AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: haloperidol
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.33
Assay: Binding affinity to human cloned 5HT2C receptor
Drug: haloperidol
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.22
Assay: Binding affinity to human cloned 5HT6 receptor
Drug: haloperidol
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.45
Drug: haloperidol
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.9
Drug: haloperidol
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.319
Drug: haloperidol
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.52
Action type: INVERSE AGONIST
Drug: haloperidol
Target: D(1B) dopamine receptor (GPCR)
Gene: DRD5
UniProt: P21918 (DRD5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.52
Drug: haloperidol
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.36
Assay: Binding affinity to human cloned histamine H1 receptor
Drug: haloperidol
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.999
Drug: haloperidol
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.8
Assay: Binding affinity to human cloned muscarinic M1 receptor
Drug: haloperidol
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5
Drug: haloperidol
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.182
Drug: haloperidol
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.569
Drug: haloperidol
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.6
Action type: ANTAGONIST
Drug: haloperidol
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.26
Drug: haloperidol
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.553
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: haloperidol
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.097
Drug: haloperidol
Target: Calmodulin (Cytosolic other)
Gene: CALM1|CALM2|CALM3
UniProt: P0DP23|P0DP24|P0DP25 (CALM1_HUMAN|CALM2_HUMAN|CALM3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.3
Drug: haloperidol
Target: 5-hydroxytryptamine receptor 5A (GPCR)
Gene: HTR5A
UniProt: P47898 (5HT5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.648
Drug: haloperidol
Target: 5-hydroxytryptamine receptor 1F (GPCR)
Gene: HTR1F
UniProt: P30939 (5HT1F_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.301
Drug: haloperidol
Target: 5-hydroxytryptamine receptor 1E (GPCR)
Gene: HTR1E
UniProt: P28566 (5HT1E_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.301
Drug: haloperidol
Target: Potassium channel subfamily K member 2 (Ion channel)
Gene: KCNK2
UniProt: O95069 (KCNK2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.26
Assay: Inhibition of of human TREK1 expressed in whole COS cells assessed as reduction in channel currents
Drug: haloperidol
Target: Potassium voltage-gated channel subfamily H member 1 (Ion channel)
Gene: KCNH1
UniProt: O95259 (KCNH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.2
Action type: BLOCKER
Drug: haloperidol
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.305
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: haloperidol
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.444
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: haloperidol
Target: Pol polyprotein (Enzyme)
Gene: pol
UniProt: Q72874 (Q72874_9HIV1)
Organism: Human immunodeficiency virus 1
Activity: Ki = 7
Assay: Binding affinity for HIV-1 protease
Drug: haloperidol
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: Kd = 7.76
Assay: Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta
Drug: haloperidol
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P31389 (HRH1_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 6.4
Drug: haloperidol
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: Chrm2
UniProt: P10980 (ACM2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.62
Assay: Inhibition of [3H]N-methylscopolamine binding to Muscarinic acetylcholine receptor M2 of rat heart membranes
Drug: haloperidol
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: Chrm1
UniProt: P08482 (ACM1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.74
Assay: Compound was tested for the binding affinity against rat cortical Muscarinic acetylcholine receptor M1 by Radio ligand [3H]pirenzepine binding assay.
Drug: haloperidol
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.7
Assay: Binding towards Dopamine receptor D2 using [3H]spiperone from rat striatal membrane
Drug: haloperidol
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.4
Assay: The compound was tested for its binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 radioligand in rat hippocampus
Drug: haloperidol
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: Htr2a
UniProt: P14842 (5HT2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.35
Assay: In vitro ability to displace [3H]ketanserin from 5-hydroxytryptamine 2A receptor in rat brain.
