AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: pindolol
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.1
Drug: pindolol
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.209
Drug: pindolol
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.1
Assay: Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug: pindolol
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.7
Assay: Evaluated for the binding affinity to hippocampus striatal membranes at 5-hydroxytryptamine 1A receptor binding site by using [3H]-8-OH- DPAT as a radioligand.
Drug: pindolol
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: Ki = 7
Assay: Evaluated for binding affinity towards rat cortical membranes at 5-hydroxytryptamine 1 receptor binding site by using [3H]-5-HT as a radioligand.
Drug: pindolol
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 = 4.53
Assay: Binding affinity to 5-hydroxytryptamine 2 receptor in rat frontal cortical membranes by [3H]- KET displacement.
Drug: pioglitazone
Target: Carbonic anhydrase 2 (Enzyme)
Gene: CA2
UniProt: P00918 (CAH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.943
Assay: DRUGMATRIX: Carbonic Anhydrase II enzyme inhibition (substrate: 4-Nitrophenyl acetate (4-NPA))
Drug: pioglitazone
Target: Bile salt export pump (Transporter)
Gene: ABCB11
UniProt: O95342 (ABCBB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.52
Drug: pioglitazone
Target: Amine oxidase [flavin-containing] B (Enzyme)
Gene: MAOB
UniProt: P27338 (AOFB_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.3
Assay: Competitive inhibition of human MAOB expressed in Pichia pastoris
Drug: pioglitazone
Target: Amine oxidase [flavin-containing] A (Enzyme)
Gene: MAOA
UniProt: P21397 (AOFA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.455
Assay: DRUGMATRIX: Monoamine Oxidase MAO-A enzyme inhibition (substrate: Kynuramine)
Drug: pioglitazone
Target: Peroxisome proliferator-activated receptor alpha (Nuclear hormone receptor)
Gene: PPARA
UniProt: Q07869 (PPARA_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.18
Assay: In vitro transactivation of human Peroxisome proliferator activated receptor alpha (hPPARalpha)
Drug: pioglitazone
Target: Peroxisome proliferator-activated receptor gamma (Nuclear hormone receptor)
Gene: PPARG
UniProt: P37231 (PPARG_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.23
Action type: AGONIST
Drug: pioglitazone
Target: Aldose reductase (Enzyme)
Gene: Akr1b1
UniProt: P07943 (ALDR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.879
Assay: DRUGMATRIX: Aldose Reductase enzyme inhibition (substrate: DL-Glyceraldehyde)
Drug: pioglitazone
Target: Amine oxidase [flavin-containing] B (Enzyme)
Gene: Maob
UniProt: P19643 (AOFB_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.68
Assay: Competitive inhibition of rat MAOB expressed in Pichia pastoris
Drug: pioglitazone
Target: Peroxisome proliferator-activated receptor alpha (Transcription factor)
Gene: Ppara
UniProt: P23204 (PPARA_MOUSE)
Organism: Mus musculus
Activity: IC50 = 5.94
Assay: Activation of mouse liver PPARalpha
Drug: pioglitazone
Target: Peroxisome proliferator-activated receptor gamma (Transcription factor)
Gene: Pparg
UniProt: P37238 (PPARG_MOUSE)
Organism: Mus musculus
Activity: IC50 = 6.15
Assay: Displacement of [3H]rosiglitazone from mouse PPARgamma receptor by scintillation proximation assay
Drug: pioglitazone
Target: Peroxisome proliferator-activated receptor gamma (Transcription factor)
Gene: Pparg
UniProt: O88275 (PPARG_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.15
Assay: Displacement of [3H]rosigliatzone from PPARgamma in rat adipocytes
Drug: pioglitazone
Target: Enoyl-[acyl-carrier-protein] reductase [NADH] (Enzyme)
Gene: fabI
UniProt: Q5NGQ3 (Q5NGQ3_FRATT)
Organism: Francisella tularensis subsp. tularensis (strain SCHU S4 / Schu 4)
Activity: IC50 = 4.1
Assay: Inhibition of C-terminal His6-tagged Francisella tularensis SCHU S4 FabI expressed in Escherichia coli BL21 (DE3) using CrCoA as substrate assessed as oxidation of NADH to NAD+ by fluorescence assay
Drug: pioglitazone
Target: Bile salt export pump (Transporter)
Gene: Abcb11
UniProt: O70127 (ABCBB_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.7
Drug: pioglitazone
Target: CDGSH iron-sulfur domain-containing protein 1 (Unclassified)
Gene: CISD1
UniProt: Q9NZ45 (CISD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.43
Assay: Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis
Drug: pioglitazone
Target: CDGSH iron-sulfur domain-containing protein 1 (Unclassified)
Gene: Cisd1
UniProt: B0K020 (CISD1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6
Assay: Displacement of [3H]rosiglitazone from rat liver mitochondrial mitoNEET by scintillation counting
Drug: pioglitazone
Target: Peroxisome proliferator-activated receptor alpha (Nuclear hormone receptor)
Gene: Ppara
UniProt: P23204 (PPARA_MOUSE)
Organism: Mus musculus
Activity: IC50 = 5.94
Assay: Activation of mouse liver PPARalpha
Drug: pioglitazone
Target: CDGSH iron-sulfur domain-containing protein 2 (Unclassified)
Gene: CISD2
UniProt: Q8N5K1 (CISD2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.32
Assay: Binding affinity to recombinant human N-terminal His6-tagged NAF1 expressed in Escherichia coli by scintillation proximity assay
Drug: pipamazine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.796
Assay: DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug: pipamazine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.87
Assay: DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
Drug: pipamazine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.602
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: pipamazine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.319
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: pipamazine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.461
