AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: phenyltoloxamine
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.56
Assay: Binding affinity for human recombinant dopamine receptor D4.4
Drug: phenyltoloxamine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Assay: Mechanism of Action
Drug: phenytoin
Target: Nuclear receptor subfamily 1 group I member 3 (Nuclear hormone receptor)
Gene: NR1I3
UniProt: Q14994 (NR1I3_HUMAN)
Organism: Homo sapiens
Drug: phenytoin
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: phenytoin
Target: Sodium channel protein type 1 subunit alpha (Ion channel)
Gene: SCN1A
UniProt: P35498 (SCN1A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Assay: Mechanism of Action
Drug: phenytoin
Target: Sodium channel protein type 2 subunit alpha (Ion channel)
Gene: SCN2A
UniProt: Q99250 (SCN2A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.9
Action type: BLOCKER
Drug: phenytoin
Target: Sodium channel protein type 3 subunit alpha (Ion channel)
Gene: SCN3A
UniProt: Q9NY46 (SCN3A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Assay: Mechanism of Action
Drug: phenytoin
Target: Sodium channel protein type 4 subunit alpha (Ion channel)
Gene: SCN4A
UniProt: P35499 (SCN4A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.62
Action type: BLOCKER
Assay: Affinity for inactive human SkM1 sodium channel expressed in HEK293 cells
Drug: phenytoin
Target: Sodium channel protein type 8 subunit alpha (Ion channel)
Gene: SCN8A
UniProt: Q9UQD0 (SCN8A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Assay: Mechanism of Action
Drug: phenytoin
Target: Sodium channel protein type 9 subunit alpha (Ion channel)
Gene: SCN9A
UniProt: Q15858 (SCN9A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Assay: Mechanism of Action
Drug: phenytoin
Target: Sodium channel protein type 2 subunit alpha (Ion channel)
Gene: Scn2a
UniProt: P04775 (SCN2A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.66
Assay: Inhibition of rat Nav1.2 channel expressed in chinese hamster CHL1610 cells at preconditioning pulse of -67 mV after 2 to 3 mins by whole-cell patch-clamp technique
Drug: phenytoin
Target: Sodium channel alpha subunits; brain (Types I, II, III) (Ion channel)
Gene: Scn1a|Scn2a|Scn3a
UniProt: P04774|P04775|P08104 (SCN1A_RAT|SCN2A_RAT|SCN3A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.4
Assay: In vitro inhibition of Voltage-gated sodium channel by the displacement of [3H]batrachotoxin A 20-alpha-benzoate in rat brain cerebral cortex synaptoneurosomes
Drug: phloroglucinol
Target: Beta-secretase 1 (Enzyme)
Gene: BACE1
UniProt: P56817 (BACE1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.44
Assay: Inhibition of human recombinant BACE1 after 60 mins by FRET assay
Drug: oxagrelate
Target: Phosphodiesterase 3 (Enzyme)
Gene: PDE3B|PDE3A
UniProt: Q13370|Q14432 (PDE3B_HUMAN|PDE3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.85
Assay: Binding affinity for low Km cAMP phosphodiesterase PDE III of human platelets
Drug: oxagrelate
Target: Phosphodiesterase 1 (Enzyme)
Gene: PDE1A|PDE1B|PDE1C
UniProt: P54750|Q01064|Q14123 (PDE1A_HUMAN|PDE1B_HUMAN|PDE1C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5
Assay: Binding affinity for [Ca(2+)]/calmodulin dependent phosphodiesterase PDE 1 of human brain
Drug: physostigmine
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.699
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: physostigmine
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P22303 (ACES_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.37
Action type: INHIBITOR
Assay: In vitro inhibitory activity against acetylcholinesterase
Drug: physostigmine
Target: Cholinesterase (Enzyme)
Gene: BCHE
UniProt: P06276 (CHLE_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.3
Assay: Inhibition of anticholinesterase activity by their ability to inactivate human serum butyrylcholinesterase
Drug: physostigmine
Target: Acetylcholinesterase (Enzyme)
Gene: ache
UniProt: P04058 (ACES_TORCA)
Organism: Torpedo californica
Activity: IC50 = 7.96
Assay: Inhibition of Pacific electric ray AChE using acetylthiocholine iodide as substrate after 60 mins by Ellman's method
Drug: physostigmine
Target: Acetylcholinesterase (Enzyme)
