AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: metoclopramide
Target: Myeloperoxidase (Enzyme)
Gene: MPO
UniProt: P05164 (PERM_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.46
Assay: Inhibition of recombinant MPO (unknown origin) assessed as reduction in taurine chloramine production preincubated with enzyme and taurine followed by H2O2 addition measured after 5 mins
Drug: metoclopramide
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.02
Assay: Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Drug: metoclopramide
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.98
Assay: Compound was evaluated for binding affinity towards DA D-2 receptor using radioligand [3H]SPI
Drug: metoclopramide
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P20288 (DRD2_BOVIN)
Organism: Bos taurus
Activity: Ki = 7.1
Assay: Compound was evaluated for the binding affinity at Dopamine receptor D2
Drug: metoclopramide
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61168 (DRD2_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.54
Action type: ANTAGONIST
Drug: metoclopramide
Target: 5-hydroxytryptamine receptor 4 (GPCR)
Gene: Htr4
UniProt: Q62758 (5HT4R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.05
Assay: Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
Drug: metoclopramide
Target: D(3) dopamine receptor (GPCR)
Gene: Drd3
UniProt: P19020 (DRD3_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.21
Assay: Concentration of compound required to inhibit the binding of radioligand [3H](R)-7-OH-DPAT to Dopamine receptor D3 in rat striatum
Drug: metoclopramide
Target: Serotonin 3 (5-HT3) receptor (Ion channel)
Gene: Htr3a|Htr3b
UniProt: P35563|Q9JJ16 (5HT3A_RAT|5HT3B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.68
Assay: Inhibition of [3H]GR-65630 binding to rat cortical membrane serotonin 5-hydroxytryptamine 3 receptor
Drug: metoclopramide
Target: Serotonin 3 (5-HT3) receptor (Ion channel)
Gene: HTR3E|HTR3B|HTR3A|HTR3D|HTR3C
UniProt: A5X5Y0|O95264|P46098|Q70Z44|Q8WXA8 (5HT3E_HUMAN|5HT3B_HUMAN|5HT3A_HUMAN|5HT3D_HUMAN|5HT3C_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.3
Assay: Potency at neuronal 5-hydroxytryptamine 3 receptors in the rabbit heart
Drug: metoclopramide
Target: Serotonin 1 (5-HT1) receptor (GPCR)
Gene: Htr1a|Htr1b|Htr1d|Htr1f
UniProt: P19327|P28564|P28565|P30940 (5HT1A_RAT|5HT1B_RAT|5HT1D_RAT|5HT1F_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.11
Assay: Inhibitory activity against 5-hydroxytryptamine 1 receptor by 3H ligand binding experiments.
Drug: metoclopramide
Target: Adrenergic receptor alpha-2 (GPCR)
Gene: Adra2b|Adra2c|Adra2a
UniProt: P19328|P22086|P22909 (ADA2B_RAT|ADA2C_RAT|ADA2A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.11
Assay: Inhibitory activity against alpha-2 adrenergic receptor by 3H ligand binding experiments.
Drug: metoclopramide
Target: Adrenergic receptor alpha-1 (GPCR)
Gene: Adra1b|Adra1d|Adra1a
UniProt: P15823|P23944|P43140 (ADA1B_RAT|ADA1D_RAT|ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.48
Assay: Inhibitory activity against Alpha-1 adrenergic receptor by 3H ligand binding experiments.
Drug: metoclopramide
Target: Serotonin 2 (5-HT2) receptor (GPCR)
Gene: Htr2c|Htr2a|Htr2b
UniProt: P08909|P14842|P30994 (5HT2C_RAT|5HT2A_RAT|5HT2B_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.88
Assay: Inhibitory activity against 5-hydroxytryptamine 2 receptor by 3H ligand binding experiments.
