AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: apomorphine
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.74
Assay: Displacement of [3H]domperidone from dopamine D2 receptor high binding site in Sprague-Dawley rat striatum by scintillation counting
Drug: apomorphine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.53
Assay: Ability to displace [3H]8-OH-DPAT binding to rat hippocampal 5-hydroxytryptamine 1A receptor
Drug: apomorphine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32305 (5HT7R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.73
Assay: Binding affinity against Rat 5-hydroxytryptamine 7 receptor using [3H]5-HT
Drug: apomorphine
Target: D(1A) dopamine receptor (GPCR)
Gene: Drd1
UniProt: P18901 (DRD1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.28
Assay: Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug: apomorphine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P20288 (DRD2_BOVIN)
Organism: Bos taurus
Activity: Ki = 6.7
Assay: Compound was tested for inhibition of [3H]spiroperidol binding against Dopamine receptor D2
Drug: apomorphine
Target: D(3) dopamine receptor (GPCR)
Gene: Drd3
UniProt: P19020 (DRD3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.44
Assay: Displacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in SF9 cells
Drug: apomorphine
Target: D(4) dopamine receptor (GPCR)
Gene: Drd4
UniProt: P30729 (DRD4_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 8.82
Assay: In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
Drug: apomorphine
Target: D(1A) dopamine receptor (GPCR)
Gene: Drd1
UniProt: Q61616 (DRD1_MOUSE)
Organism: Mus musculus
Activity: Ki = 7
Assay: Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
Drug: apomorphine
Target: Zinc finger protein mex-5 (Cytosolic other)
Gene: mex-5
UniProt: Q9XUB2 (MEX5_CAEEL)
Organism: Caenorhabditis elegans
Activity: EC50 = 5.35
Assay: Active
Drug: apomorphine
Target: Opioid receptor (GPCR)
Gene: Oprd1|Oprm1|Oprk1|Sigmar1
UniProt: P33533|P33535|P34975|Q9R0C9 (OPRD_RAT|OPRM_RAT|OPRK_RAT|SGMR1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.52
Assay: Ability to inhibit the specific binding of [3H]- dihydromorphine to opiate receptors in rat brain membrane preparation by 50%
Drug: apomorphine
Target: Serotonin (5-HT) receptor (GPCR)
Gene: Htr2c|Htr2a|Htr1a|Htr1b|Htr1d|Htr1f|Htr2b|Htr6|Htr7|Htr5a|Htr5b|Htr3a|Htr4|Htr3b
UniProt: P08909|P14842|P19327|P28564|P28565|P30940|P30994|P31388|P32305|P35364|P35365|P35563|Q62758|Q9JJ16 (5HT2C_RAT|5HT2A_RAT|5HT1A_RAT|5HT1B_RAT|5HT1D_RAT|5HT1F_RAT|5HT2B_RAT|5HT6R_RAT|5HT7R_RAT|5HT5A_RAT|5HT5B_RAT|5HT3A_RAT|5HT4R_RAT|5HT3B_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.35
Assay: In vitro inhibitory activity against serotonin receptor from rat frontal cortex using [3H]spiperone as radioligand
Drug: apomorphine
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 = 7.2
Assay: Alpha-2 adrenergic receptor activity assessed in vitro for displacement of [3H]clonidine from specific binding sites on rat striatal membranes
Drug: apomorphine
Target: Dopamine receptor (GPCR)
Gene: DRD2|DRD1
UniProt: P20288|Q95136 (DRD2_BOVIN|DRD1_BOVIN)
Organism: Bos taurus
Activity: IC50 = 9
Assay: Tested for binding to dopamine receptor using [3H]apomorphine as radioligand in calf caudate nucleus homogenates.