Gene: Ache
UniProt: P21836 (ACES_MOUSE)
Organism: Mus musculus
Activity: IC50 = 9.17
Assay: Inhibitory activity against acetylcholinesterase
Drug: physostigmine
Target: Butyrylcholinesterase; Protein Bche (Enzyme)
Gene: Bche
UniProt: Q9JKC1 (Q9JKC1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.12
Assay: Inhibition of rat plasma BChE by Ellman's method
Drug: physostigmine
Target: Acetylcholinesterase (Enzyme)
Gene: Ache
UniProt: P37136 (ACES_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 9.17
Assay: Inhibitory concentration in vitro and ex vivo for anti-AChE activity in rat brain
Drug: physostigmine
Target: Acetylcholinesterase (Enzyme)
Gene: ache
UniProt: O42275 (ACES_ELEEL)
Organism: Electrophorus electricus
Activity: Ki = 7.47
Assay: Time dependent inhibition of Electric eel AChE assessed as stability constants of inhibitor-enzyme complex using acetylthiocholine as substrate after 60 mins
Drug: physostigmine
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P23795 (ACES_BOVIN)
Organism: Bos taurus
Activity: IC50 = 7.52
Assay: Concentration required to inhibit hydrolytic activity of Acetylcholinesterase by 50%
Drug: physostigmine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: Chrm1
UniProt: P12657 (ACM1_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4.43
Assay: Binding affinity against mouse muscarinic acetylcholine receptor M1 using cerebral cortex and [3H]pirenzepine
Drug: physostigmine
Target: Cholinesterase (Enzyme)
Gene: Bche
UniProt: Q03311 (CHLE_MOUSE)
Organism: Mus musculus
Activity: IC50 = 6.55
Assay: Inhibition of mouse serum BChE after 1 hr by modified Ellman's colorimetric method
Drug: physostigmine
Target: Butyrylcholinesterase (Enzyme)
Gene: BCHE
UniProt: Q9N1N9 (Q9N1N9_HORSE)
Organism: Equus caballus
Activity: IC50 = 7.8
Assay: Compound was evaluated for its inhibitory concentration against Horse serum Butyrylcholinesterase
Drug: physostigmine
Target: Cholinesterase (Enzyme)
Gene: BCHE
UniProt: P81908 (CHLE_HORSE)
Organism: Equus caballus
Activity: Ki = 7.39
Assay: Time dependent inhibition of equine serum BChE assessed as stability constants of inhibitor-enzyme complex using acetylthiocholine as substrate after 60 mins
Drug: physostigmine
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P36196 (ACES_CHICK)
Organism: Gallus gallus
Activity: IC50 = 7.7
Assay: Inhibition of acetylcholine esterase in chicken biventer cervicis muscle assessed as rate of acetylcholine hydrolysis by Ellman's method
Drug: picrotoxin
Target: Glycine receptor subunit alpha-1 (Ion channel)
Gene: GLRA1
UniProt: P23415 (GLRA1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.2
Action type: BLOCKER
Drug: picrotoxin
Target: Glycine receptor subunit alpha-2 (Ion channel)
Gene: GLRA2
UniProt: P23416 (GLRA2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.6
Action type: BLOCKER
Drug: picrotoxin
Target: Glycine receptor subunit beta (Ion channel)
Gene: GLRB
UniProt: P48167 (GLRB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.5
Action type: BLOCKER
Drug: picrotoxin
Target: 5-hydroxytryptamine receptor 3A (Ion channel)
Gene: Htr3a
UniProt: P23979 (5HT3A_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4.5
Action type: BLOCKER
Drug: picrotoxin
Target: GABA-A receptor; anion channel (Ion channel)
Gene: Gabrp|Gabrb1|Gabrd|Gabrg2|Gabra5|Gabra3|Gabrg1|Gabra2|Gabra4|Gabrg3|Gabra6|Gabra1|Gabrb3|Gabrb2|Gabrq|Gabre
UniProt: O09028|P15431|P18506|P18508|P19969|P20236|P23574|P23576|P28471|P28473|P30191|P62813|P63079|P63138|Q91ZM7|Q9ES14 (GBRP_RAT|GBRB1_RAT|GBRD_RAT|GBRG2_RAT|GBRA5_RAT|GBRA3_RAT|GBRG1_RAT|GBRA2_RAT|GBRA4_RAT|GBRG3_RAT|GBRA6_RAT|GBRA1_RAT|GBRB3_RAT|GBRB2_RAT|Q91ZM7_RAT|GBRE_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.88
Assay: Tested for inhibition of specific binding of [3H]-EBOB to GABA-Gated Chloride channels of Gamma-aminobutyric acid A receptor in rat brain cortex (Potency expressed as IC50)
Drug: picrotin
Target: Glycine receptor subunit alpha-1 (Ion channel)
Gene: GLRA1
UniProt: P23415 (GLRA1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.28
Assay: GRAC: human Glycine receptor subunit alpha-1 channel blocker
Drug: picrotin
Target: Glycine receptor subunit alpha-2 (Ion channel)
