AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: enalaprilat
Target: Angiotensin-converting enzyme (Enzyme)
Gene: Ace
UniProt: P09470 (ACE_MOUSE)
Organism: Mus musculus
Activity: IC50 = 7.94
Assay: Inhibition of ob/ob mouse plasma ACE
Drug: encainide
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Drug: encainide
Target: Sodium channel subunit beta-1 (Ion channel)
Gene: SCN1B
UniProt: Q07699 (SCN1B_HUMAN)
Organism: Homo sapiens
Drug: encainide
Target: Sodium channel subunit beta-2 (Ion channel)
Gene: SCN2B
UniProt: O60939 (SCN2B_HUMAN)
Organism: Homo sapiens
Drug: encainide
Target: Sodium channel subunit beta-3 (Ion channel)
Gene: SCN3B
UniProt: Q9NY72 (SCN3B_HUMAN)
Organism: Homo sapiens
Drug: encainide
Target: Sodium channel subunit beta-4 (Ion channel)
Gene: SCN4B
UniProt: Q8IWT1 (SCN4B_HUMAN)
Organism: Homo sapiens
Drug: endralazine
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: CACNA1C
UniProt: Q13936 (CAC1C_HUMAN)
Organism: Homo sapiens
Drug: enflurane
Target: Glycine receptor subunit alpha-1 (Ion channel)
Gene: GLRA1
UniProt: P23415 (GLRA1_HUMAN)
Organism: Homo sapiens
Action type: POSITIVE MODULATOR
Drug: enflurane
Target: Potassium channel subfamily K member 2 (Ion channel)
Gene: KCNK2
UniProt: O95069 (KCNK2_HUMAN)
Organism: Homo sapiens
Action type: OPENER
Assay: Mechanism of Action; CHEMBL2321615; SINGLE PROTEIN
Drug: enflurane
Target: Potassium channel subfamily K member 3 (Ion channel)
Gene: KCNK3
UniProt: O14649 (KCNK3_HUMAN)
Organism: Homo sapiens
Action type: OPENER
Assay: Mechanism of Action; CHEMBL2321613; SINGLE PROTEIN
Drug: enflurane
Target: Potassium channel subfamily K member 9 (Ion channel)
Gene: KCNK9
UniProt: Q9NPC2 (KCNK9_HUMAN)
Organism: Homo sapiens
Action type: OPENER
Assay: Mechanism of Action; CHEMBL2321614; SINGLE PROTEIN
Drug: enflurane
Target: Potassium channel subfamily K member 10 (Ion channel)
Gene: KCNK10
UniProt: P57789 (KCNKA_HUMAN)
Organism: Homo sapiens
Action type: OPENER
Assay: Mechanism of Action; CHEMBL2331041; SINGLE PROTEIN
Drug: enflurane
Target: Potassium channel subfamily K member 18 (Ion channel)
Gene: KCNK18
UniProt: Q7Z418 (KCNKI_HUMAN)
Organism: Homo sapiens
Action type: OPENER
Assay: Mechanism of Action; CHEMBL2331042; SINGLE PROTEIN
Drug: enfuvirtide
Target: Envelope glycoprotein (Viral envelope protein)
Gene: gp41
UniProt: Q53I07 (Q53I07_9HIV1)
Organism: Human immunodeficiency virus 1
Drug: enfuvirtide
Target: Transmembrane glycoprotein gp41 (Membrane other)
Gene: env
UniProt: O40239 (O40239_9PLVG)
Organism: Human immunodeficiency virus
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2362987; SINGLE PROTEIN
Drug: enfuvirtide
Target: GP41 (Unclassified)
Gene: HIV1 ENV
UniProt: Q76270 (Q76270_9HIV1)
Organism: Human immunodeficiency virus 1
Activity: EC50 = 8
Drug: enoxacin
Target: DNA gyrase subunit A (Enzyme)
Gene: gyrA
UniProt: P43700 (GYRA_HAEIN)
Organism: Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
Drug: enoxacin