Drug: haloperidol
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: Sigmar1
UniProt: Q9R0C9 (SGMR1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.05
Assay: Displacement of [3H](+)-pentazocine from sigma 1 receptor in rat brain homogenate
Drug: haloperidol
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32305 (5HT7R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.58
Assay: Binding affinity towards rat 5-hydroxytryptamine 7 receptor
Drug: haloperidol
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32304 (5HT7R_MOUSE)
Organism: Mus musculus
Activity: Ki = 6.3
Action type: ANTAGONIST
Drug: haloperidol
Target: D(1A) dopamine receptor (GPCR)
Gene: Drd1
UniProt: P18901 (DRD1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.7
Assay: Affinity for Dopamine receptor D1
Drug: haloperidol
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P20288 (DRD2_BOVIN)
Organism: Bos taurus
Activity: Ki = 9.52
Assay: Evaluated for binding towards Dopamine receptor D2 using [3H]-spiperone as radioligand, in cloned mammalian receptors expressed in CHO-K1 cells
Drug: haloperidol
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P18130 (ADA1A_BOVIN)
Organism: Bos taurus
Activity: IC50 = 7.7
Assay: Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
Drug: haloperidol
Target: Histamine H1 receptor (GPCR)
Gene: Hrh1
UniProt: P31390 (HRH1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.42
Assay: Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
Drug: haloperidol
Target: D(3) dopamine receptor (GPCR)
Gene: Drd3
UniProt: P19020 (DRD3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.52
Assay: Binding affinity towards baculovirus expressed rat dopamine D3 receptors
Drug: haloperidol
Target: Protease (Enzyme)
Gene: protease
UniProt: Q4U254 (Q4U254_9ENTO)
Organism: Human rhinovirus sp
Activity: Ki = 7
Assay: The compound was tested for its affinity against HIV-2 protease
Drug: haloperidol
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P52702 (DRD2_CHLAE)
Organism: Chlorocebus aethiops
Activity: Ki = 8.32
Assay: Displacement of [3H]YM-09151 from recombinant African green monkey Dopamine receptor D2
Drug: haloperidol
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: Q75Z89 (5HT2A_BOVIN)
Organism: Bos taurus
Activity: IC50 = 7.52
Assay: Affinity towards 5-hydroxytryptamine 2A receptor in membranes from bovine frontal cortex using [3H]ketanserin
Drug: haloperidol
Target: C-8 sterol isomerase (Enzyme)
Gene: ERG2
UniProt: P32352 (ERG2_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: Ki = 9.3
Assay: Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand
Drug: haloperidol
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P50130 (DRD1_PIG)
Organism: Sus scrofa
Activity: Ki = 7.03
Assay: Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
Drug: haloperidol
Target: Sigma non-opioid intracellular receptor 1 (Membrane other)
Gene: SIGMAR1
UniProt: Q60492 (SGMR1_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 9.08
Assay: Displacement of [3H](+)-PTZ from sigma1 receptor in Hartley guinea pig brain
Drug: haloperidol
Target: Transporter (Transporter)
Gene: NET
UniProt: Q63380 (Q63380_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.26
Assay: Binding affinity to rat NET
Drug: haloperidol
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P50129 (5HT2A_PIG)
Organism: Sus scrofa
Activity: Ki = 7.52
Assay: Displacement of [3H]Ketanserin from 5-HT2 receptor in pig cortex membranes
Drug: haloperidol
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P52703 (DRD3_CHLAE)
Organism: Chlorocebus aethiops
Activity: Ki = 8.52
Assay: Displacement of [3H]-YM 09151 from african monkey Dopamine receptor D3
Drug: haloperidol
Target: Vesicular acetylcholine transporter (Transporter)
Gene: Slc18a3
UniProt: Q62666 (VACHT_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.41
Assay: Displacement of (-)-[3H]vesamicol from rat VAChT expressed in rat PC12 cell membranes after 60 mins by liquid scintillation counting method
Drug: haloperidol
Target: AP-2 complex subunit sigma (Unclassified)
Gene: Ap2s1
UniProt: P62744 (AP2S1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.62
Assay: Displacement of [3H]-DTG from rat sigma2 receptor by liquid scintillation counting
Drug: haloperidol
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: Ki = 5.13
Assay: In vitro binding affinity against Muscarinic acetylcholine receptors in rat brain.
