AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: promethazine
Target: Chloroquine resistance transporter (Transporter)
Gene: CRT
UniProt: Q9N623 (CRT_PLAFA)
Organism: Plasmodium falciparum
Activity: IC50 = 4.07
Assay: Inhibition of chloroquine-resistant Plasmodium falciparum Dd2 CRT expressed in Xenopus laevis oocytes plasma membrane assessed as reduction of [3H]-chloroquine transportation after 1 to 2 hrs
Drug: promethazine
Target: FAD-linked sulfhydryl oxidase ALR (Enzyme)
Gene: GFER
UniProt: P55789 (ALR_HUMAN)
Organism: Homo sapiens
Activity: AC50 = 6.44
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: promethazine
Target: Calmodulin (Cytosolic other)
Gene: CALM
UniProt: P62157 (CALM_BOVIN)
Organism: Bos taurus
Activity: Kd = 4.3
Assay: Binding affinity to bovine brain CaM by FTPFACE analysis
Drug: promethazine
Target: Calmodulin-1 (Cytosolic other)
Gene: CALM1
UniProt: P0DP23 (CALM1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.22
Assay: Binding affinity to CaM (unknown origin) by equilibrium dialysis method
Drug: pronetalol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: Q28044 (ADRB2_BOVIN)
Organism: Bos taurus
Activity: Kd = 6.8
Assay: Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug: propafenone
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.688
Action type: ANTAGONIST
Assay: DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug: propafenone
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.444
Action type: ANTAGONIST
Assay: DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug: propafenone
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.48
Action type: BLOCKER
Assay: Inhibition of human cloned Nav1.5 channel expressed in chinese hamster CHO cells assessed as tonic inhibition after 5 mins by patch clamp assay
Drug: propafenone
Target: Sodium channel subunit beta-1 (Ion channel)
Gene: SCN1B
UniProt: Q07699 (SCN1B_HUMAN)
Organism: Homo sapiens
Drug: propafenone
Target: Sodium channel subunit beta-2 (Ion channel)
Gene: SCN2B
UniProt: O60939 (SCN2B_HUMAN)
Organism: Homo sapiens
Drug: propafenone
Target: Sodium channel subunit beta-3 (Ion channel)
Gene: SCN3B
UniProt: Q9NY72 (SCN3B_HUMAN)
Organism: Homo sapiens
Drug: propafenone
Target: Sodium channel subunit beta-4 (Ion channel)
Gene: SCN4B
UniProt: Q8IWT1 (SCN4B_HUMAN)
Organism: Homo sapiens
Drug: propafenone
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.96
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: propafenone
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.097
Drug: propafenone
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: ED50 = 7.056
Drug: propafenone
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.524
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: propafenone
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.029
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
Drug: propafenone
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.728
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: propafenone
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.237
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: propafenone
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.697
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: propafenone
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.063
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: propafenone
Target: Aldehyde oxidase (Enzyme)
Gene: AOX1
UniProt: Q06278 (AOXA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.602
Drug: propafenone
Target: Beta-3 adrenergic receptor (GPCR)
Gene: ADRB3
UniProt: P13945 (ADRB3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.498
Assay: DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug: propafenone
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.829
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: propafenone
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.337
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: propafenone
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.604
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: propafenone
Target: Cytochrome P450 1A2 (Enzyme)
Gene: CYP1A2
UniProt: P05177 (CP1A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.483
Assay: DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: propafenone
Target: Potassium channel subfamily K member 2 (Ion channel)
Gene: KCNK2
UniProt: O95069 (KCNK2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.12
Assay: Inhibition of of human TREK1 expressed in CHO cells assessed as reduction in channel currents
Drug: propafenone
Target: Potassium voltage-gated channel subfamily A member 5 (Ion channel)
Gene: KCNA5
UniProt: P22460 (KCNA5_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.4
Action type: BLOCKER
Drug: propafenone
Target: Potassium channel subfamily K member 3 (Ion channel)
Gene: KCNK3
UniProt: O14649 (KCNK3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.29
Assay: Inhibition of of TASK1 (unknown origin) expressed in CHO cells assessed as reduction in channel currents
Drug: propafenone
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.95
Assay: Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Drug: propafenone
Target: Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (Ion channel)
Gene: HCN4
UniProt: Q9Y3Q4 (HCN4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.845
Drug: propafenone
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.849
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: propafenone
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.21
Drug: propafenone
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.79