Target: V-type proton ATPase subunit B, brain isoform (Enzyme)
Gene: ATP6V1B2
UniProt: P21281 (VATB2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5
Assay: Inhibition of maltose binding protein-fused human V-ATPase subunit B2 binding to F-actin
Drug: enoxacin
Target: Topoisomerase IV (Enzyme)
Gene: parC|topB
UniProt: P48374|Q5EP76 (PARC_NEIGO|Q5EP76_NEIGO)
Organism: Neisseria gonorrhoeae
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2363077; PROTEIN COMPLEX
Drug: enoxacin
Target: DNA gyrase (Enzyme)
Gene: gyrB|gyrA
UniProt: P22118|P48371 (GYRB_NEIGO|GYRA_NEIGO)
Organism: Neisseria gonorrhoeae
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2311244; PROTEIN COMPLEX
Drug: enoximone
Target: cGMP-inhibited 3',5'-cyclic phosphodiesterase A (Enzyme)
Gene: PDE3A
UniProt: Q14432 (PDE3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.345
Drug: enoximone
Target: Phosphodiesterase 4 (Enzyme)
Gene: PDE4A|PDE4B|PDE4C|PDE4D
UniProt: P27815|Q07343|Q08493|Q08499 (PDE4A_HUMAN|PDE4B_HUMAN|PDE4C_HUMAN|PDE4D_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.54
Assay: Inhibition of canine heart Phosphodiesterase 4
Drug: enprofylline
Target: Adenosine receptor A2a (GPCR)
Gene: ADORA2A
UniProt: P29274 (AA2AR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.49
Assay: Binding affinity to human adenosine A2A receptor
Drug: enprofylline
Target: Adenosine receptor A1 (GPCR)
Gene: ADORA1
UniProt: P30542 (AA1R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.38
Assay: Displacement of [3H]CPX from human adenosine A3 receptor expressed in CHO cells
Drug: enprofylline
Target: Adenosine receptor A2b (GPCR)
Gene: ADORA2B
UniProt: P29275 (AA2BR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.33
Assay: Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
Drug: enprofylline
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.03
Assay: Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells
Drug: enprofylline
Target: cAMP-specific 3',5'-cyclic phosphodiesterase 4B (Enzyme)
Gene: PDE4B
UniProt: Q07343 (PDE4B_HUMAN)
Organism: Homo sapiens
Drug: enprofylline
Target: Adenosine receptor A1 (GPCR)
Gene: Adora1
UniProt: P25099 (AA1R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.49
Assay: Binding affinity at Adenosine A1 receptor in rat brain cortical membrane using [3H]N6-R-phenylisopropyladenosine (R-PIA) as radioligand
Drug: enprofylline
Target: Adenosine receptor A2a (GPCR)
Gene: Adora2a
UniProt: P30543 (AA2AR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.49
Assay: Binding affinity to rat adenosine A2A receptor
Drug: enprofylline
Target: Adenosine receptor A3 (GPCR)
Gene: Adora3
UniProt: P28647 (AA3R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.19
Assay: Binding affinity to rat adenosine A3 receptor
Drug: enprofylline
Target: Adenosine receptor A1 (GPCR)
Gene: ADORA1
UniProt: P47745 (AA1R_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 4.22
Assay: Affinity against adenosine A1 receptor in the brain membranes by the displacement of [3H]CPX.