Drug: haloperidol
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: Ki = 5.92
Assay: Binding affinity was measured against opioid receptor in rat using [3H]naloxone as radioligand
Drug: haloperidol
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 = 4.7
Assay: Binding affinity against serotonin-1 receptor in rat brain using [3H]5-HT
Drug: haloperidol
Target: Adrenergic receptor alpha-2 (GPCR)
Gene: Adra2b|Adra2c|Adra2a
UniProt: P19328|P22086|P22909 (ADA2B_RAT|ADA2C_RAT|ADA2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.57
Assay: Half-maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor in rat frontal cortex homogenate
Drug: haloperidol
Target: Dopamine receptor (GPCR)
Gene: DRD2|DRD1
UniProt: P20288|Q95136 (DRD2_BOVIN|DRD1_BOVIN)
Organism: Bos taurus
Activity: IC50 = 8.74
Assay: Inhibition of [3H]haloperidol binding to Dopamine receptor in calf caudate nuclei.
Drug: haloperidol
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: Ki = 8.7
Assay: In vitro ability to displace [3H]spiroperidol from rat dopamine receptor
Drug: haloperidol
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 = 5.92
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: haloperidol
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: Ki = 8.38
Assay: Binding affinity towards 5-hydroxytryptamine 2 receptor
Drug: haloperidol
Target: Adenylate cyclase (Enzyme)
Gene: Adcy1|Adcy3|Adcy2|Adcy4|Adcy8|Adcy6|Adcy5
UniProt: D4A3N4|P21932|P26769|P26770|P40146|Q03343|Q04400|Q8CFM9 (D4A3N4_RAT|ADCY3_RAT|ADCY2_RAT|ADCY4_RAT|ADCY8_RAT|ADCY6_RAT|ADCY5_RAT|Q8CFM9_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.64
Assay: Inhibition of dopamine-sensitive rat brain adenylyl cyclase activity assessed as cAMP level
Drug: haloperidol
Target: Serotonin 2 (5-HT2) receptor (GPCR)
Gene: Htr2c|Htr2a|Htr2b
UniProt: P34968|P35363|Q02152 (5HT2C_MOUSE|5HT2A_MOUSE|5HT2B_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.58
Assay: Binding affinity against 5-hydroxytryptamine 2 receptor from rat cortical synaptosomal membrane using radioligand [3H]ketanserin.
Drug: haloperidol
Target: G protein-activated inward rectifier potassium channel 2 (Ion channel)
Gene: Kcnj6
UniProt: P48542 (KCNJ6_MOUSE)
Organism: Mus musculus
Activity: EC50 = 4.1
Action type: GATING INHIBITOR
Drug: haloperidol
Target: Histone H1.0 (Nuclear other)
Gene: H1F0
UniProt: P07305 (H10_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.11
Assay: Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
Drug: haloperidol
Target: Transmembrane protein 97 (Enzyme)
Gene: TMEM97
UniProt: Q5BJF2 (TMM97_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.8
Assay: Displacement of [3H]-DTG from sigma 2 receptor (unknown origin) after 120 mins by liquid scintillation counting method
Drug: haloperidol
Target: Sigma intracellular receptor 2 (Unclassified)
Gene: Tmem97
UniProt: Q5U3Y7 (SGMR2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.36
Assay: Displacement of [3H]DTG from sigma2 receptor in rat liver membranes after 60 mins by liquid scintillation counting method
Drug: haloperidol
Target: Zinc finger protein 664 (Unclassified)
Gene: ZNF664
UniProt: Q60493 (ZN664_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 8.18
Assay: Displacement of [3H]-(+)-pentazocine from sigma1-type opioid receptor in guinea pig cortex membranes after 120 mins by solid scintillation counting
Drug: haloperidol
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 9.42
Action type: INVERSE AGONIST
Assay: radioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cells
Drug: halopredone acetate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action
Drug: haloprogin
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.55
Assay: DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug: haloprogin
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.339
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: haloprogin
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.366
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: haloprogin
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.561