Gene: GLRA2
UniProt: P23416 (GLRA2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.9
Action type: BLOCKER
Drug: picrotin
Target: Glycine receptor subunit beta (Ion channel)
Gene: GLRB
UniProt: P48167 (GLRB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.6
Action type: BLOCKER
Drug: picrotin
Target: Glycine receptor subunit alpha-3 (Ion channel)
Gene: GLRA3
UniProt: O75311 (GLRA3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.22
Assay: GRAC: human Glycine receptor subunit alpha-3 channel blocker
Drug: piketoprofen
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Drug: piketoprofen
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Drug: pilocarpine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: Chrm2
UniProt: P10980 (ACM2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.01
Assay: Compound was evaluated for its affinity towards Muscarinic acetylcholine receptor M2, using [3H]- N-methyl-scopolamine, a radioligand displacement assay in rat heart membranes
Drug: pilocarpine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: Chrm1
UniProt: P08482 (ACM1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.51
Assay: Compound was evaluated for its affinity towards Muscarinic acetylcholine receptor M1, using [3H]- pirenzepine, a radioligand displacement assay in rat hippocampal membranes
Drug: pilocarpine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: Chrm1
UniProt: P12657 (ACM1_MOUSE)
Organism: Mus musculus
Activity: EC50 = 5.16
Assay: Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
Drug: pilocarpine
Target: Muscarinic acetylcholine receptor DM1 (GPCR)
Gene: mAChR-A
UniProt: P16395 (ACM1_DROME)
Organism: Drosophila melanogaster
Activity: Ki = 5.55
Assay: Displacement of [3H]AF-DX 384 from Drosophila melanogaster mAChR by scintillation counting
Drug: pilocarpine
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 = 7.08
Assay: Inhibition of [3H]OXO-M binding against muscarinic acetylcholine receptor in rat brain membranes
Drug: pilocarpine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.02
Action type: AGONIST
Assay: calcium response in CHO cells
Drug: pilocarpine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.95
Action type: AGONIST
Assay: calcium response in CHO cells
Drug: pilocarpine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.97
Action type: AGONIST
Assay: calcium response in CHO cells
Drug: pilocarpine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.15
Action type: AGONIST
Assay: calcium response in CHO cells
Drug: pilocarpine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7
Action type: AGONIST
Assay: calcium response in CHO cells
Drug: pilsicainide
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.69
Assay: Inhibition of human ERG channel in HEK293 cells by voltage-clamp method
Drug: pilsicainide
Target: Sodium channel protein type 4 subunit alpha (Ion channel)
Gene: SCN4A
UniProt: P35499 (SCN4A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.377
Action type: BLOCKER
Assay: pH 8.2; use-dependent block at -70mV
Drug: pimecrolimus
Target: Interleukin-5 (Cytokine)
Gene: IL5
UniProt: P05113 (IL5_HUMAN)
Organism: Homo sapiens
Drug: pimecrolimus
Target: Interferon gamma (Cytokine)
Gene: IFNG
UniProt: P01579 (IFNG_HUMAN)
Organism: Homo sapiens
Drug: pimecrolimus
Target: Peptidyl-prolyl cis-trans isomerase FKBP1A (Enzyme)
Gene: FKBP1A
UniProt: P62942 (FKB1A_HUMAN)
Organism: Homo sapiens
Activity: Kd = 9
Action type: INHIBITOR
Drug: pimecrolimus
Target: Interleukin-2 (Cytokine)
Gene: IL2
UniProt: P60568 (IL2_HUMAN)
Organism: Homo sapiens
Drug: pimecrolimus
Target: Serine/threonine-protein phosphatase 2B catalytic subunit gamma isoform (Enzyme)
Gene: PPP3CC
UniProt: P48454 (PP2BC_HUMAN)
Organism: Homo sapiens
Drug: pimecrolimus
Target: Peptidyl-prolyl cis-trans isomerase FKBP1A (Enzyme)
Gene: Fkbp1a
UniProt: Q62658 (FKB1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.22
Action type: INHIBITOR
Assay: Indirect measurement of primary target inhibition via rotamase inhibition
Drug: pimethixene
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: Htr2a
UniProt: P14842 (5HT2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.6