Drug: enprofylline
Target: Adenosine A2a receptor (GPCR)
Gene: ADORA2A
UniProt: P46616 (AA2AR_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 4.04
Assay: Affinity against adenosine A2 receptor in the brain membranes measured by the displacement of [3H]-CPX
Drug: enprostil
Target: Prostaglandin E2 receptor EP1 subtype (GPCR)
Gene: PTGER1
UniProt: P34995 (PE2R1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.5
Drug: enprostil
Target: Prostaglandin E2 receptor EP3 subtype (GPCR)
Gene: PTGER3
UniProt: P43115 (PE2R3_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.9
Drug: enprostil
Target: Prostacyclin receptor (GPCR)
Gene: PTGIR
UniProt: P43119 (PI2R_HUMAN)
Organism: Homo sapiens
Drug: enprostil
Target: Prostaglandin E2 receptor EP4 subtype (GPCR)
Gene: PTGER4
UniProt: P35408 (PE2R4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.4
Action type: AGONIST
Drug: enprostil
Target: Prostaglandin F2-alpha receptor (GPCR)
Gene: PTGFR
UniProt: P43088 (PF2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.1
Action type: AGONIST
Drug: enprostil
Target: Prostaglandin E2 receptor EP3 subtype (GPCR)
Gene: Ptger3
UniProt: P34980 (PE2R3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.13
Action type: AGONIST
Drug: enprostil
Target: Prostaglandin E2 receptor EP1 subtype (GPCR)
Gene: Ptger1
UniProt: P70597 (PE2R1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.7
Action type: AGONIST
Drug: entacapone
Target: Catechol O-methyltransferase (Enzyme)
Gene: Comt
UniProt: P22734 (COMT_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.89
Assay: Inhibition of Catechol O-methyltransferase activity in rat brain
Drug: entacapone
Target: G-protein coupled receptor 35 (GPCR)
Gene: GPR35
UniProt: Q9HC97 (GPR35_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.25
Drug: entacapone
Target: Alpha-ketoglutarate-dependent dioxygenase FTO (Unclassified)
Gene: FTO
UniProt: Q9C0B1 (FTO_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.52
Assay: Inhibition of FTO (unknown origin) assessed as reduction in demethylation by measuring N6-mA and A level incubated for 2 hrs by HPLC-MS/MS analysis
Drug: entacapone
Target: Catechol O-methyltransferase (Enzyme)
Gene: COMT
UniProt: P21964 (COMT_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.523
Action type: INHIBITOR
Drug: entecavir
Target: Protein P (Polyprotein)
Gene: P
UniProt: P17394 (DPOL_HBVB1)
Organism: Hepatitis B virus genotype B1 subtype adw (isolate Japan/pJDW233/1988)
Drug: entecavir
Target: Protein P (Polyprotein)
Gene: P
UniProt: Q9IF40 (Q9IF40_HBV)
Organism: Hepatitis B virus
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2362994; SINGLE PROTEIN
Drug: entecavir
Target: Capsid protein (Unclassified)
Gene: HBcAg
UniProt: Q03732 (Q03732_HBV)
Organism: Hepatitis B virus
Activity: EC50 = 9.62
Assay: Inhibition of hepatitis B virus capsid assembly infected in human HepG2.215 cells assessed as reduction in viral DNA replication measured on day 7 by real time PCR analysis
Drug: epalrestat
Target: Alcohol dehydrogenase [NADP(+)] (Enzyme)
Gene: AKR1A1
UniProt: P14550 (AK1A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.59
Assay: Inhibition of N-terminal 6His-tagged human aldehyde reductase expressed in Escherichia coli BL21(DE3) mediated D-glucuronate reduction
Drug: epalrestat
Target: Alcohol dehydrogenase [NADP(+)] (Enzyme)
Gene: AKR1A1
UniProt: P50578 (AK1A1_PIG)
Organism: Sus scrofa
Activity: IC50 = 5.82
Assay: Selectivity ratio measured as the IC50 ratio of aldehyde/aldose reductase values
Drug: epalrestat
Target: Aldose reductase (Enzyme)
Gene: Akr1b1
UniProt: P07943 (ALDR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8
Assay: Inhibition of crude aldose reductase of rat lens
Drug: epalrestat
Target: Aldose reductase (Enzyme)
Gene: AKR1B1
UniProt: P16116 (ALDR_BOVIN)
Organism: Bos taurus
Activity: IC50 = 6.77
Assay: Inhibition of bovine lens aldose reductase assessed as inhibition of NDAPH oxidation by non-linear regression analysis
Drug: epalrestat
Target: Alcohol dehydrogenase [NADP(+)] (Enzyme)
Gene: Akr1a1
UniProt: P51635 (AK1A1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.82
Assay: In vitro inhibitory activity against rat kidney aldehyde reductase(ALR).
