AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: pergolide
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.98
Drug: pergolide
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.5
Drug: pergolide
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 9
Action type: AGONIST
Drug: pergolide
Target: D(1B) dopamine receptor (GPCR)
Gene: DRD5
UniProt: P21918 (DRD5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.76
Action type: AGONIST
Drug: pergolide
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.6
Drug: pergolide
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.9
Drug: pergolide
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.2
Drug: pergolide
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: pergolide
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.25
Action type: AGONIST
Drug: pergolide
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.128
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: pergolide
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.16
Drug: pergolide
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.838
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: pergolide
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.398
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug: pergolide
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.71
Drug: pergolide
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Kd = 8.4
Assay: In vitro affinity at mutant D2 receptor (S194A) in C6 (glioma) cell membranes.
Drug: pergolide
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.82
Drug: pergolide
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32305 (5HT7R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9
Action type: AGONIST
Drug: pergolide
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P20288 (DRD2_BOVIN)
Organism: Bos taurus
Activity: IC50 = 7.32
Assay: Inhibitory activity against Dopamine receptor D2 in calf corpus striatum using [3H]spiperone as radioligand
Drug: pergolide
Target: D(3) dopamine receptor (GPCR)
Gene: Drd3
UniProt: P19020 (DRD3_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.62
Assay: Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
Drug: pergolide
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: Htr6
UniProt: P31388 (5HT6R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.5
Action type: AGONIST
Drug: pergolide
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 = 7.39
Assay: Alpha-2 adrenergic receptor activity assessed in vitro for displacement of [3H]clonidine from specific binding sites on rat striatal membranes
Drug: pergolide
Target: Dopamine receptor (GPCR)
Gene: DRD2|DRD1
UniProt: P20288|Q95136 (DRD2_BOVIN|DRD1_BOVIN)
Organism: Bos taurus
Activity: IC50 = 7.74
Assay: In vitro inhibitory activity against dopamine receptor from calf caudate using [3H]dopamine as radioligand
Drug: pergolide
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 = 8.51
Assay: In vitro affinity for dopamine receptor by displacement of [3H]- apomorphine in rat striatal membranes
Drug: pergolide
Target: Cerebral cortex alpha adrenergic receptor (GPCR)
Gene: ADRA1A|ADRA2A
UniProt: P18130|Q28838 (ADA1A_BOVIN|ADA2A_BOVIN)
Organism: Bos taurus
Activity: IC50 = 7.39
Assay: In vitro affinity for alpha adrenergic receptor by displacement of 3[H]clonidine in calf cerebral cortex
Drug: pergolide
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.3
Action type: AGONIST
Drug: pergolide
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.47
Action type: AGONIST
Drug: perhexiline
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.962
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: perhexiline
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.11
Assay: Inhibition of human Potassium channel HERG expressed in mammalian cells
Drug: perhexiline
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.486
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: perhexiline
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.185
Assay: DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: perhexiline
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.18
Assay: DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: perhexiline
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.3
Assay: DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: perhexiline