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: haloprogin
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.16
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: haloprogin
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.866
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: haloprogin
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.73
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: haloprogin
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.6
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: haloprogin
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.78
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: haloprogin
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.231
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: haloprogin
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.805
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: haloprogin
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.9
Assay: DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
Drug: haloprogin
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.338
Assay: DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine)
Drug: haloprogin
Target: Substance-K receptor (GPCR)
Gene: TACR2
UniProt: P21452 (NK2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.309
Assay: DRUGMATRIX: Tachykinin NK2  radioligand binding (ligand: [3H] SR-48968)
Drug: haloprogin
Target: UDP-glucose 4-epimerase (Enzyme)
Gene: GALE
UniProt: Q14376 (GALE_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.3
Assay: Inhibition of human GalE by HPAEC assay
Drug: halothane
Target: Potassium channel subfamily K member 2 (Ion channel)
Gene: KCNK2
UniProt: O95069 (KCNK2_HUMAN)
Organism: Homo sapiens
Action type: OPENER
Assay: Mechanism of Action; CHEMBL2321615; SINGLE PROTEIN
Drug: halothane
Target: Potassium channel subfamily K member 3 (Ion channel)
Gene: KCNK3
UniProt: O14649 (KCNK3_HUMAN)
Organism: Homo sapiens
Action type: OPENER
Assay: Mechanism of Action; CHEMBL2321613; SINGLE PROTEIN
Drug: halothane
Target: Potassium channel subfamily K member 9 (Ion channel)
Gene: KCNK9
UniProt: Q9NPC2 (KCNK9_HUMAN)
Organism: Homo sapiens
Action type: OPENER
Assay: Mechanism of Action; CHEMBL2321614; SINGLE PROTEIN
Drug: halothane
Target: Potassium channel subfamily K member 10 (Ion channel)
Gene: KCNK10
UniProt: P57789 (KCNKA_HUMAN)
Organism: Homo sapiens
Action type: OPENER
Assay: Mechanism of Action; CHEMBL2331041; SINGLE PROTEIN
Drug: halothane
Target: Potassium channel subfamily K member 18 (Ion channel)
Gene: KCNK18
UniProt: Q7Z418 (KCNKI_HUMAN)
Organism: Homo sapiens
Action type: OPENER
Assay: Mechanism of Action; CHEMBL2331042; SINGLE PROTEIN
Drug: halothane
Target: Glycine receptor (alpha-1/beta) (Ion channel)
Gene: GLRA1|GLRB
UniProt: P23415|P48167 (GLRA1_HUMAN|GLRB_HUMAN)
Organism: Homo sapiens
Action type: POSITIVE MODULATOR
Assay: Mechanism of Action; CHEMBL2363052; PROTEIN COMPLEX
Drug: halothane
Target: GABA-A receptor; anion channel (Ion channel)
Gene: GABRP|GABRD|GABRA1|GABRB1|GABRG2|GABRB3|GABRA5|GABRA3|GABRA2|GABRB2|GABRA4|GABRE|GABRA6|GABRG1|GABRG3|GABRQ
UniProt: O00591|O14764|P14867|P18505|P18507|P28472|P31644|P34903|P47869|P47870|P48169|P78334|Q16445|Q8N1C3|Q99928|Q9UN88 (GBRP_HUMAN|GBRD_HUMAN|GBRA1_HUMAN|GBRB1_HUMAN|GBRG2_HUMAN|GBRB3_HUMAN|GBRA5_HUMAN|GBRA3_HUMAN|GBRA2_HUMAN|GBRB2_HUMAN|GBRA4_HUMAN|GBRE_HUMAN|GBRA6_HUMAN|GBRG1_HUMAN|GBRG3_HUMAN|GBRT_HUMAN)
Organism: Homo sapiens
Action type: POSITIVE ALLOSTERIC MODULATOR
Assay: Mechanism of Action; CHEMBL2093872; PROTEIN COMPLEX GROUP
Drug: heparin
Target: Antithrombin-III (Secreted)
Gene: SERPINC1
UniProt: P01008 (ANT3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.85
Action type: ACTIVATOR
Assay: Catalyses the inactivation of coagulation proteases by activatted antithrombin-III
Drug: heparin
Target: Spike glycoprotein (Glycoprotein)
Gene: S
UniProt: P0DTC2 (SPIKE_SARS2)
Organism: Severe acute respiratory syndrome coronavirus 2 (2019-nCoV) (SARS-CoV-2)
Activity: Kd = 10.14
Assay: Binding affinity of trimeric SARS-CoV-2 spike protein to immobilized heparin.