Drug: metoclopramide
Target: Serotonin 3 receptor (5HT3) (Ion channel)
Gene: Htr3a|Htr3b
UniProt: P23979|Q9JHJ5 (5HT3A_MOUSE|5HT3B_MOUSE)
Organism: Mus musculus
Activity: Ki = 6.7
Assay: Compound was evaluated for the binding affinity at 5- HT3 receptor subtype
Drug: metoclopramide
Target: 5-hydroxytryptamine receptor 4 (GPCR)
Gene: Htr4
UniProt: P97288 (5HT4R_MOUSE)
Organism: Mus musculus
Activity: Ki = 6
Action type: AGONIST
Drug: metolazone
Target: Solute carrier family 12 member 1 (Transporter)
Gene: SLC12A1
UniProt: Q13621 (S12A1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.45
Drug: metolazone
Target: Solute carrier family 12 member 3 (Transporter)
Gene: SLC12A3
UniProt: P55017 (S12A3_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL1876; SINGLE PROTEIN
Drug: metolazone
Target: Carbonic anhydrase 7 (Enzyme)
Gene: CA7
UniProt: P43166 (CAH7_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.68
Assay: Inhibition of human recombinant carbonic anhydrase 7 preincubated for 15 mins by stopped flow CO2 hydration assay
Drug: metopimazine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 10.15
Assay: Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.
Drug: metopimazine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.21
Assay: Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.
Drug: metopimazine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.08
Assay: Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.
Drug: metoprolol
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.6
Action type: ANTAGONIST
Drug: metoprolol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.3
Drug: metoprolol
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5
Drug: metoprolol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: Adrb2
UniProt: Q8K4Z4 (ADRB2_CAVPO)
Organism: Cavia porcellus
Activity: Kd = 6.79
Assay: In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
Drug: metoprolol
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: B0FL73 (B0FL73_CAVPO)
Organism: Cavia porcellus
Activity: Kd = 7.83
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: metoprolol
Target: Adrenergic receptor beta (GPCR)
Gene: Adrb2|Adrb1|Adrb3
UniProt: P10608|P18090|P26255 (ADRB2_RAT|ADRB1_RAT|ADRB3_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.3
Assay: The compound was tested for its ability to inhibit (-)-[3H]dihydroalprenolol binding to beta-adrenergic receptor sites in rat cortex
Drug: metoprolol
Target: Beta-1 adrenergic receptor (GPCR)
Gene: Adrb1
UniProt: P34971 (ADRB1_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.31
Assay: Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug: metronidazole
Target: Thioredoxin reductase (Enzyme)
UniProt: C4LW95 (C4LW95_ENTHI)
Organism: Entamoeba histolytica
Activity: Ki = 5.48
Assay: Inhibition of Entamoeba histolytica thioredoxin reductase
Drug: metyrapone
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.097
Assay: DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin)
Drug: metyrapone
Target: Cytochrome P450 11B2, mitochondrial (Enzyme)
Gene: CYP11B2
UniProt: P19099 (C11B2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.38
Assay: Inhibition of human CYP11B2 expressed in hamster V79MZh cells using [1,2-3H]-11-deoxycorticosterone as substrate
Drug: metyrapone
Target: Cytochrome P450 11B1 (Enzyme)
Gene: CYP11B1
UniProt: P15150 (C11B1_BOVIN)
Organism: Bos taurus
Activity: Ki = 6.24
Assay: Inhibition of bovine adrenal gland 11beta-hydroxylase assessed as inhibition of [14C]-deoxycorticosterone hydroxylation
Drug: metyrapone
Target: Cytochrome P450 11B1, mitochondrial (Enzyme)
Gene: Cyp11b1
UniProt: P15393 (C11B1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.34
Drug: metyrapone
Target: Cytochrome P450 11B1, mitochondrial (Enzyme)
Gene: CYP11B1
UniProt: P15538 (C11B1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.84
Action type: INHIBITOR
Assay: Inhibition of human steroid-11beta-hydroxylase expressed in chinese hamster V79 cells using 11-deoxycorticosterone as substrate
Drug: metirosine
Target: Tyrosine 3-monooxygenase (Enzyme)
Gene: TH
UniProt: P07101 (TY3H_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Drug: mexiletine
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.53
Action type: BLOCKER
Drug: mexiletine
Target: Sodium channel subunit beta-1 (Ion channel)
Gene: SCN1B
UniProt: Q07699 (SCN1B_HUMAN)
Organism: Homo sapiens
Drug: mexiletine
Target: Sodium channel subunit beta-2 (Ion channel)
Gene: SCN2B
UniProt: O60939 (SCN2B_HUMAN)
Organism: Homo sapiens
Drug: mexiletine
Target: Sodium channel subunit beta-3 (Ion channel)
Gene: SCN3B
UniProt: Q9NY72 (SCN3B_HUMAN)
Organism: Homo sapiens
Drug: mexiletine
Target: Sodium channel subunit beta-4 (Ion channel)
Gene: SCN4B
UniProt: Q8IWT1 (SCN4B_HUMAN)
Organism: Homo sapiens
Drug: mexiletine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5
Assay: Inhibition of human ERG
Drug: mexiletine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.14
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: mexiletine