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.105
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: perhexiline
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.027
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: perhexiline
Target: Voltage-dependent T-type calcium channel subunit alpha-1G (Ion channel)
Gene: CACNA1G
UniProt: O43497 (CAC1G_HUMAN)
Organism: Homo sapiens
Drug: perhexiline
Target: Voltage-dependent T-type calcium channel subunit alpha-1H (Ion channel)
Gene: CACNA1H
UniProt: O95180 (CAC1H_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.356
Drug: perhexiline
Target: Voltage-dependent T-type calcium channel subunit alpha-1I (Ion channel)
Gene: CACNA1I
UniProt: Q9P0X4 (CAC1I_HUMAN)
Organism: Homo sapiens
Drug: perhexiline
Target: Carnitine O-palmitoyltransferase 1, liver isoform (Enzyme)
Gene: CPT1A
UniProt: P50416 (CPT1A_HUMAN)
Organism: Homo sapiens
Drug: perhexiline
Target: Carnitine O-palmitoyltransferase 2, mitochondrial (Enzyme)
Gene: CPT2
UniProt: P23786 (CPT2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.14
Assay: Inhibition of human CPT2
Drug: perhexiline
Target: Epidermal growth factor receptor (Kinase)
Gene: EGFR
UniProt: P00533 (EGFR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.828
Assay: DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: perhexiline
Target: Tyrosine-protein kinase Fyn (Kinase)
Gene: FYN
UniProt: P06241 (FYN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.391
Assay: DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: perhexiline
Target: Carnitine O-palmitoyltransferase 1, muscle isoform (Enzyme)
Gene: Cpt1b
UniProt: Q63704 (CPT1B_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.96
Assay: Inhibition of Wistar rat heart mitochondrial CPT-1 assessed as reduction in conversion of palmitoyl CoA and L-carnitine into palmitoylcarnitine preincubated for 3 mins followed by L-carnitine and palmitoyl CoA addition measured for 3.5 mins by spectrophotometric analysis
Drug: perhexiline
Target: Adrenergic receptor alpha-1 (GPCR)
Gene: Adra1b|Adra1d|Adra1a
UniProt: P15823|P23944|P43140 (ADA1B_RAT|ADA1D_RAT|ADA1A_RAT)
Organism: Rattus norvegicus
Activity: Kd = 6.7
Assay: Alpha adrenergic receptor activity in rat aorta
Drug: perhexiline
Target: Carnitine palmitoyltransferase 2 (Enzyme)
Gene: Cpt2
UniProt: P18886 (CPT2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.1
Assay: Inhibition of CPT2 in rat mitochondria using [3H]carnitine by radiometric method
Drug: perhexiline
Target: Carnitine palmitoyltransferase 1A (Enzyme)
Gene: Cpt1a
UniProt: P32198 (CPT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.11
Assay: Inhibition of CPT1 in rat cardiac mitochondria using [3H]carnitine by radiometric method
Drug: periciazine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8
Action type: ANTAGONIST
Drug: periciazine
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.52
Assay: Displacement of [3H]mibolerone from rat androgen receptor
Drug: periciazine
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P23795 (ACES_BOVIN)
Organism: Bos taurus
Activity: IC50 = 5.15
Assay: Inhibition of bovine erythrocyte AChE using acetylthiocholine iodide as a substrate after 20 mins by Ellman's assay
Drug: periciazine
Target: Cholinesterase (Enzyme)
Gene: BCHE
UniProt: P81908 (CHLE_HORSE)
Organism: Equus caballus
Activity: IC50 = 6.64
Assay: Inhibition of Equine serum BChE using butyrylthiocholine iodide as a substrate after 20 mins by Ellman's assay
Drug: perindopril
Target: Angiotensin-converting enzyme (Enzyme)
Gene: ACE
UniProt: P12821 (ACE_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.82
Action type: INHIBITOR
Assay: Inhibition of ACE (unknown origin)
Drug: perlapine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.222
Drug: perlapine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.704
Drug: perlapine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.824
Drug: perlapine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7
Drug: perlapine
Target: Histamine H4 receptor (GPCR)
Gene: HRH4
UniProt: Q9H3N8 (HRH4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.32
Drug: perlapine
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.523
Drug: perlapine
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.57
Assay: Inhibition of spiropiperidone binding at dopamine receptor D2 of rat.
