AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: amiodarone
Target: Lysine-specific demethylase PHF2 (Enzyme)
Gene: PHF2
UniProt: O75151 (PHF2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.08
Assay: Displacement of C-terminally biotinylated-H3K4me3 (1 to 21 residues) peptide from KDM7C (PHD) (unknown origin) preincubated for 15 mins followed by peptide addition measured after 1 hr by luminescence-based AlphaScreen assay
Drug: amiodarone
Target: Lysine-specific demethylase 5A (Enzyme)
Gene: KDM5A
UniProt: P29375 (KDM5A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4
Assay: Displacement of C-terminally biotinylated-H3K4me3 (1 to 21 residues) peptide from recombinant His6-tagged human KDM5A (PHD3) (1542 to 1660 residues) expressed in Escherichia coli 2(DE3)pLysS Rosetta competent cells preincubated for 15 mins followed by peptide addition measured after 1 hr by luminescence-based AlphaScreen assay
Drug: amiodarone
Target: Lysine-specific demethylase 7A (Enzyme)
Gene: KDM7A
UniProt: Q6ZMT4 (KDM7A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.1
Assay: Displacement of C-terminally biotinylated-H3K4me3 (1 to 21 residues) peptide from KDM7A (PHD-JmjC) (unknown origin) preincubated for 15 mins followed by peptide addition measured after 1 hr by luminescence-based AlphaScreen assay
Drug: amisulpride
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.953
Drug: amisulpride
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.081
Drug: amisulpride
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki  7.886
Drug: amisulpride
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.382
Drug: amisulpride
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki  7.939
Drug: amisulpride
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.758
Drug: amisulpride
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.873
Drug: amisulpride
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.812
Drug: amisulpride
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.625
Drug: amisulpride
Target: D(3) dopamine receptor (GPCR)
Gene: Drd3
UniProt: P19020 (DRD3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.4
Action type: ANTAGONIST
Drug: amisulpride
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.553
Action type: ANTAGONIST
Drug: amisulpride
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.495
Action type: ANTAGONIST
Drug: amitriptyline
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.8
Assay: Inhibition of human NaV1.5 alpha subunit expressed in CHOK1 cells at -90 mV holding potential by patch clamp electrophysiological assay
Drug: amitriptyline
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.051
Drug: amitriptyline
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.708
Drug: amitriptyline
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.879
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: amitriptyline
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.25
Drug: amitriptyline
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5
Drug: amitriptyline
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.367
Action type: INHIBITOR
Drug: amitriptyline
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.456
Action type: INHIBITOR
Drug: amitriptyline
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.721
Drug: amitriptyline
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.96
Drug: amitriptyline
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.4
Drug: amitriptyline
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.1
Drug: amitriptyline
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.05
Drug: amitriptyline
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.4
Drug: amitriptyline
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.9
Drug: amitriptyline
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8
Drug: amitriptyline
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.686
Drug: amitriptyline
Target: D(1B) dopamine receptor (GPCR)
Gene: DRD5
UniProt: P21918 (DRD5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.77
Drug: amitriptyline
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.3
Action type: ANTAGONIST
Drug: amitriptyline
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.8
Drug: amitriptyline
Target: Histamine H4 receptor (GPCR)
Gene: HRH4
UniProt: Q9H3N8 (HRH4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.14
Drug: amitriptyline
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.83
Action type: ANTAGONIST
Drug: amitriptyline
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.1
Drug: amitriptyline
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.89
Drug: amitriptyline
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.14
Drug: amitriptyline
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.8
Drug: amitriptyline
Target: Aldehyde oxidase (Enzyme)
Gene: AOX1
