacement of FITC-MBM1 from full length human menin measured after 2 hrs by fluorescence polarization assay
Drug: loperamide
Target: Calmodulin (Cytosolic other)
Gene: CALM
UniProt: P62157 (CALM_BOVIN)
Organism: Bos taurus
Activity: Kd = 5.46
Assay: Binding affinity to bovine brain CaM by FTPFACE analysis
Drug: lopinavir
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.07
Assay: Inhibition of human ERG
Drug: lopinavir
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.99
Assay: Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells
Drug: lopinavir
Target: Gag-Pol polyprotein (Polyprotein)
Gene: gag-pol
UniProt: P03367 (POL_HV1BR)
Organism: Human immunodeficiency virus type 1 group M subtype B (isolate BRU/LAI)
Drug: lopinavir
Target: Pol polyprotein (Enzyme)
Gene: pol
UniProt: Q72874 (Q72874_9HIV1)
Organism: Human immunodeficiency virus 1
Activity: Ki = 10.4
Action type: INHIBITOR
Assay: Inhibition of HIV1 protease D30N/L63P/N88D mutant
Drug: lopinavir
Target: CAAX prenyl protease 1 homolog (Enzyme)
Gene: Zmpste24
UniProt: Q80W54 (FACE1_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4.74
Assay: Inhibition of mouse ZMPSTE24 expressed n delta ste24 delta rce1 yeast
Drug: lopinavir
Target: Protease (Enzyme)
Gene: protease
UniProt: Q9YQ12 (Q9YQ12_9HIV1)
Organism: Human immunodeficiency virus 1
Activity: IC50 = 7.6
Assay: Inhibition of wild type C-South African Human immunodeficiency virus 1 protease using chromogenic peptide H-1048 as substrate by UV spectrophotometric analysis
Drug: lopinavir
Target: Protease (Unclassified)
Gene: HIV-1 protease
UniProt: O90781 (O90781_9PLVG)
Organism: Human immunodeficiency virus
Activity: Ki = 10.59
Assay: Inhibition of HIV1 recombinant protease D30N/N88D mutant expressed in Escherichia coli by spectrophotometric assay
Drug: lopinavir
Target: Protease (Unclassified)
Gene: HIV-1 protease
UniProt: Q9YQ30 (Q9YQ30_9PLVG)
Organism: Human immunodeficiency virus
Activity: Ki = 10.54
Assay: Inhibition of HIV1 recombinant protease L10I/I15V/E35D/N37S/R41K/I62V/L63P/A71V/G73S/L90M mutant expressed in Escherichia coli by spectrophotometric assay
Drug: loprazolam
Target: GABA-A receptor alpha-2/beta-3/gamma-2 (Ion channel)
Gene: GABRG2|GABRB3|GABRA2
UniProt: P18507|P28472|P47869 (GBRG2_HUMAN|GBRB3_HUMAN|GBRA2_HUMAN)
Organism: Homo sapiens
Drug: loprazolam
Target: GABA-A receptor alpha-3/beta-3/gamma-2 (Ion channel)
Gene: GABRG2|GABRB3|GABRA3
UniProt: P18507|P28472|P34903 (GBRG2_HUMAN|GBRB3_HUMAN|GBRA3_HUMAN)
Organism: Homo sapiens
Drug: loprazolam
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
Drug: loprazolam
Target: GABA-A receptor alpha-1/beta-3/gamma-2 (Ion channel)
Gene: GABRA1|GABRG2|GABRB3
UniProt: P14867|P18507|P28472 (GBRA1_HUMAN|GBRG2_HUMAN|GBRB3_HUMAN)
Organism: Homo sapiens
Drug: loracarbef
Target: Penicillin-binding protein 1A (Enzyme)
Gene: pbpA
UniProt: Q8XJ01 (PBPA_CLOPE)
Organism: Clostridium perfringens (strain 13 / Type A)
Drug: loracarbef
Target: Bacterial penicillin-binding protein (Enzyme)
Gene: mrcA|mrcB|dacC|mrdA|ftsI|dacA|dacB
UniProt: P02918|P02919|P08506|P0AD65|P0AD68|P0AEB2|P24228 (PBPA_ECOLI|PBPB_ECOLI|DACC_ECOLI|PBP2_ECOLI|FTSI_ECOLI|DACA_ECOLI|DACB_ECOLI)
Organism: Escherichia coli (strain K12)
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2354204; PROTEIN FAMILY
Drug: loratadine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.77
Drug: loratadine
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.94
Drug: loratadine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.807
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: loratadine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.97
Action type: ANTAGONIST
Drug: loratadine
Target: Nuclear receptor subfamily 1 group I member 2 (Nuclear hormone receptor)
Gene: NR1I2