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: pipamazine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.351
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: pipamazine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.992
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
Drug: pipamazine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.256
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: pipamazine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.509
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: pipamazine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.959
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: pipamazine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.284
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: pipamazine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.105
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: pipamazine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.799
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: pipamazine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.939
Assay: DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug: pipamazine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.646
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: pipamazine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.189
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: pipamazine
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: pipamazine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.02
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: pipamazine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.848
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: pipamazine
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.864
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug: pipamazine
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.429
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: pipamazine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.29
Drug: pipamazine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.75
Drug: pipamperone
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.301
Drug: pipamperone
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.301
Drug: pipamperone
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.94
Drug: pipamperone
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.066
Drug: pipamperone
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.6
Action type: ANTAGONIST
Drug: pipamperone
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.3
Action type: ANTAGONIST
Drug: pipamperone
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.324
Drug: pipamperone
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.644
Drug: pipamperone
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.456
Drug: pipamperone
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.602
Drug: pipamperone
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.6
Action type: ANTAGONIST
Drug: pipamperone
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.2
Action type: ANTAGONIST
Drug: pipamperone
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.8
Action type: ANTAGONIST
Drug: pipamperone
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.538
Drug: pipamperone
Target: 5-hydroxytryptamine receptor 1F (GPCR)
Gene: HTR1F
UniProt: P30939 (5HT1F_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.301
Drug: pipamperone
Target: 5-hydroxytryptamine receptor 1E (GPCR)
Gene: HTR1E
UniProt: P28566 (5HT1E_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.301
Drug: pipecuronium
Target: Neuronal acetylcholine receptor; alpha2/beta4 (Ion channel)
Gene: CHRNB4|CHRNA2
UniProt: P30926|Q15822 (ACHB4_HUMAN|ACHA2_HUMAN)
Organism: Homo sapiens
Drug: pipecuronium
Target: Acetylcholine receptor (Ion channel)
Gene: CHRNA1|CHRNB1|CHRND
UniProt: P02708|P11230|Q07001 (ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Drug: pipecuronium
Target: Neuronal acetylcholine receptor; alpha4/beta2 (Ion channel)
Gene: CHRNB2|CHRNA4
UniProt: P17787|P43681 (ACHB2_HUMAN|ACHA4_HUMAN)
Organism: Homo sapiens
Drug: pipecuronium
Target: Neuronal acetylcholine receptor; alpha4/beta4 (Ion channel)
Gene: CHRNB4|CHRNA4
UniProt: P30926|P43681 (ACHB4_HUMAN|ACHA4_HUMAN)
Organism: Homo sapiens
Drug: piperacillin
Target: Penicillin-binding protein 1A (Enzyme)
Gene: pbpA
UniProt: Q8XJ01 (PBPA_CLOPE)
Organism: Clostridium perfringens (strain 13 / Type A)
Drug: piperacillin
Target: Beta-lactamase (Enzyme)
Gene: blaPER-2
UniProt: A2RP81 (A2RP81_CITFR)
Organism: Citrobacter freundii
Activity: Ki = 6.7
Assay: Inhibition of Citrobacter freundii PER2 beta lactamase
Drug: piperacillin
Target: Streptokinase A (Enzyme)
Gene: ska
UniProt: P10520 (STRP_STRP1)
Organism: Streptococcus pyogenes serotype M1
Activity: EC50 = 6.55
Drug: piperacillin
Target: Bacterial penicillin-binding protein (Enzyme)
Gene: mrcA|mrcB|dacC|mrdA|ftsI|dacA|dacB
UniProt: P02918|P02919|P08506|P0AD65|P0AD68|P0AEB2|P24228 (PBPA_ECOLI|PBPB_ECOLI|DACC_ECOLI|PBP2_ECOLI|FTSI_ECOLI|DACA_ECOLI|DACB_ECOLI)
Organism: Escherichia coli (strain K12)
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2354204; PROTEIN FAMILY
Drug: piperazine
Target: Gamma-aminobutyric acid receptor subunit beta (Ion channel)
Gene: gab-1
UniProt: O18276 (GBRB_CAEEL)
Organism: Caenorhabditis elegans
Drug: pipotiazine palmitate
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.699
Action type: ANTAGONIST
Drug: pipotiazine palmitate
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.553
Drug: pirbuterol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Drug: pirenzepine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.68
Action type: ANTAGONIST
Drug: pirenzepine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.76
Assay: Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M2 receptor expressed in CHOK1 cells
Drug: pirenzepine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.61