Drug: propafenone
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.602
Drug: propafenone
Target: Sulfonylurea receptor 2, Kir6.2 (Ion channel)
Gene: ABCC9|KCNJ11
UniProt: O60706|Q14654 (ABCC9_HUMAN|KCJ11_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.66
Assay: Inhibition of human kir6.2/SUR2A ion channel coexpressed in human HEK293 cells after 5 mins by patch clamp assay
Drug: propantheline
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.7
Action type: ANTAGONIST
Drug: propantheline
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.5
Action type: ANTAGONIST
Drug: propantheline
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 10
Action type: ANTAGONIST
Drug: propantheline
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 10.2
Action type: ANTAGONIST
Drug: proparacaine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: proparacaine
Target: Amine oxidase [flavin-containing] A (Enzyme)
Gene: MAOA
UniProt: P21397 (AOFA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.75
Assay: DRUGMATRIX: Monoamine Oxidase MAO-A enzyme inhibition (substrate: Kynuramine)
Drug: proparacaine
Target: Sodium channel protein type 10 subunit alpha (Ion channel)
Gene: SCN10A
UniProt: Q9Y5Y9 (SCNAA_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: proparacaine
Target: Sodium channel alpha subunits; brain (Types I, II, III) (Ion channel)
Gene: SCN1A|SCN2A|SCN3A
UniProt: P35498|Q99250|Q9NY46 (SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.72
Action type: BLOCKER
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: propentofylline
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P22303 (ACES_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.19
Assay: Inhibition of human AChE using acetylthiocholine iodide as substrate treated 5 mins before substrate addition measured up to 4 mins by Ellman's method
Drug: propiomazine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Drug: propiomazine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Drug: propiomazine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Drug: propiomazine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Drug: propiomazine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Drug: propiomazine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Drug: propiomazine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Drug: propiomazine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Drug: propiomazine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Drug: propiomazine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Drug: propiomazine
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Drug: propiomazine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Drug: propiram
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action
Drug: propofol
Target: Fatty-acid amide hydrolase 1 (Enzyme)
Gene: FAAH
UniProt: O00519 (FAAH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.284
Drug: propofol
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.417
Assay: DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid)
Drug: propofol
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.031
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: propofol
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.456
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: propofol
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.218
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: propofol
Target: Carbonic anhydrase 2 (Enzyme)
Gene: CA2
UniProt: P00918 (CAH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.005
Drug: propofol
Target: Carbonic anhydrase 1 (Enzyme)
Gene: CA1
UniProt: P00915 (CAH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.71
Drug: propofol
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.91
Drug: propofol
Target: Arachidonate 15-lipoxygenase (Enzyme)
Gene: ALOX15
UniProt: P12530 (LOX15_RABIT)
Organism: Oryctolagus cuniculus
Activity: IC50 = 5.119
Assay: DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid)
Drug: propofol
Target: Fatty-acid amide hydrolase 1 (Enzyme)
Gene: Faah
UniProt: P97612 (FAAH1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.85
Assay: Inhibition of rat FAAH
Drug: propofol
Target: Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 1 (Ion channel)
Gene: Hcn1
UniProt: O88704 (HCN1_MOUSE)
Organism: Mus musculus
Activity: IC50 = 5.2
Action type: BLOCKER
Drug: propofol
Target: GABA-A receptor alpha-1/beta-2/gamma-2 (Ion channel)
Gene: GABRA1|GABRG2|GABRB2
UniProt: P14867|P18507|P47870 (GBRA1_HUMAN|GBRG2_HUMAN|GBRB2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.7
Action type: POSITIVE ALLOSTERIC MODULATOR
Assay: Potentiation of GABA responses at human Gamma-aminobutyric acid A receptor alpha-1-beta-2-gamma-2
Drug: propofol
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: EC50 = 5.39
Action type: POSITIVE ALLOSTERIC MODULATOR
Assay: GABA-modulatory action compound was evaluated on Oocytes expressing recombinant human alpha-1-beta-3-gamma-2L GABA A receptor at concentrations of >=100 micro<M
Drug: propofol
Target: GABA-A receptor; anion channel (Ion channel)
Gene: Gabrp|Gabrb1|Gabrd|Gabrg2|Gabra5|Gabra3|Gabrg1|Gabra2|Gabra4|Gabrg3|Gabra6|Gabra1|Gabrb3|Gabrb2|Gabrq|Gabre
UniProt: O09028|P15431|P18506|P18508|P19969|P20236|P23574|P23576|P28471|P28473|P30191|P62813|P63079|P63138|Q91ZM7|Q9ES14 (GBRP_RAT|GBRB1_RAT|GBRD_RAT|GBRG2_RAT|GBRA5_RAT|GBRA3_RAT|GBRG1_RAT|GBRA2_RAT|GBRA4_RAT|GBRG3_RAT|GBRA6_RAT|GBRA1_RAT|GBRB3_RAT|GBRB2_RAT|Q91ZM7_RAT|GBRE_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.4
Assay: Inhibition of [35S]TBPS binding to GABA-A receptor in rat cerebral cortex.