UniProt: O75469 (NR1I2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.52
Assay: Agonist activity at PXR (unknown origin) expressed in human HepG2 cells assessed as induction of CYP3A4 transactivation after 16 hrs by luciferase reporter gene assay
Drug: loratadine
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: loratadine
Target: Potassium channel subfamily K member 9 (Ion channel)
Gene: KCNK9
UniProt: Q9NPC2 (KCNK9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.2
Assay: Inhibition of human TASK3 expressed in HEK293 cells by Ti+ flux assay
Drug: loratadine
Target: Bile acid receptor (Nuclear hormone receptor)
Gene: NR1H4
UniProt: Q96RI1 (NR1H4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.51
Assay: Antagonist activity at human GTS-tagged FXR after 20 mins by TR-FRET assay
Drug: loratadine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P31389 (HRH1_CAVPO)
Organism: Cavia porcellus
Activity: Kd = 7.14
Drug: loratadine
Target: Histamine H1 receptor (GPCR)
Gene: Hrh1
UniProt: P31390 (HRH1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.46
Assay: Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
Drug: loratadine
Target: Sodium-dependent neutral amino acid transporter B(0)AT2 (Transporter)
Gene: SLC6A15
UniProt: Q9H2J7 (S6A15_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.4
Drug: lorazepam
Target: Fatty acid-binding protein, liver (Unclassified)
Gene: Fabp1
UniProt: P02692 (FABPL_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.89
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: lorazepam
Target: GABA-A receptor alpha-1/beta-3/gamma-2 (Ion channel)
Gene: GABRA1|GABRG2|GABRB3
UniProt: P14867|P18507|P28472 (GBRA1_HUMAN|GBRG2_HUMAN|GBRB3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.456
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: lorcainide
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Drug: lorcainide
Target: Sodium channel subunit beta-1 (Ion channel)
Gene: SCN1B
UniProt: Q07699 (SCN1B_HUMAN)
Organism: Homo sapiens
Drug: lorcainide
Target: Sodium channel subunit beta-2 (Ion channel)
Gene: SCN2B
UniProt: O60939 (SCN2B_HUMAN)
Organism: Homo sapiens
Drug: lorcainide
Target: Sodium channel subunit beta-3 (Ion channel)
Gene: SCN3B
UniProt: Q9NY72 (SCN3B_HUMAN)
Organism: Homo sapiens
Drug: lorcainide
Target: Sodium channel subunit beta-4 (Ion channel)
Gene: SCN4B
UniProt: Q8IWT1 (SCN4B_HUMAN)
Organism: Homo sapiens
Drug: losartan
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: Km = 3.498
Drug: losartan
Target: Angiotensin-converting enzyme (Enzyme)
Gene: ACE
UniProt: P12821 (ACE_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.72
Assay: Inhibitory activity against angiotensin I converting enzyme (ACE)
Drug: losartan
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.54
Assay: DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: losartan
Target: Type-1 angiotensin II receptor (GPCR)
Gene: AGTR1
UniProt: P30556 (AGTR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.48
Action type: ANTAGONIST
Assay: Inhibition of angiotensin AT1 receptor
Drug: losartan
Target: Type-2 angiotensin II receptor (GPCR)
Gene: AGTR2
UniProt: P50052 (AGTR2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5
Assay: In vitro binding affinity of compound against angiotensin II AT-2 receptor
Drug: losartan
Target: Type-1B angiotensin II receptor (GPCR)
Gene: Agtr1b
UniProt: P29089 (AGTRB_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.44
Assay: Displacement of [125I]-Sar1-Ile8-A II from rat adrenal Angiotensin-1 (AT-1) receptor
Drug: losartan
Target: Type-2 angiotensin II receptor (GPCR)
Gene: Agtr2
UniProt: P35351 (AGTR2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.13
Assay: In vitro inhibitory activity against Angiotensin II receptor, type 2 in rat midbrain membrane preparations.