Drug: heparin
Target: Spike glycoprotein (Unclassified)
Gene: S
UniProt: P0DTC2 (SPIKE_SARS2)
Organism: Severe acute respiratory syndrome coronavirus 2 (2019-nCoV) (SARS-CoV-2)
Activity: Kd = 10.14
Assay: Binding affinity of trimeric SARS-CoV-2 spike protein to immobilized heparin.
Drug: hesperetin
Target: Carbonic anhydrase 4 (Enzyme)
Gene: CA4
UniProt: P22748 (CAH4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.99
Drug: hesperetin
Target: Carbonic anhydrase 12 (Enzyme)
Gene: CA12
UniProt: O43570 (CAH12_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.34
Drug: hesperetin
Target: Carbonic anhydrase 7 (Enzyme)
Gene: CA7
UniProt: P43166 (CAH7_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.48
Drug: hesperetin
Target: Dipeptidyl peptidase 4 (Enzyme)
Gene: DPP4
UniProt: P27487 (DPP4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.55
Assay: Inhibition of DPP4 (unknown origin) using Gly-Pro-AMC as substrate preincubated for 4 secs followed by substrate addition and measured after 30 mins by luminescence assay
Drug: hesperetin
Target: Glycogen synthase kinase-3 beta (Kinase)
Gene: GSK3B
UniProt: P49841 (GSK3B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.57
Assay: Inhibition of Homo sapiens (human) recombinant GSK3beta after 30 min by Kinase-Glo assay
Drug: hesperetin
Target: Cytochrome P450 1B1 (Enzyme)
Gene: CYP1B1
UniProt: Q16678 (CP1B1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.29
Assay: Inhibition of human CYP1B1 by EROD assay
Drug: hesperetin
Target: Replicase polyprotein 1ab (Enzyme)
Gene: rep
UniProt: P0C6X7 (R1AB_CVHSA)
Organism: Human SARS coronavirus
Activity: IC50 = 5.08
Assay: Inhibition of SARS coronavirus 3C-like protease cis-cleavage activity transfected in african green monkey Vero cells by luciferase reporter gene assay
Drug: hesperetin
Target: Lysine-specific histone demethylase 1A (Enzyme)
Gene: KDM1A
UniProt: O60341 (KDM1A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.1
Assay: Inhibition of LSD1 (unknown origin) by fluorescence assay
Drug: hetacillin
Target: Penicillin-binding protein (Enzyme)
Gene: pbp2b|pbp3|PBP2X|pbp2a|pbp1b|pbp1a
UniProt: Q54618|Q75Y37|Q75Y54|Q75YD8|Q75YK0|Q9RET4 (Q54618_STREE|Q75Y37_STREE|Q75Y54_STREE|Q75YD8_STREE|Q75YK0_STREE|Q9RET4_STREE)
Organism: Streptococcus pneumoniae
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2362973; PROTEIN FAMILY