Drug: propofol
Target: GABA A receptor alpha-2/beta-2/gamma-2 (Ion channel)
Gene: GABRG2|GABRA2|GABRB2
UniProt: P18507|P47869|P47870 (GBRG2_HUMAN|GBRA2_HUMAN|GBRB2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.95
Action type: POSITIVE ALLOSTERIC MODULATOR
Assay: Effective concentration against GABA-evoked chloride currents mediated by human Gamma-aminobutyric acid GABA-A receptor alpha2-beta2-gamma2L expressed in Xenopus oocytes
Drug: propranolol
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.919
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: propranolol
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.32
Assay: High affinity constant at binding site of human P-Glycoprotein (P-gp) in two-affinity model
Drug: propranolol
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.695
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: propranolol
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.913
Drug: propranolol
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.378
Drug: propranolol
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.662
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: propranolol
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.92
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: propranolol
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.847
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: propranolol
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.699
Drug: propranolol
Target: Beta-3 adrenergic receptor (GPCR)
Gene: ADRB3
UniProt: P13945 (ADRB3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.22
Action type: ANTAGONIST
Drug: propranolol
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.197
Drug: propranolol
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.346
Drug: propranolol
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: propranolol
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: CACNA1C
UniProt: Q13936 (CAC1C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.319
Drug: propranolol
Target: Cytochrome P450 1A2 (Enzyme)
Gene: CYP1A2
UniProt: P05177 (CP1A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.398
Assay: DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: propranolol
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.2
Assay: Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Drug: propranolol
Target: Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (Ion channel)
Gene: HCN4
UniProt: Q9Y3Q4 (HCN4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.297
Drug: propranolol
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.3
Assay: Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
Drug: propranolol
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.671
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: propranolol
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.89
Assay: Inhibitory constant against binding of [125I]- IBZM to D2 receptor in rat striatal membrane
Drug: propranolol
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.05
Assay: Inhibitory activity against 5-hydroxytryptamine 1A receptor of rat hippocampal tissue using [3H]OH-DPAT as radioligand.
Drug: propranolol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: Adrb2
UniProt: Q8K4Z4 (ADRB2_CAVPO)
Organism: Cavia porcellus
Activity: Kd = 9.01
Assay: In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
Drug: propranolol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: Q28044 (ADRB2_BOVIN)
Organism: Bos taurus
Activity: Kd = 9.05
Assay: Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug: propranolol
Target: Beta-1 adrenergic receptor (GPCR)
Gene: Adrb1
UniProt: P18090 (ADRB1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.52
Assay: Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
Drug: propranolol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P54833 (ADRB2_CANFA)
Organism: Canis familiaris
Activity: IC50 = 7.77
Assay: Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
Drug: propranolol
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: B0FL73 (B0FL73_CAVPO)
Organism: Cavia porcellus
Activity: Kd = 8.76
Assay: In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug: propranolol
Target: Adrenergic receptor beta (GPCR)
Gene: Adrb2|Adrb1|Adrb3
UniProt: P10608|P18090|P26255 (ADRB2_RAT|ADRB1_RAT|ADRB3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.62
Assay: Inhibitory activity against beta adrenergic receptor of rat frontal cortex homogenate using (1.0 nM) [3H]- dihydroalprenolol
Drug: propranolol
Target: Beta-3 adrenergic receptor (GPCR)
Gene: Adrb3
UniProt: P25962 (ADRB3_MOUSE)
Organism: Mus musculus
Activity: Ki = 6.6
Action type: ANTAGONIST
Drug: propranolol
Target: Beta-1 adrenergic receptor (GPCR)
Gene: Adrb1
UniProt: P34971 (ADRB1_MOUSE)
Organism: Mus musculus
Activity: Ki = 8.62
Assay: Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug: propranolol
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.71
Action type: ANTAGONIST
Drug: propranolol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.25
Action type: ANTAGONIST
Drug: propylthiouracil
Target: Thyroid peroxidase (Enzyme)
Gene: TPO
UniProt: P07202 (PERT_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.06
Action type: INHIBITOR
Drug: propylthiouracil
Target: Myeloperoxidase (Enzyme)
Gene: MPO
UniProt: P05164 (PERM_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.55
Drug: propylthiouracil
Target: Type I iodothyronine deiodinase (Enzyme)
Gene: DIO1
UniProt: P49895 (IOD1_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2019; SINGLE PROTEIN