UniProt: Q06278 (AOXA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.585
Drug: amitriptyline
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.066
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: amitriptyline
Target: Sodium channel protein type 2 subunit alpha (Ion channel)
Gene: SCN2A
UniProt: Q99250 (SCN2A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.51
Assay: Inhibition of human NaV1.2 alpha subunit expressed in CHOK1 cells at -65 mV holding potential by patch clamp electrophysiological assay
Drug: amitriptyline
Target: Sodium channel protein type 9 subunit alpha (Ion channel)
Gene: SCN9A
UniProt: Q15858 (SCN9A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Assay: Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -65 mV holding potential by patch clamp electrophysiological assay
Drug: amitriptyline
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.21
Assay: Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay
Drug: amitriptyline
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.252
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: amitriptyline
Target: Proto-oncogene tyrosine-protein kinase receptor Ret (Kinase)
Gene: RET
UniProt: P07949 (RET_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Drug: amitriptyline
Target: High affinity nerve growth factor receptor (Kinase)
Gene: NTRK1
UniProt: P04629 (NTRK1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.22
Drug: amitriptyline
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.77
Assay: Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Drug: amitriptyline
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.377
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: amitriptyline
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.771
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug: amitriptyline
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 10.7
Assay: Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug: amitriptyline
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.7
Drug: amitriptyline
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: Slc6a4
UniProt: P31652 (SC6A4_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.07
Assay: In vitro inhibition of [14C]5-HT transporter uptake by rat brain slices
Drug: amitriptyline
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: Htr2a
UniProt: P14842 (5HT2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.4
Action type: ANTAGONIST
Drug: amitriptyline
Target: Transporter (Transporter)
Gene: Slc6a2
UniProt: Q9WTR4 (Q9WTR4_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.6
Assay: Inhibition of the NE [3H]norepinephrine uptake by rat brain slices In vitro
Drug: amitriptyline
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32305 (5HT7R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7
Action type: ANTAGONIST
Drug: amitriptyline
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32304 (5HT7R_MOUSE)
Organism: Mus musculus
Activity: Ki = 6.4
Action type: ANTAGONIST
Drug: amitriptyline
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: Htr2c
UniProt: P08909 (5HT2C_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.1
Action type: ANTAGONIST
Drug: amitriptyline
Target: Histamine H1 receptor (GPCR)
Gene: Hrh1
UniProt: P31390 (HRH1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 10.7
Assay: Compound tested for its inhibitory activity against Histamine H1 receptor
Drug: amitriptyline
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: Htr6
UniProt: P31388 (5HT6R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.2
Action type: ANTAGONIST
Drug: amitriptyline
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.854
Drug: amitriptyline
Target: Muscarinic acetylcholine receptor (GPCR)
Gene: Chrm1|Chrm3|Chrm4|Chrm5|Chrm2
UniProt: P08482|P08483|P08485|P08911|P10980 (ACM1_RAT|ACM3_RAT|ACM4_RAT|ACM5_RAT|ACM2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.52
Assay: Inhibition of radioligand [3H]QNB binding to muscarinic acetylcholine receptor in the rat forebrain in the presence of zinc
Drug: amitriptyline
Target: G protein-activated inward rectifier potassium channel 2 (Ion channel)
Gene: Kcnj6
UniProt: P48542 (KCNJ6_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4
Action type: BLOCKER
Drug: amitriptylinoxide
Target: Proto-oncogene tyrosine-protein kinase receptor Ret (Kinase)
Gene: RET
UniProt: P07949 (RET_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5
Drug: amlexanox
Target: Inhibitor of nuclear factor kappa-B kinase subunit epsilon (Kinase)
Gene: IKBKE
UniProt: Q14164 (IKKE_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Action type: INHIBITOR
Assay: Inhibition of substrate phosphorylation.
Drug: amlexanox
Target: Serine/threonine-protein kinase TBK1 (Kinase)
Gene: TBK1
UniProt: Q9UHD2 (TBK1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Action type: INHIBITOR
Assay: Inhibition of substrate phosphorylation.