Drug: pirenzepine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.12
Drug: pirenzepine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.55
Drug: pirenzepine
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.66
Assay: Inhibitory concentration against human Adenosine A3 receptor expressed in HEK293 cells using 0.1 nM [3H]AB-MECA
Drug: pirenzepine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: Chrm2
UniProt: P10980 (ACM2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.92
Assay: Inhibition of carbachol-induced release of alpha-amylase from pancreatic acinar cells from that of rat ileum contained the muscarinic acetylcholine receptor M2 subtypes
Drug: pirenzepine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: Chrm1
UniProt: P08482 (ACM1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.28
Assay: Displacement of [3H]pirenzepine from muscarinic acetylcholine receptor M1 in rat cortex homogenates
Drug: pirenzepine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: Chrm3
UniProt: P08483 (ACM3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.55
Assay: Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
Drug: pirenzepine
Target: Muscarinic receptor M1 (GPCR)
UniProt: Q8WMX0 (Q8WMX0_BOVIN)
Organism: Bos taurus
Activity: Ki = 8.44
Assay: Binding affinity against Muscarinic acetylcholine receptor M1 by displacement of [3H]pirenzepine in bovine striatum
Drug: pirenzepine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: Chrm4
UniProt: P08485 (ACM4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.48
Assay: Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells
Drug: pirenzepine
Target: Muscarinic acetylcholine receptor (GPCR)
Gene: GPM3
UniProt: Q8VH26 (Q8VH26_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 6.96
Assay: Binding affinity for muscarinic acetylcholine receptor M3 by measuring displacement of [3H]QNB from guinea pig parotid gland
Drug: pirenzepine
Target: Muscarinic acetylcholine receptor DM1 (GPCR)
Gene: mAChR-A
UniProt: P16395 (ACM1_DROME)
Organism: Drosophila melanogaster
Activity: Ki = 6.41
Assay: Displacement of [3H]AF-DX 384 from Drosophila melanogaster mAChR by scintillation counting
Drug: pirenzepine
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 = 7.22
Assay: Binding affinity against Muscarinic acetylcholine receptor was determined in homogenized rat cortex tissue using [3H]N-methylscopolamine as radioligand
Drug: pirenzepine
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: IC50 = 6.12
Assay: Ability (10 ug/kg) to inhibit binding of [125I]iododexetimide to muscarinic receptor in mice
Drug: piretanide
Target: Solute carrier family 12 member 1 (Transporter)
Gene: SLC12A1
UniProt: Q13621 (S12A1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.3
Action type: INHIBITOR
Drug: piretanide
Target: Solute carrier family 12 member 2 (Transporter)
Gene: SLC12A2
UniProt: P55011 (S12A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.62
Action type: INHIBITOR
Drug: piribedil
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.1
Action type: ANTAGONIST
Drug: piribedil
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.4
Action type: AGONIST
Drug: piribedil
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.9
Action type: ANTAGONIST
Drug: piribedil
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.1
Action type: ANTAGONIST
Drug: piribedil
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.54
Drug: piribedil
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.6
Action type: AGONIST
Drug: piribedil
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.2
Action type: ANTAGONIST
Drug: piribedil
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.5
Action type: ANTAGONIST
Drug: piribedil
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.66
Drug: piribedil
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.21
Drug: piribedil
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.9
Action type: AGONIST
Drug: pirlindole
Target: Transcriptional enhancer factor TEF-3 (Transcription factor)
Gene: TEAD4
UniProt: Q15561 (TEAD4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.44
Assay: Inhibition of Gal4-fused TEAD4 (unknown origin) interaction with YAP expressed in human HeLa cells assessed as basal transcriptional activity level after 6 hrs by nanoluciferase reporter gene assay
Drug: pirlindole
Target: Transcriptional enhancer factor TEF-1 (Transcription factor)
Gene: TEAD1
UniProt: P28347 (TEAD1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.92
Assay: Binding affinity to TEAD1 (194 to 411 residues) (unknown origin) by ITC assay
Drug: pirlindole
Target: Transcriptional enhancer factor TEF-4 (Transcription factor)
Gene: TEAD2
UniProt: Q15562 (TEAD2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.48
Assay: Inhibition of Gal4-fused TEAD2 (unknown origin) interaction with YAP expressed in human HeLa cells assessed as basal transcriptional activity level after 6 hrs by nanoluciferase reporter gene assay
Drug: pirlindole
Target: Transcriptional enhancer factor TEF-5 (Transcription factor)
Gene: TEAD3
UniProt: Q99594 (TEAD3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.36
Assay: Inhibition of Gal4-fused TEAD3 (unknown origin) interaction with YAP expressed in human HeLa cells assessed as basal transcriptional activity level after 6 hrs by nanoluciferase reporter gene assay
Drug: pirlindole
Target: Amine oxidase [flavin-containing] A (Enzyme)
Gene: MAOA
UniProt: P21397 (AOFA_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.409
Action type: INHIBITOR
Assay: Monoamine oxidase A (human liver form) inhibitor induced spectral changes
Drug: pirmenol
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Drug: piroxicam
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.7
Action type: INHIBITOR
Drug: piroxicam
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.18
Action type: INHIBITOR