Drug: apomorphine
Target: Dopamine receptor (GPCR)
Gene: Drd1|Drd3|Drd5|Drd4|Drd2
UniProt: P18901|P19020|P25115|P30729|P61169 (DRD1_RAT|DRD3_RAT|DRD5_RAT|DRD4_RAT|DRD2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 9
Assay: Inhibition of [3H]apomorphine binding to calf caudate membrane preparation (p4)
Drug: apomorphine
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 = 5.11
Assay: In vitro inhibitory activity against alpha-1 adrenergic receptor from whole rat brain using [3H]WB-4101 as radioligand
Drug: apomorphine
Target: Mannose-6-phosphate isomerase (Enzyme)
Gene: MPI
UniProt: P34949 (MPI_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.84
Assay: PUBCHEM_BIOASSAY: HTS identification of compounds inhibiting phosphomannose isomerase (PMI) via a fluorescence intensity assay using a high concentration of mannose 6-phosphate. (Class of assay: confirmatory) [Related pubchem assays: 1209 ]
Drug: apomorphine
Target: Cytoplasmic zinc-finger protein (Unclassified)
Gene: pos-1
UniProt: G5EF15 (G5EF15_CAEEL)
Organism: Caenorhabditis elegans
Activity: EC50 = 4.77
Assay: Inconclusive
Drug: apomorphine
Target: E3 ubiquitin-protein ligase Mdm2 (Nuclear other)
Gene: MDM2
UniProt: Q00987 (MDM2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.71
Assay: Inhibition of biotin-labelled D-p53 binding to D-MDM2 (25 to 109 residues) (unknown origin) by FAM labeled P4 peptide based fluorescence polarization assay
Drug: apraclonidine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.54
Action type: AGONIST
Assay: Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells
Drug: apraclonidine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.938
Action type: AGONIST
Drug: apraclonidine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.52
Action type: AGONIST
Assay: Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cells
Drug: apraclonidine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: Adra2b
UniProt: P19328 (ADA2B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.32
Assay: Compound was tested in vitro for binding affinity against Alpha-2B adrenergic receptor from cloned rat RNG receptor transfected into Chinese hamster ovary (CHO) cells
Drug: apraclonidine
Target: Adrenergic receptor alpha-1 (GPCR)
Gene: ADRA1D|ADRA1A|ADRA1B
UniProt: P25100|P35348|P35368 (ADA1D_HUMAN|ADA1A_HUMAN|ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.74
Assay: Compound was tested for binding affinity based on dissociation constant of Alpha-1 adrenergic receptor
Drug: aprepitant
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Drug: aprepitant
Target: Substance-P receptor (GPCR)
Gene: TACR1
UniProt: P25103 (NK1R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 10.7
Action type: ANTAGONIST
Assay: GRAC: human NK1 selective antagonist
Drug: aprepitant
Target: Neuromedin-K receptor (GPCR)
Gene: TACR3
UniProt: P29371 (NK3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.34
Assay: Displacement of [3H]osanetant from wild type human NK3 receptor expressed in HEK293 cells
Drug: aprepitant
Target: Substance-P receptor (GPCR)
Gene: TACR1
UniProt: Q5DUB1 (NK1R_MERUN)
Organism: Meriones unguiculatus
Activity: IC50 = 10.05
Drug: aprindine
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Drug: aprindine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Drug: aprindine
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.757
Drug: aprindine
Target: Proteasome subunit alpha type-1 (Enzyme)
Gene: PSMA1
UniProt: P25786 (PSA1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.398
Drug: aprindine
Target: Sodium/calcium exchanger 1 (Transporter)
Gene: SLC8A1
UniProt: P32418 (NAC1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.301
Drug: aprindine
Target: Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (Ion channel)
Gene: HCN4
UniProt: Q9Y3Q4 (HCN4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.359
Drug: aprindine
Target: Calmodulin (Cytosolic other)
Gene: CALM1|CALM2|CALM3
UniProt: P0DP23|P0DP24|P0DP25 (CALM1_HUMAN|CALM2_HUMAN|CALM3_HUMAN)
Organism: Homo sapiens
Activity: ID50 = 4.745
Action type: INHIBITOR
Drug: aranidipine
Target: Voltage-gated L-type calcium channel (Ion channel)
Gene: CACNA1D|CACNA1C
UniProt: Q01668|Q13936 (CAC1D_HUMAN|CAC1C_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Assay: Mechanism of Action
Drug: arbutamine
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action
Drug: argatroban
Target: Prothrombin (Enzyme)
Gene: F2
UniProt: P00734 (THRB_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.398
Action type: INHIBITOR
Drug: argatroban
Target: Coagulation factor X (Enzyme)
Gene: F10
UniProt: P00742 (FA10_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.28
Assay: Inhibition of human factor 10a
Drug: argatroban
Target: Tissue-type plasminogen activator (Enzyme)
Gene: PLAT
UniProt: P00750 (TPA_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.06
Assay: Inhibition of human t-PA
Drug: argatroban
Target: Cationic trypsin (Enzyme)
UniProt: P00760 (TRY1_BOVIN)
Organism: Bos taurus
Activity: Ki = 5.54
Assay: Inhibition of bovine trypsin
Drug: argatroban
Target: Prothrombin (Enzyme)
Gene: F2
UniProt: P00735 (THRB_BOVIN)
Organism: Bos taurus
Activity: Ki = 8.02
Assay: Inhibitory activity against thrombin.
Drug: aripiprazole
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.851
Drug: aripiprazole
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.788
Drug: aripiprazole
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.06
Drug: aripiprazole
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.71
Action type: PARTIAL AGONIST
Drug: aripiprazole
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.131
Drug: aripiprazole
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.22
Assay: Displacement of [3H]dofetilide from human ERG
Drug: aripiprazole
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.11
Assay: Inhibition of human ABCB1-mediated rhodamine 123 efflux in mouse L5178 cells expressing human MDR1 after 20 mins by FACS analysis
Drug: aripiprazole
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.83
Drug: aripiprazole
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.68
Drug: aripiprazole
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.9
Action type: ANTAGONIST
Drug: aripiprazole
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.444
Drug: aripiprazole
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.36
Drug: aripiprazole
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.51
Drug: aripiprazole
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.69
Drug: aripiprazole
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.244
Drug: aripiprazole
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.991
Drug: aripiprazole
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.53
Drug: aripiprazole
Target: D(1B) dopamine receptor (GPCR)
Gene: DRD5
UniProt: P21918 (DRD5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.681
Drug: aripiprazole
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.215
Drug: aripiprazole
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.169
Drug: aripiprazole
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.455
Drug: aripiprazole
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.33
Drug: aripiprazole
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.818
Drug: aripiprazole
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.633
Drug: aripiprazole
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.1
Drug: aripiprazole
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.2
Drug: aripiprazole
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.421
Drug: aripiprazole
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.492
Drug: aripiprazole
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.65
Drug: aripiprazole
Target: 5-hydroxytryptamine receptor 3A (Ion channel)
Gene: HTR3A
UniProt: P46098 (5HT3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.202
Drug: aripiprazole
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.463
Drug: aripiprazole
Target: 5-hydroxytryptamine receptor 5A (GPCR)
Gene: HTR5A
UniProt: P47898 (5HT5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.906
Drug: aripiprazole
Target: 5-hydroxytryptamine receptor 1E (GPCR)
Gene: HTR1E
UniProt: P28566 (5HT1E_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.097
Drug: aripiprazole
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P31389 (HRH1_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 7
Drug: aripiprazole
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.1
Assay: Displacement of [3H]spiperone from dopamine D2 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
Drug: aripiprazole
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.4
Assay: Displacement of [3H]-8-OH-DPAT from 5HT1A receptor in Wistar rat hippocampus homogenate
Drug: aripiprazole
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: Slc6a4
UniProt: P31652 (SC6A4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.97
Assay: Displacement of [3H]-citalopram from SERT in rat cerebral cortex after 1 hr by scintillation counting
Drug: aripiprazole
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: Htr2a
UniProt: P14842 (5HT2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.15
Assay: Displacement of [3H]ketanserin from 5HT2A receptor in Wistar rat cortex homogenate
Drug: aripiprazole
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32305 (5HT7R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.8
Action type: AGONIST
Drug: aripiprazole
Target: D(1A) dopamine receptor (GPCR)
Gene: Drd1
UniProt: P18901 (DRD1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.1
Assay: Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
Drug: aripiprazole
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: Htr2c
UniProt: P08909 (5HT2C_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.59
Drug: aripiprazole
Target: D(3) dopamine receptor (GPCR)
Gene: Drd3
UniProt: P19020 (DRD3_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.42
Drug: aripiprazole
Target: D(4) dopamine receptor (GPCR)
Gene: Drd4
UniProt: P30729 (DRD4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.3
Action type: ANTAGONIST
Drug: aripiprazole
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: Htr6
UniProt: P31388 (5HT6R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.8
Action type: AGONIST
Drug: aripiprazole
Target: Histone H1.0 (Nuclear other)
Gene: H1F0
UniProt: P07305 (H10_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.55
Assay: Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
Drug: aripiprazole
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.15
Action type: PARTIAL AGONIST
Drug: arsenic trioxide
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.824
Drug: arsenic trioxide
Target: Thioredoxin reductase 1, cytoplasmic (Enzyme)
Gene: TXNRD1
UniProt: Q16881 (TRXR1_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL1927; SINGLE PROTEIN
Drug: astemizole
Target: Sodium/nucleoside cotransporter 1 (Transporter)
Gene: SLC28A1
UniProt: O00337 (S28A1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.312
Assay: DRUGMATRIX: Sodium/nucleoside co-transporter radioligand binding (ligand: nitrobenzylthioinosine)
Drug: astemizole
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.998
Assay: DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug: astemizole
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.218
Assay: DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine)
Drug: astemizole
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.698
Assay: DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug: astemizole
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.822
Assay: DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
Drug: astemizole
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.741
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: astemizole
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.025
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: astemizole
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.046
Drug: astemizole
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.481
Drug: astemizole
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.05
Drug: astemizole
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.155
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: astemizole
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.865
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: astemizole
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.359
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
Drug: astemizole
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.253
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: astemizole
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.126
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: astemizole
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.027
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: astemizole
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.819
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: astemizole
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.756
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: astemizole
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.83
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: astemizole
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.781
Assay: DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug: astemizole
Target: Histamine H4 receptor (GPCR)
Gene: HRH4
UniProt: Q9H3N8 (HRH4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.1
Assay: Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
Drug: astemizole
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.59
Assay: DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: astemizole
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.3
Assay: DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: astemizole
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.75
Assay: DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: astemizole
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.587
Assay: DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: astemizole
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.297
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)