Drug: amlexanox
Target: G-protein coupled receptor 35 (GPCR)
Gene: GPR35
UniProt: Q9HC97 (GPR35_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.4
Assay: Agonist activity at human GPR35 expressed in CHO-K1 cells after 90 mins by beta-arrestin 2 recruitment assay
Drug: amlexanox
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
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2093863; PROTEIN FAMILY
Drug: amlodipine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.646
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: amlodipine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.871
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: amlodipine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.63
Assay: Binding affinity against human Alpha-1a adrenergic receptor
Drug: amlodipine
Target: Aldehyde oxidase (Enzyme)
Gene: AOX1
UniProt: Q06278 (AOXA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.26
Drug: amlodipine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.583
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: amlodipine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.358
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: amlodipine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.27
Assay: Binding affinity against human Alpha-1d adrenergic receptor
Drug: amlodipine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.1
Assay: Binding affinity against human Alpha-1b adrenergic receptor
Drug: amlodipine
Target: Voltage-dependent calcium channel gamma-1 subunit (Ion channel)
Gene: CACNG1
UniProt: Q06432 (CCG1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.2
Drug: amlodipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: CACNA1C
UniProt: Q13936 (CAC1C_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: amlodipine
Target: Carbonic anhydrase 1 (Enzyme)
Gene: CA1
UniProt: P00915 (CAH1_HUMAN)
Organism: Homo sapiens
Drug: amlodipine
Target: Voltage-dependent calcium channel subunit alpha-2/delta-1 (Ion channel)
Gene: CACNA2D1
UniProt: P54289 (CA2D1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.2
Drug: amlodipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1D (Ion channel)
Gene: CACNA1D
UniProt: Q01668 (CAC1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7
Action type: BLOCKER
Drug: amlodipine
Target: Voltage-dependent T-type calcium channel subunit alpha-1H (Ion channel)
Gene: CACNA1H
UniProt: O95180 (CAC1H_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.507
Drug: amlodipine
Target: Potassium channel subfamily K member 2 (Ion channel)
Gene: KCNK2
UniProt: O95069 (KCNK2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.4
Assay: Inhibition of TREK-1 (unknown origin)
Drug: amlodipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: Cacna1c
UniProt: P22002 (CAC1C_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.7
Assay: Binding affinity against rat L-type calcium channel
Drug: amlodipine
Target: Potassium channel subfamily K member 2 (Ion channel)
Gene: Kcnk2
UniProt: Q8HY88 (Q8HY88_BOVIN)
Organism: Bos taurus
Activity: IC50 = 6.37
Assay: Activation of bovine TREK1 expressed in AZT cells assessed as reduction in channel currents
Drug: amodiaquine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.62
Assay: Inhibition of human cloned ERG
Drug: amodiaquine
Target: Histamine N-methyltransferase (Enzyme)
Gene: HNMT
UniProt: P50135 (HNMT_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.72
Assay: Inhibition of histamine N-methyltransferase by radiochemical assay
Drug: amodiaquine
Target: Heparanase (Enzyme)
Gene: HPSE
UniProt: Q9Y251 (HPSE_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.28
Assay: Binding affinity to recombinant heparanase catalytic stie (unknown origin) expressed in Escherichia coli BL21 (DE3) by surface plasmon resonance assay
Drug: amodiaquine
Target: Amyloid beta A4 protein (Unclassified)
Gene: APP
UniProt: P05067 (A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.4
Assay: Modulation of human wild-type APP695 expressed in SH-SY5Y cells assessed as inhibition of amyloid beta (1 to 40 residues) production measured after 24 hrs
Drug: amoxapine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.708
Assay: DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug: amoxapine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.796
Drug: amoxapine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.307
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: amoxapine
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Drug: amoxapine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.469
Action type: INHIBITOR
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: amoxapine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.886
Action type: INHIBITOR
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: amoxapine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.66
Assay: Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug: amoxapine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.75
Assay: Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug: amoxapine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.182
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: amoxapine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.7
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: amoxapine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.3
Action type: ANTAGONIST
Drug: amoxapine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.3
Assay: Binding affinity towards human 5-hydroxytryptamine 7 receptor
Drug: amoxapine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.593
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: amoxapine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.734
Drug: amoxapine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.959
Assay: DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug: amoxapine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.542
Assay: DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: amoxapine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.03
Assay: DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: amoxapine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.423
Assay: DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: amoxapine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.616
Assay: DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: amoxapine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.211
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: amoxapine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.336
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: amoxapine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.365
Drug: amoxapine
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: amoxapine
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.47
Action type: ANTAGONIST
Assay: Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
Drug: amoxapine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.842
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)