Assay: Binding affinity against 5-hydroxytryptamine 2A receptor from rat forebrain using [3H]ketanserin as radioligand
Drug: pimethixene
Target: Transcriptional activator protein luxR (Unclassified)
Gene: luxR
UniProt: P12746 (LUXR_ALIFS)
Organism: Aliivibrio fischeri
Activity: IC50 = 4.25
Assay: Inhibition of LuxR-dependent quorum sensing in Vibrio fischeri assessed as reduction of 3-oxo-C6-HSL-induced bioluminescence intensity
Drug: pimethixene
Target: Histone-lysine N-methyltransferase SETD7 (Enzyme)
Gene: SETD7
UniProt: Q8WTS6 (SETD7_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.37
Assay: Inhibition of recombinant SET7/9 (unknown origin) using biotinylated histone H3-derived peptide/SAM as substrate after 60 mins by AlphaLISA assay
Drug: pimobendan
Target: Type-1 angiotensin II receptor (GPCR)
Gene: AGTR1
UniProt: P25104 (AGTR1_BOVIN)
Organism: Bos taurus
Activity: IC50 = 4.77
Assay: Concentration required for 50% inhibition of binding against Angiotensin II receptor, type 1 in bovine adrenal cortex
Drug: pimobendan
Target: Phosphodiesterase 3 (Enzyme)
Gene: PDE3B|PDE3A
UniProt: Q13370|Q14432 (PDE3B_HUMAN|PDE3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.39
Action type: INHIBITOR
Assay: Inhibition of phosphodiesterase 3
Drug: pimozide
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.43
Assay: Binding affinity against mu opioid receptor using [3H]DAMGO
Drug: pimozide
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.862
Action type: ANTAGONIST
Drug: pimozide
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.798
Drug: pimozide
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.842
Drug: pimozide
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.745
Drug: pimozide
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.538
Drug: pimozide
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.63
Drug: pimozide
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.559
Action type: ANTAGONIST
Drug: pimozide
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.058
Drug: pimozide
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.149
Drug: pimozide
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.301
Drug: pimozide
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.704
Drug: pimozide
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.086
Drug: pimozide
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.046
Action type: ANTAGONIST
Drug: pimozide
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.71
Drug: pimozide
Target: Histamine H4 receptor (GPCR)
Gene: HRH4
UniProt: Q9H3N8 (HRH4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.7
Assay: Antagonist activity at H4 receptor (unknown origin)
Drug: pimozide
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.709
Drug: pimozide
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.509
Drug: pimozide
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.424
Drug: pimozide
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.745
Action type: ANTAGONIST
Drug: pimozide
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Assay: Binding affinity against opioid receptor kappa 1 by using [3H]U-69593 as radioligand
Drug: pimozide
Target: Multidrug resistance-associated protein 1 (Transporter)
Gene: ABCC1
UniProt: P33527 (MRP1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Drug: pimozide
Target: Glycine receptor subunit alpha-1 (Ion channel)
Gene: GLRA1
UniProt: P23415 (GLRA1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.77
Drug: pimozide
Target: Voltage-dependent T-type calcium channel subunit alpha-1G (Ion channel)
Gene: CACNA1G
UniProt: O43497 (CAC1G_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.4
Assay: Inhibition of T-type alpha1G calcium channel
Drug: pimozide
Target: Calmodulin (Cytosolic other)
Gene: CALM1|CALM2|CALM3
UniProt: P0DP23|P0DP24|P0DP25 (CALM1_HUMAN|CALM2_HUMAN|CALM3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.222
Drug: pimozide
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.42
Assay: Binding affinity against delta opiate receptor using [3H]DPDPE
Drug: pimozide
Target: Voltage-dependent T-type calcium channel subunit alpha-1I (Ion channel)
Gene: CACNA1I
UniProt: Q9P0X4 (CAC1I_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.5