Drug: perospirone
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.22
Action type: ANTAGONIST
Drug: perospirone
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.55
Action type: ANTAGONIST
Drug: perospirone
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 10.05
Action type: ANTAGONIST
Drug: perospirone
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: Htr2a
UniProt: P14842 (5HT2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.74
Action type: ANTAGONIST
Drug: perphenazine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.32
Action type: ANTAGONIST
Drug: perphenazine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.19
Drug: perphenazine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.462
Assay: DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole)
Drug: perphenazine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.07
Drug: perphenazine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.252
Drug: perphenazine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.879
Drug: perphenazine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.55
Drug: perphenazine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.638
Drug: perphenazine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8
Drug: perphenazine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.979
Drug: perphenazine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.521
Drug: perphenazine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.088
Drug: perphenazine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.733
Drug: perphenazine
Target: Aldehyde oxidase (Enzyme)
Gene: AOX1
UniProt: Q06278 (AOXA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.481
Drug: perphenazine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.07
Drug: perphenazine
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.588
Drug: perphenazine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32305 (5HT7R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.6
Action type: ANTAGONIST
Drug: perphenazine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: Htr6
UniProt: P31388 (5HT6R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.8
Action type: ANTAGONIST
Drug: perphenazine
Target: Pleiotropic ABC efflux transporter of multiple drugs (Transporter)
Gene: PDR5
UniProt: P33302 (PDR5_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: IC50 = 5.85
Assay: Inhibition of Pdr5p-mediated rhodamine 6G transport in Saccharomyces cerevisiae MKPDR5h plasma membrane by spectrofluorometric assay
Drug: phenacemide
Target: Sodium channel protein type 1 subunit alpha (Ion channel)
Gene: SCN1A
UniProt: P35498 (SCN1A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: phenacetin
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Drug: phenazocine
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.7
Assay: Displacement of [3H]DAMGO form human mu opioid receptor expressed in CHO cells
Drug: phenazocine
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.7
Assay: Displacement of [3H]U69593 form human kappa opioid receptor expressed in CHO cells
Drug: phenazocine
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.3
Assay: Displacement of [3H]Naltrindole form human delta opioid receptor expressed in CHO cells
Drug: phenazocine
Target: Mu-type opioid receptor (GPCR)
Gene: Oprm1
UniProt: P42866 (OPRM_MOUSE)
Organism: Mus musculus
Activity: IC50 = 8.1
Assay: Ability to induce 50% of maximal effect in mouse vas deferens expressing Opioid receptor delta 1
Drug: phenazocine
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P97266 (OPRM_CAVPO)
Organism: Cavia porcellus
Activity: IC50 = 8.01
Assay: Ability to induce 50% of maximal effect in guinea pig ileum expressing Opioid receptor mu 1
Drug: phenazopyridine
Target: Sodium channel alpha subunit (Ion channel)
Gene: SCN1A|SCN4A|SCN7A|SCN5A|SCN9A|SCN2A|SCN3A|SCN11A|SCN8A|SCN10A
UniProt: P35498|P35499|Q01118|Q14524|Q15858|Q99250|Q9NY46|Q9UI33|Q9UQD0|Q9Y5Y9 (SCN1A_HUMAN|SCN4A_HUMAN|SCN7A_HUMAN|SCN5A_HUMAN|SCN9A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN|SCNBA_HUMAN|SCN8A_HUMAN|SCNAA_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Assay: Mechanism of Action; CHEMBL2331043; PROTEIN FAMILY
Drug: phenazopyridine
Target: Snake venom metalloproteinase Bap1 (Enzyme)
UniProt: P83512 (VM1B1_BOTAS)
Organism: Bothrops asper
Activity: IC50 = 4.27
Assay: Inhibition of snake venom BaP1 using Abz-Ala-Gly-Leu-Ala-Nba as substrate incubated for 30 mins prior to substrate addition by fluorescence spectrophotometry
Drug: phencyclidine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.96
Assay: Compound was evaluated for its ability to displace [3H](+)-pentazocine from sigma receptor in Guinea pig brain
Drug: phencyclidine
Target: Lysosomal Pro-X carboxypeptidase (Enzyme)
Gene: PRCP
UniProt: P42785 (PCP_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.04
Assay: Inhibition of [3H]-TCP binding to PCP receptor obtained from tissue homogenate preparation of fresh whole rat brain minus cerebellum
Drug: phencyclidine
Target: Glutamate receptor ionotropic, NMDA 1 (Ion channel)
Gene: Grin1
UniProt: P35439 (NMDZ1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.28
Assay: Binding affinity by displacement of [3H]TCP from PCP N-methyl-D-aspartate glutamate receptor of tissue homogenate preparation of rat brain without cerebellum (in vitro)
Drug: phencyclidine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: Sigmar1
UniProt: Q9R0C9 (SGMR1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.28
Assay: Inhibition of [3H]NANM binding to sigma receptor obtained from tissue homogenate preparation of fresh whole rat brain minus cerebellum
Drug: phencyclidine
Target: Glutamate receptor ionotropic, NMDA 2C (Ion channel)
Gene: Grin2c
UniProt: Q00961 (NMDE3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.22
Assay: Binding affinity against phencyclidine receptor was determined by the displacement of [3H]TCP of whole rat brain minus cerebellum.