Target: Sodium channel protein type 1 subunit alpha (Ion channel)
Gene: SCN1A
UniProt: P35498 (SCN1A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.96
Drug: mexiletine
Target: Sodium channel protein type 2 subunit alpha (Ion channel)
Gene: SCN2A
UniProt: Q99250 (SCN2A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.54
Action type: BLOCKER
Assay: Inhibition of human recombinant Nav1.2 channel expressed in HEK293 cells by whole cell voltage clamp technique
Drug: mexiletine
Target: Sodium channel protein type 4 subunit alpha (Ion channel)
Gene: SCN4A
UniProt: P35499 (SCN4A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.38
Action type: BLOCKER
Drug: mexiletine
Target: Sodium channel protein type 9 subunit alpha (Ion channel)
Gene: SCN9A
UniProt: Q15858 (SCN9A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.89
Action type: BLOCKER
Assay: Binding affinity to inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay
Drug: mexiletine
Target: Sodium channel protein type 10 subunit alpha (Ion channel)
Gene: SCN10A
UniProt: Q9Y5Y9 (SCNAA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.25
Action type: BLOCKER
Assay: Inhibition of human recombinant Nav1.8 channel expressed in HEK293 cells by whole cell voltage clamp technique
Drug: mexiletine
Target: Potassium channel subfamily K member 3 (Ion channel)
Gene: KCNK3
UniProt: O14649 (KCNK3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.01
Assay: Inhibition of of TASK1 (unknown origin) expressed in CHO cells assessed as reduction in channel currents
Drug: mexiletine
Target: Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (Ion channel)
Gene: HCN4
UniProt: Q9Y3Q4 (HCN4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 3.51
Drug: mexiletine
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.26
Drug: mexiletine
Target: Sodium channel protein type X alpha subunit (Ion channel)
Gene: Scn10a
UniProt: Q62968 (SCNAA_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.51
Assay: Blockade of Nav1.8 channel in rat dorsal root ganglion neurons assessed as inhibition of TTX-R current by whole cell patch clamp technique
Drug: mexiletine
Target: Sodium channel protein type 9 subunit alpha (Ion channel)
Gene: Scn9a
UniProt: Q62205 (SCN9A_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4.96
Drug: mexiletine
Target: Sodium channel protein type 1 subunit alpha (Ion channel)
Gene: Scn1a
UniProt: A2APX8 (SCN1A_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4.68
Assay: Inhibition of mouse NaV1.1 by IonWorks quattro automated electrophysiology assay
Drug: mezlocillin
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.22
Drug: mezlocillin
Target: Cannabinoid receptor 1 (GPCR)
Gene: CNR1
UniProt: P21554 (CNR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4
Drug: mezlocillin
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.41
Drug: mezlocillin
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.17
Drug: mezlocillin
Target: Penicillin-binding protein 1A (Enzyme)
Gene: pbpA
UniProt: Q8XJ01 (PBPA_CLOPE)
Organism: Clostridium perfringens (strain 13 / Type A)
Drug: mezlocillin
Target: Prostaglandin E2 receptor EP1 subtype (GPCR)
Gene: PTGER1
UniProt: P34995 (PE2R1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.33
Drug: mezlocillin
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.89
Drug: mezlocillin
Target: Carbonic anhydrase 2 (Enzyme)
Gene: CA2
UniProt: P00918 (CAH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5
Drug: mezlocillin
Target: Multidrug resistance-associated protein 1 (Transporter)
Gene: ABCC1
UniProt: P33527 (MRP1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.92
Drug: mezlocillin
Target: Cytochrome P450 2C8 (Enzyme)
Gene: CYP2C8
UniProt: P10632 (CP2C8_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.74
Drug: mezlocillin
Target: Prostaglandin D2 receptor 2 (GPCR)
Gene: PTGDR2
UniProt: Q9Y5Y4 (PD2R2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.26
Drug: mezlocillin
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.72
Drug: mezlocillin
Target: Aldose reductase (Enzyme)
Gene: AKR1B1
UniProt: P15121 (ALDR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.34
Drug: mezlocillin
Target: Prostaglandin E2 receptor EP3 subtype (GPCR)
Gene: PTGER3
UniProt: P43115 (PE2R3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.33
Drug: mezlocillin
Target: Aldo-keto reductase family 1 member C3 (Enzyme)
Gene: AKR1C3
UniProt: P42330 (AK1C3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.12
Drug: mezlocillin
Target: Arachidonate 5-lipoxygenase (Enzyme)
Gene: ALOX5
UniProt: P09917 (LOX5_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.01
Drug: mezlocillin
Target: Peroxisome proliferator-activated receptor gamma (Nuclear hormone receptor)
Gene: PPARG
UniProt: P37231 (PPARG_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.3
Drug: mezlocillin
Target: Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A (Enzyme)
Gene: PDE11A
UniProt: Q9HCR9 (PDE11_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.13
Drug: mezlocillin
Target: Prostaglandin E2 receptor EP2 subtype (GPCR)
Gene: PTGER2
UniProt: P43116 (PE2R2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.68
Drug: mezlocillin
Target: Prostaglandin E2 receptor EP4 subtype (GPCR)
Gene: PTGER4
UniProt: P35408 (PE2R4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.33
Drug: mezlocillin
Target: Prostaglandin D2 receptor (GPCR)
Gene: PTGDR
UniProt: Q13258 (PD2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.92
Drug: mezlocillin
Target: Cannabinoid receptor 2 (GPCR)
Gene: CNR2
UniProt: P34972 (CNR2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.2
Drug: mezlocillin
Target: Thromboxane-A synthase (Enzyme)
Gene: TBXAS1
UniProt: P24557 (THAS_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.25
Drug: mezlocillin
Target: Serum albumin (Secreted)
Gene: ALB
UniProt: P02768 (ALBU_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.18
Drug: mezlocillin
Target: Interleukin-8 (Cytokine)
Gene: CXCL8
UniProt: P10145 (IL8_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.3
Drug: mezlocillin
Target: Interleukin-1 receptor type 1 (Membrane receptor)
Gene: IL1R1
UniProt: P14778 (IL1R1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.52
Drug: mezlocillin
Target: Prostaglandin-H2 D-isomerase (Enzyme)
Gene: PTGDS
UniProt: P41222 (PTGDS_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.3
Drug: mezlocillin
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: mianserin
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6
Drug: mianserin
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.66
Assay: Inhibition of [3H]-spiperone binding to human Dopamine receptor D2
Drug: mianserin
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.319
Drug: mianserin
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.398
Drug: mianserin
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.149
Drug: mianserin
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.13
Drug: mianserin
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.17
Action type: ANTAGONIST
Drug: mianserin
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.12
Action type: ANTAGONIST
Drug: mianserin
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.52
Action type: ANTAGONIST
Drug: mianserin
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.175
Drug: mianserin
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.06
Drug: mianserin
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.39
Assay: Binding affinity for human cloned Alpha-1A adrenergic receptor
Drug: mianserin
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.569
Drug: mianserin
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.55
Assay: Inhibition of [125I]iodosulpiride binding to human Dopamine receptor D3
Drug: mianserin
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.245
Drug: mianserin
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.003
Assay: DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug: mianserin
Target: Histamine H4 receptor (GPCR)
Gene: HRH4
UniProt: Q9H3N8 (HRH4_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.125
Drug: mianserin
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.465
Assay: DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: mianserin
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.417
Assay: DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: mianserin
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.526
Assay: DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: mianserin
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.541
Assay: DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: mianserin
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.638
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: mianserin
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.53
Drug: mianserin
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.99
Drug: mianserin
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.42
Drug: mianserin
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.027
Drug: mianserin
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.48
Assay: Binding affinity for human cloned Dopamine receptor D4
Drug: mianserin
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.5
Action type: ANTAGONIST
Drug: mianserin
Target: 5-hydroxytryptamine receptor 3A (Ion channel)
Gene: HTR3A
UniProt: P46098 (5HT3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.21
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT3 radioligand binding (ligand: [3H] GR-65630)
Drug: mianserin
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.4
Action type: ANTAGONIST
Drug: mianserin
Target: 5-hydroxytryptamine receptor 1F (GPCR)
Gene: HTR1F
UniProt: P30939 (5HT1F_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.06
Drug: mianserin
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.18
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: mianserin
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.33
Assay: Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.