Drug: losartan
Target: Type-1 angiotensin II receptor (GPCR)
Gene: AGTR1
UniProt: P25104 (AGTR1_BOVIN)
Organism: Bos taurus
Activity: IC50 = 7.02
Assay: Displacement of [125I]AngII from type 1 angiotensin 2 receptor in bovine adrenal cortex
Drug: losartan
Target: Type-1A angiotensin II receptor (GPCR)
Gene: Agtr1
UniProt: P25095 (AGTRA_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.84
Assay: Binding affinity against angiotensin II receptor from rat liver; n=8
Drug: losartan
Target: Type-1 angiotensin II receptor (GPCR)
Gene: AGTR1
UniProt: P34976 (AGTR1_RABIT)
Organism: Oryctolagus cuniculus
Activity: Kd = 8.8
Assay: In vitro binding affinity against Angiotensin II receptor in rabbit aorta rings
Drug: losartan
Target: Type-1 angiotensin II receptor (GPCR)
Gene: AGTR1
UniProt: Q9WV26 (AGTR1_CAVPO)
Organism: Cavia porcellus
Activity: IC50 = 7.74
Assay: In vitro inhibition of the specific binding of [125I]angiotensin II to a guinea pig adrenal membrane preparation
Drug: losartan
Target: Phosphodiesterase 3 (Enzyme)
Gene: PDE3B|PDE3A
UniProt: Q13370|Q14432 (PDE3B_HUMAN|PDE3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.89
Assay: Inhibition of Phosphodiesterase 3
Drug: losartan
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 = 4.59
Assay: Inhibitory effect in cAMP-specific Phosphodiesterase 4 (PDE 4) isolated from guinea pig ventricular tissue.
Drug: losartan
Target: Angiotensin II receptor (AT-1) type-1 (GPCR)
Gene: Agtr1|Agtr1b
UniProt: P25095|P29089 (AGTRA_RAT|AGTRB_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.72
Assay: Displacement of [125I]-Ang II from rat liver membrane angiotensin II type 1 (AT1) receptor
Drug: losartan
Target: Angiotensin II receptor (GPCR)
Gene: Agtr1|Agtr1b|Agtr2
UniProt: P25095|P29089|P35351 (AGTRA_RAT|AGTRB_RAT|AGTR2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.34
Assay: Displacement of [3H]-AII from the Angiotensin II receptor isolated from the liver of rats
Drug: losartan
Target: Angiotensin II receptor (GPCR)
Gene: AGTR1|AGTR2
UniProt: P30556|P50052 (AGTR1_HUMAN|AGTR2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.43
Assay: Potency to antagonize the ability of angiotensin II to contract rabbit aorta
Drug: losartan
Target: Platelet glycoprotein VI (Unclassified)
Gene: GP6
UniProt: Q9HCN6 (GPVI_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.98
Assay: Antagonist activity at GP6 receptor in human platelet rich plasma assessed as inhibition of collagen-induced platelet aggregation preincubated for 5 mins followed by collagen addition measured after 5 mins by turbidimetric method
Drug: loteprednol etabonate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Drug: lovastatin
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.061
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: lovastatin
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.095
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: lovastatin
Target: Adenosine receptor A1 (GPCR)
Gene: ADORA1
UniProt: P30542 (AA1R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.807
Assay: DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX)
Drug: lovastatin
Target: Nuclear receptor subfamily 1 group I member 2 (Nuclear hormone receptor)
Gene: NR1I2
UniProt: O75469 (NR1I2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6
Action type: AGONIST
Drug: lovastatin
Target: 3-hydroxy-3-methylglutaryl-coenzyme A reductase (Enzyme)
Gene: HMGCR
UniProt: P04035 (HMDH_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.67
Action type: INHIBITOR
Drug: lovastatin
Target: Hydroxycarboxylic acid receptor 2 (GPCR)
Gene: HCAR2
UniProt: Q8TDS4 (HCAR2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.3
Drug: lovastatin
Target: Hydroxycarboxylic acid receptor 3 (GPCR)
Gene: HCAR3