Drug: epalrestat
Target: Aldo-keto reductase family 1 member B10 (Enzyme)
Gene: AKR1B10
UniProt: O60218 (AK1BA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.48
Assay: Inhibition of reductase activity of N-terminal 6His-tagged AKR1B10 expressed in Escherichia coli BL21(DE3) assessed as inhibition of NADPH linked pyridine-3-aldehyde reduction
Drug: epalrestat
Target: Sorbitol dehydrogenase (Enzyme)
Gene: SORD
UniProt: Q00796 (DHSO_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.17
Assay: Inhibition sorbitol dehydrogenase by spectrophotometric analysis
Drug: epalrestat
Target: Cytochrome P450 4A11 (Enzyme)
Gene: CYP4A11
UniProt: Q02928 (CP4AB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.74
Action type: INHIBITOR
Drug: epalrestat
Target: Aldose reductase (Enzyme)
Gene: AKR1B1
UniProt: P15121 (ALDR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.678
Action type: INHIBITOR
Drug: eperisone
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.77
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: eperisone
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.859
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: eperisone
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.08
Assay: DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: eperisone
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.31
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: ephedrine
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.6
Action type: AGONIST
Drug: epinastine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Drug: epinastine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4
Drug: epinastine
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Drug: epinastine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Drug: epinastine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Drug: epinastine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.9
Action type: ANTAGONIST
Drug: epinastine
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Drug: epinastine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P31389 (HRH1_CAVPO)
Organism: Cavia porcellus
Activity: IC50 = 8.8
Assay: Potency against histamine H1 receptor on guinea pig ileum
Drug: epinastine
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.37
Assay: Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Drug: epinastine
Target: Multidrug and toxin extrusion protein 1 (Transporter)
Gene: SLC47A1
UniProt: Q96FL8 (S47A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.96
Assay: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Drug: epinastine
Target: Multidrug and toxin extrusion protein 2 (Transporter)
Gene: SLC47A2
UniProt: Q86VL8 (S47A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.53
Assay: Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Drug: epinephrine
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.401
Drug: epinephrine
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.2
Action type: AGONIST
Assay: Binding affinity to human adrenergic beta2 receptor
Drug: epinephrine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.26
Assay: Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug: epinephrine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.04
Assay: Displacement of [3H]spiperone from human D2S receptor expressed in CHO cells
Drug: epinephrine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.559
Action type: AGONIST
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: epinephrine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.434
Drug: epinephrine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.7
Action type: AGONIST
Assay: Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
Drug: epinephrine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.401
Action type: AGONIST
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: epinephrine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.449
Action type: AGONIST
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: epinephrine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.66
Action type: AGONIST
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: epinephrine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.5
Action type: AGONIST
Drug: epinephrine
Target: Arachidonate 15-lipoxygenase (Enzyme)
Gene: ALOX15
UniProt: P12530 (LOX15_RABIT)
Organism: Oryctolagus cuniculus
Activity: IC50 = 5.484
Assay: DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid)
Drug: epinephrine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.01
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: epinephrine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.2
Drug: epinephrine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: Adra1d
UniProt: P23944 (ADA1D_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.3
Action type: AGONIST
Drug: epinephrine
Target: Mu-type opioid receptor (GPCR)
Gene: Oprm1
UniProt: P33535 (OPRM_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.4
Assay: Compound was evaluated for binding affinity towards mu-specific opiate receptor from combinatorial peptoid library
Drug: epinephrine
Target: Beta-1 adrenergic receptor (GPCR)
Gene: Adrb1
UniProt: P18090 (ADRB1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.96
Assay: Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes
Drug: epinephrine
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P54833 (ADRB2_CANFA)
Organism: Canis familiaris
Activity: Ki = 6.18