Drug: phencyclidine
Target: Cholinesterase (Enzyme)
Gene: Bche
UniProt: Q03311 (CHLE_MOUSE)
Organism: Mus musculus
Activity: Ki = 6.28
Assay: Compound was evaluated for the protection of butyrylcholinesterase against DFT in mice
Drug: phencyclidine
Target: Acetylcholine receptor subunit alpha (Ion channel)
Gene: CHRNA1
UniProt: P02710 (ACHA_TORCA)
Organism: Torpedo californica
Activity: IC50 = 6.66
Assay: Displacement of [3H]PCP from nAChR in Torpedo nobiliana electric organs membranes in presence of 100 uM carbachol by scintillation counting method
Drug: phencyclidine
Target: Glutamate [NMDA] receptor (Ion channel)
Gene: GRIN2D|GRIN3B|GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN3A
UniProt: O15399|O60391|Q05586|Q12879|Q13224|Q14957|Q8TCU5 (NMDE4_HUMAN|NMD3B_HUMAN|NMDZ1_HUMAN|NMDE1_HUMAN|NMDE2_HUMAN|NMDE3_HUMAN|NMD3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.82
Assay: Affinity to NMDA receptor, using [3H]MK-801 as radioligand in pig brain cortex membranes
Drug: phencyclidine
Target: Glutamate NMDA receptor (Ion channel)
Gene: Grin1|Grin2a|Grin2b|Grin2c|Grin2d|Grin3b|Grin3a
UniProt: P35439|Q00959|Q00960|Q00961|Q62645|Q8VHN2|Q9R1M7 (NMDZ1_RAT|NMDE1_RAT|NMDE2_RAT|NMDE3_RAT|NMDE4_RAT|NMD3B_RAT|NMD3A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.42
Assay: Binding affinity was determined towards NMDA receptor using [3H]thienylcyclidine as radioligand
Drug: phencyclidine
Target: Glutamate NMDA receptor; GRIN1/GRIN2B (Ion channel)
Gene: GRIN1|GRIN2B
UniProt: Q05586|Q13224 (NMDZ1_HUMAN|NMDE2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.9
Assay: Inhibition of human recombinant NR1/NR2B receptor expressed in U2OS assessed as change in intracellular calcium level by FLIPR assay
Drug: phencyclidine
Target: Glutamate NMDA receptor; GRIN1/GRIN2A (Ion channel)
Gene: GRIN1|GRIN2A
UniProt: Q05586|Q12879 (NMDZ1_HUMAN|NMDE1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.4
Assay: Inhibition of human recombinant NR1/NR2A receptor expressed in U2OS assessed as change in intracellular calcium level by FLIPR assay
Drug: phencyclidine
Target: Muscarinic acetylcholine receptor (GPCR)
Gene: Chrm1|Chrm4|Chrm5|Chrm3|Chrm2
UniProt: P12657|P32211|Q920H4|Q9ERZ3|Q9ERZ4 (ACM1_MOUSE|ACM4_MOUSE|ACM5_MOUSE|ACM3_MOUSE|ACM2_MOUSE)
Organism: Mus musculus
Activity: Kd = 5.04
Assay: Dissociation constant towards Muscarinic acetylcholine receptor was determined by using [3H]4NMPB as radioligand
Drug: phendimetrazine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL222; SINGLE PROTEIN
Drug: phendimetrazine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.9
Assay: Binding affinity to 5HT1A receptor
Drug: phendimetrazine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL238; SINGLE PROTEIN
Drug: phenelzine
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.699
Assay: DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin)
Drug: phenelzine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.076
Drug: phenelzine
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: phenelzine
Target: Cytochrome P450 2C8 (Enzyme)
Gene: CYP2C8
UniProt: P10632 (CP2C8_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.14
Action type: INHIBITOR
Drug: phenelzine
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.398
Assay: DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: phenelzine
Target: Amine oxidase [flavin-containing] B (Enzyme)
Gene: MAOB
UniProt: P27338 (AOFB_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.82
Action type: INHIBITOR
Drug: phenelzine
Target: Amine oxidase [flavin-containing] A (Enzyme)
Gene: MAOA
UniProt: P21397 (AOFA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.836
Action type: INHIBITOR
Assay: DRUGMATRIX: Monoamine Oxidase MAO-A enzyme inhibition (substrate: Kynuramine)
Drug: phenelzine
Target: Cytochrome P450 2C19 (Enzyme)
Gene: CYP2C19
UniProt: P33261 (CP2CJ_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.097
Assay: DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)