UniProt: P49019 (HCAR3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.53
Drug: lovastatin
Target: Histone deacetylase 2 (Enzyme)
Gene: HDAC2
UniProt: Q92769 (HDAC2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.59
Assay: Inhibition of recombinant HDAC2 (unknown origin) after 10 mins by fluorimetric analysis
Drug: lovastatin
Target: Histone deacetylase 1 (Enzyme)
Gene: HDAC1
UniProt: Q13547 (HDAC1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.92
Assay: Inhibition of recombinant HDAC1 (unknown origin) after 10 mins by fluorimetric analysis
Drug: lovastatin
Target: Histone deacetylase 6 (Enzyme)
Gene: HDAC6
UniProt: Q9UBN7 (HDAC6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.79
Assay: Inhibition of recombinant HDAC6 (unknown origin) after 10 mins by fluorimetric analysis
Drug: lovastatin
Target: Substance-K receptor (GPCR)
Gene: TACR2
UniProt: P21452 (NK2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.027
Assay: DRUGMATRIX: Tachykinin NK2  radioligand binding (ligand: [3H] SR-48968)
Drug: lovastatin
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.697
Assay: DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
Drug: lovastatin
Target: Acetylcholinesterase (Enzyme)
Gene: ache
UniProt: O42275 (ACES_ELEEL)
Organism: Electrophorus electricus
Activity: Ki = 5.57
Assay: Inhibition of Electrophorus electricus (electric eel) acetylcholinesterase (AChE) assessed as inhibition of ATCh hydrolysis by Ellman method
Drug: lovastatin
Target: 3-hydroxy-3-methylglutaryl-coenzyme A reductase (Enzyme)
Gene: Hmgcr
UniProt: P51639 (HMDH_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.52
Assay: Inhibition of rat liver microsomal HMG-CoA reductase
Drug: lovastatin
Target: 3-hydroxy-3-methylglutaryl-coenzyme A reductase (Enzyme)
Gene: Hmgcr
UniProt: Q01237 (HMDH_MOUSE)
Organism: Mus musculus
Activity: IC50 = 7.57
Assay: In vitro inhibitory activity against isolated enzyme HMG-CoA reductase
Drug: lovastatin
Target: Cholinesterase (Enzyme)
Gene: BCHE
UniProt: P81908 (CHLE_HORSE)
Organism: Equus caballus
Activity: Ki = 5.96
Assay: Inhibition of Equus caballus (horse) serum butyrylcholinesterase (BChE) assessed as inhibition of BTCh hydrolysis by Ellman method
Drug: lovastatin
Target: Leukocyte adhesion glycoprotein LFA-1 alpha (Adhesion)
Gene: ITGAL
UniProt: P20701 (ITAL_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.89
Assay: Binding affinity to I-domain of human integrin alphaL (amino acid residues 128 to 307) plus initial methionine expressed in Escherichia coli by NMR spectroscopy
Drug: lovastatin
Target: Acyl-CoA:cholesterol acyltransferase (Enzyme)
Gene: ACAT
UniProt: Q95214 (Q95214_RABIT)
Organism: Oryctolagus cuniculus
Activity: IC50 = 4.77
Drug: loxapine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.268
Drug: loxapine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.68
Action type: ANTAGONIST
Assay: Affinity was evaluated by inhibition of [3H]spiperone binding to COS cells transfected with human dopamine D-2(long) receptor
Drug: loxapine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.821
Drug: loxapine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.244
Drug: loxapine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.61
Drug: loxapine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.62
Action type: ANTAGONIST
Assay: Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug: loxapine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8
Action type: ANTAGONIST
Drug: loxapine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.82
Assay: Binding affinity towards human 5-hydroxytryptamine 6 receptor
Drug: loxapine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.509
Drug: loxapine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.967