Assay: Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
Drug: epinephrine
Target: Beta-2 adrenergic receptor (GPCR)
Gene: Adrb2
UniProt: P10608 (ADRB2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.14
Assay: Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
Drug: epinephrine
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: B0FL73 (B0FL73_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 5.52
Assay: Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
Drug: epinephrine
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 = 7.89
Assay: Binding of [3H]clonidine to alpha-2-adrenergic receptor of rat cerebral cortical membranes
Drug: epinephrine
Target: Adrenergic receptor beta (GPCR)
Gene: Adrb2|Adrb1|Adrb3
UniProt: P10608|P18090|P26255 (ADRB2_RAT|ADRB1_RAT|ADRB3_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.54
Assay: Binding affinity against Beta adrenergic receptor using [3H]dihydroalprenolol radioligand in rat brain homogenate
Drug: epinephrine
Target: M18 aspartyl aminopeptidase (Enzyme)
UniProt: Q8I2J3 (Q8I2J3_PLAF7)
Organism: Plasmodium falciparum (isolate 3D7)
Activity: IC50 = 5.52
Assay: Active
Drug: epirubicin
Target: 5-hydroxytryptamine receptor 4 (GPCR)
Gene: HTR4
UniProt: O70528 (5HT4R_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 5.878
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug: epirubicin
Target: Tyrosine-protein kinase Fyn (Kinase)
Gene: FYN
UniProt: P06241 (FYN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.286
Assay: DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: epirubicin
Target: NS3 (Enzyme)
Gene: NS3
UniProt: A3EZI9 (A3EZI9_9HEPC)
Organism: Hepatitis C virus
Activity: IC50 = 6.12
Assay: Inhibitory concentration against hepatitis C virus helicase
Drug: eplerenone
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.74
Assay: Antagonist activity at glucocorticoid receptor (unknown origin) by NH Pro assay
Drug: eplerenone
Target: Mineralocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C2
UniProt: P08235 (MCR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7
Action type: ANTAGONIST
Drug: eplerenone
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.7
Assay: Binding affinity to recombinant human progesterone receptor LBD by fluormone PL red-fluorescence polarization assay
Drug: eplerenone
Target: Mineralocorticoid receptor (Transcription factor)
Gene: Nr3c2
UniProt: P22199 (MCR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.4
Assay: Antagonist activity at gal4-fused rat mineralocorticoid receptor LBD in expressed in human U2OS cells by luciferase reporter gene assay
Drug: eplerenone
Target: Progesterone receptor (Nuclear other)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.7
Assay: Binding affinity to recombinant human progesterone receptor LBD by fluormone PL red-fluorescence polarization assay
Drug: eplerenone
Target: Mineralocorticoid receptor (Nuclear hormone receptor)
Gene: Nr3c2
UniProt: P22199 (MCR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.4
Assay: Antagonist activity at gal4-fused rat mineralocorticoid receptor LBD in expressed in human U2OS cells by luciferase reporter gene assay
Drug: epoprostenol
Target: Prostaglandin E2 receptor EP1 subtype (GPCR)
Gene: PTGER1
UniProt: P34995 (PE2R1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.8
Action type: AGONIST
Drug: epoprostenol
Target: P2Y purinoceptor 12 (GPCR)
Gene: P2RY12
UniProt: Q9H244 (P2Y12_HUMAN)
Organism: Homo sapiens
Drug: epoprostenol
Target: Prostacyclin receptor (GPCR)
Gene: PTGIR
UniProt: P43119 (PI2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.8
Action type: AGONIST
Drug: epoprostenol
Target: Prostaglandin E2 receptor EP4 subtype (GPCR)
Gene: PTGER4
UniProt: P35408 (PE2R4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.1
Action type: AGONIST
Drug: eprosartan
Target: Type-1 angiotensin II receptor (GPCR)
Gene: AGTR1
UniProt: P30556 (AGTR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.7
Action type: ANTAGONIST
Assay: Tested for Angiotensin II receptor, type 1 affinity in the absence of bovine serum albumin (BSA)
Drug: eprosartan
Target: Type-1B angiotensin II receptor (GPCR)
Gene: Agtr1b
UniProt: P29089 (AGTRB_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 9
Assay: Tested for inhibition of [125I]- AII specific binding to rat mesenteric arteries, expressed as IC50
Drug: eprosartan
Target: Type-2 angiotensin II receptor (GPCR)
Gene: Agtr2
UniProt: P35351 (AGTR2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 9
Assay: In vitro inhibition of [125I]AII specific binding towards Angiotensin II receptor in rat mesenteric membranes.
Drug: eprosartan
Target: Angiotensin II receptor (AT-1) type-1 (GPCR)
Gene: Agtr1|Agtr1b
UniProt: P25095|P29089 (AGTRA_RAT|AGTRB_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 9
Assay: Compound was tested for inhibition of 125 I-Angiotensin II specific binding to rat mesenteric arteries
Drug: eprosartan
Target: Angiotensin II receptor (GPCR)
Gene: Agtr1|Agtr1b|Agtr2
UniProt: P25095|P29089|P35351 (AGTRA_RAT|AGTRB_RAT|AGTR2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 9
Assay: Inhibition of [125I]AII binding to Angiotensin II receptor, type 1 of rat mesenteric arteries
Drug: eptifibatide
Target: Integrin alpha-IIb/beta-3 (Adhesion)
Gene: ITGB3|ITGA2B
UniProt: P05106|P08514 (ITB3_HUMAN|ITA2B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.244
Action type: INHIBITOR
Assay: platelet aggregation inhibition in plasma anticoagulated PPACK