Action type: BLOCKER
Drug: pimozide
Target: Potassium channel subfamily K member 2 (Ion channel)
Gene: KCNK2
UniProt: O95069 (KCNK2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.75
Assay: Inhibition of of human TREK1 expressed in whole COS cells assessed as reduction in channel currents
Drug: pimozide
Target: Potassium voltage-gated channel subfamily A member 10 (Ion channel)
Gene: KCNA10
UniProt: Q16322 (KCA10_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.5
Action type: BLOCKER
Drug: pimozide
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32305 (5HT7R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.3
Assay: Binding affinity towards rat 5-hydroxytryptamine 7 receptor
Drug: pimozide
Target: Sodium channel protein type 2 subunit alpha (Ion channel)
Gene: Scn2a
UniProt: P04775 (SCN2A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.47
Assay: Inhibitory activity against type IIA sodium channel in CNaIIA-1 cell line expressed in CHO cells
Drug: pimozide
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P20288 (DRD2_BOVIN)
Organism: Bos taurus
Activity: Ki = 9.22
Assay: Binding affinity of compound towards Dopamine receptor D2 using [3H]raclopride (1.2 nM) ligand in striatum bovine was determined
Drug: pimozide
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: Htr6
UniProt: P31388 (5HT6R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.2
Action type: ANTAGONIST
Drug: pimozide
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.47
Assay: Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Drug: pimozide
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 = 9.4
Assay: Inhibition of [3H]haloperidol binding to dopamine receptors in rat striatal membranes.
Drug: pimozide
Target: Ubiquitin carboxyl-terminal hydrolase 1 (Enzyme)
Gene: USP1
UniProt: O94782 (UBP1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.7
Drug: pimozide
Target: Voltage-dependent T-type calcium channel subunit alpha-1H (Ion channel)
Gene: Cacna1h
UniProt: Q9EQ60 (CAC1H_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.3
Action type: BLOCKER
Drug: pimozide
Target: G protein-activated inward rectifier potassium channel 2 (Ion channel)
Gene: Kcnj6
UniProt: P48542 (KCNJ6_MOUSE)
Organism: Mus musculus
Activity: EC50 = 5.5
Action type: GATING INHIBITOR
Drug: pimozide
Target: Voltage-dependent T-type calcium channel subunit alpha-1G (Ion channel)
Gene: Cacna1g
UniProt: O54898 (CAC1G_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.5
Action type: BLOCKER
Drug: pinacidil
Target: ATP-binding cassette sub-family C member 9 (Ion channel)
Gene: ABCC9
UniProt: O60706 (ABCC9_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.45
Assay: Channel opening activity at SUR2B/Kir6.2 potassium ATP channel in human TE671 cells assessed as isometric force by FLIPR
Drug: pinacidil
Target: Calcium-activated potassium channel subunit alpha-1 (Ion channel)
Gene: KCNMA1
UniProt: Q12791 (KCMA1_HUMAN)
Organism: Homo sapiens
Drug: pinacidil
Target: Sulfonylurea receptor 2, Kir6.2 (Ion channel)
Gene: ABCC9|KCNJ11
UniProt: O60706|Q14654 (ABCC9_HUMAN|KCJ11_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.49
Action type: OPENER
Assay: Binding affinity was determined by displacement of [3H]P1075 from its binding sites in canine cardiac membranes
Drug: pindolol
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.4
Action type: PARTIAL AGONIST
Drug: pindolol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9
Action type: PARTIAL AGONIST
Drug: pindolol
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.1
Drug: pindolol
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5
Action type: AGONIST
Drug: pindolol
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.7
Action type: AGONIST
Drug: pindolol
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.27
Assay: Evaluated for the binding affinity to porcine choroid plexus at 5-hydroxytryptamine 2C receptor binding site by using [3H]-MES as a radioligand.
Drug: pindolol
Target: Beta-3 adrenergic receptor (GPCR)
Gene: ADRB3
UniProt: P13945 (ADRB3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.78
Assay: Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells