AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: opipramol
Target: C-8 sterol isomerase (Enzyme)
Gene: ERG2
UniProt: P32352 (ERG2_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: Ki = 7.77
Assay: Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand
Drug: orlistat
Target: Cannabinoid receptor 1 (GPCR)
Gene: CNR1
UniProt: P21554 (CNR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.6
Assay: Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells by scintillation counting
Drug: orlistat
Target: Lipoprotein lipase (Enzyme)
Gene: LPL
UniProt: P06858 (LIPL_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.18
Assay: Inhibition of recombinant human LPL expressed in COS7 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay
Drug: orlistat
Target: Fatty acid synthase (Enzyme)
Gene: FASN
UniProt: P49327 (FAS_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.33
Assay: Inhibition of human FAS thioster domain preincubated for 30 mins followed by 4-methylumbelliferyl heptanoate substrate addition measured every 5 mins for 60 mins by fluorescence assay
Drug: orlistat
Target: Sn1-specific diacylglycerol lipase alpha (Enzyme)
Gene: DAGLA
UniProt: Q9Y4D2 (DGLA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8
Assay: Inhibition of human DAGLalpha expressed in HEK293T cell membrane using [14C]SAG substrate in detergent free solution by FRET assay
Drug: orlistat
Target: Fatty-acid amide hydrolase 1 (Enzyme)
Gene: Faah
UniProt: P97612 (FAAH1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8
Assay: Inhibition of rat histidine tagged FAAH expressed in Escherichia coli by coumarin ester substrate fluorescence assay
Drug: orlistat
Target: Sn1-specific diacylglycerol lipase beta (Enzyme)
Gene: DAGLB
UniProt: Q8NCG7 (DGLB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.22
Assay: Inhibition of human recombinant DAGLbeta overexpressed in african green monkey COS7 cells
Drug: orlistat
Target: Abhydrolase domain-containing protein 16A (Enzyme)
Gene: ABHD16A
UniProt: O95870 (ABHGA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.52
Assay: Inhibition of recombinant BAT5 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe
Drug: orlistat
Target: Monoacylglycerol lipase ABHD12 (Enzyme)
Gene: ABHD12
UniProt: Q8N2K0 (ABD12_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.1
Assay: Inhibition of recombinant ABHD12 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe
Drug: orlistat
Target: Platelet-activating factor acetylhydrolase (Enzyme)
Gene: PLA2G7
UniProt: Q13093 (PAFA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.3
Assay: Inhibition of recombinant PLA2g7 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe
Drug: orlistat
Target: Pancreatic triacylglycerol lipase (Enzyme)
Gene: PNLIP
UniProt: P00591 (LIPP_PIG)
Organism: Sus scrofa
Activity: IC50 = 6.66
Assay: Inhibition of porcine pancreatic lipase using micellar solution of triolein as substrate preincubated for 5 mins before substrate addition measured after 30 mins
Drug: orlistat
Target: Monoacylglycerol lipase ABHD6 (Enzyme)
Gene: ABHD6
UniProt: Q9BV23 (ABHD6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.32
Drug: orlistat
Target: Sn1-specific diacylglycerol lipase alpha (Enzyme)
Gene: Dagla
UniProt: Q6WQJ1 (DGLA_MOUSE)
Organism: Mus musculus
Activity: IC50 = 7.7
Assay: Inhibition of DAGLalpha in mouse N18TG2 cells assessed as inhibition of ionomycin-induced formation of 2-AG incubated for 20 mins by LC-MS analysis
Drug: orlistat
Target: Hepatic triacylglycerol lipase (Enzyme)
Gene: LIPC
UniProt: P11150 (LIPC_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.52
Assay: Inhibition of recombinant human HL expressed in COS7 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay
Drug: orlistat
Target: Endothelial lipase (Enzyme)
Gene: LIPG
UniProt: Q9Y5X9 (LIPE_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.22
Assay: Inhibition of endothelial lipase in human HT1080 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay
Drug: orlistat
Target: Pancreatic triacylglycerol lipase (Enzyme)
Gene: PNLIP
UniProt: P16233 (LIPP_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.9
Action type: INHIBITOR
Drug: orlistat
Target: Gastric triacylglycerol lipase (Enzyme)
Gene: LIPF
UniProt: P07098 (LIPG_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL1796; SINGLE PROTEIN
Drug: orphenadrine
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.886
Action type: BLOCKER
Drug: orphenadrine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.092
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: orphenadrine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.174
Drug: orphenadrine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.614
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: orphenadrine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.578
Action type: INHIBITOR
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: orphenadrine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.903
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: orphenadrine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.666
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: orphenadrine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.553
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: orphenadrine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.283
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: orphenadrine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.063
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: orphenadrine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.959
Action type: ANTAGONIST
Drug: orphenadrine
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.165
Assay: DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug: orphenadrine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.39
Drug: orphenadrine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.873
Assay: DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: orphenadrine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.432
Assay: DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: orphenadrine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.77
Assay: DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: orphenadrine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.699
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: orphenadrine
Target: Sodium channel protein type 1 subunit alpha (Ion channel)
Gene: SCN1A
UniProt: P35498 (SCN1A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.889
Action type: BLOCKER
Drug: orphenadrine
Target: Sodium channel protein type 4 subunit alpha (Ion channel)
Gene: SCN4A
UniProt: P35499 (SCN4A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.658
Action type: BLOCKER
Drug: orphenadrine
Target: Sodium channel protein type 9 subunit alpha (Ion channel)
Gene: SCN9A
UniProt: Q15858 (SCN9A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.764
Action type: BLOCKER
Drug: orphenadrine
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.398
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: orphenadrine
Target: Sodium channel protein type 10 subunit alpha (Ion channel)
Gene: SCN10A
UniProt: Q9Y5Y9 (SCNAA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.201
Action type: BLOCKER
Drug: orphenadrine
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.9
Assay: Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Drug: orphenadrine
Target: Histamine H1 receptor (GPCR)
Gene: Hrh1
UniProt: P31390 (HRH1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.79
Assay: Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug: orphenadrine
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 = 5.22
Assay: The compound was tested for its ability to block PCP N-methyl-D-aspartate glutamate receptor at the PCP (phencyclidine) binding site in postmortem human frontal cortex.
Drug: oseltamivir
Target: Neuraminidase (Enzyme)
UniProt: P06818 (NRAM_I79A0)
Organism: Influenza A virus (strain A/Bangkok/1/1979 H3N2)
Activity: IC50 = 9.83
Drug: oseltamivir
Target: Neuraminidase (Enzyme)
UniProt: P16207 (NRAM_INBVI)
Organism: Influenza B virus (strain B/Victoria/3/1985)
Activity: IC50 = 8.1
Drug: oseltamivir
Target: Neuraminidase (Enzyme)
UniProt: P03468 (NRAM_I34A1)
Organism: Influenza A virus (strain A/Puerto Rico/8/1934 H1N1)
Activity: IC50 = 8.15
Action type: INHIBITOR
Assay: Inhibition of human Influenza A virus A/PR/8/34(H1N1) neuraminidase by fluorometric method using 4MU-NeuAc substrate
Drug: oseltamivir
Target: Neuraminidase (Enzyme)
UniProt: P03474 (NRAM_INBLE)
Organism: Influenza B virus (strain B/Lee/1940)
Activity: Ki = 8.96
Action type: INHIBITOR
Assay: Inhibition of influenza B/Memphis/3/89 neuraminidase
Drug: oseltamivir
Target: Neuraminidase (Enzyme)
UniProt: B4URF0 (B4URF0_9INFA)
Organism: Influenza A virus (A/WSN/1933(H1N1))
Activity: IC50 = 10.22
Assay: Inhibition of Influenza Virus A/Horneburg/IDT7489/08 (H1N1) neuraminidase
Drug: oseltamivir
Target: Sialidase (Enzyme)
Gene: nanH
UniProt: P10481 (NANH_CLOPF)
Organism: Clostridium perfringens
Activity: IC50 = 9
Assay: Inhibition of Clostridium perfringenes neuraminidase activity using 4-methylumbelliferyl-1-alpha-D-N-acetylneuramic acid sodium salt hydrate as substrate by fluorescence based assay
Drug: oseltamivir
Target: Neuraminidase (Enzyme)
UniProt: Q75VQ4 (NRAM_I68A0)
Organism: Influenza A virus (strain A/Aichi/2/1968 H3N2)
Activity: IC50 = 8.81
Assay: Inhibition of human influenza A virus A/Aichi/2/1968(H3N2) neuraminidase by fluorometric method using 4MU-NeuAc substrate
Drug: oseltamivir
Target: Neuraminidase (Enzyme)
UniProt: Q6Q793 (Q6Q793_9INFA)
Organism: Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1))
Activity: Ki = 10
Assay: Inhibition of Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1)) neuraminidase by by Michaelis-Menten equation analysis
Drug: oseltamivir
Target: Neuraminidase (Enzyme)
UniProt: A5Z252 (A5Z252_9INFA)
Organism: Influenza A virus (A/Turkey/651242/2006(H5N1))
Activity: Ki = 8.1
Assay: Inhibition of Influenza A virus (A/Turkey/651242/2006(H5N1)) neuraminidase by Michaelis-Menten equation analysis
Drug: oseltamivir
Target: Neuraminidase (Enzyme)
UniProt: Q2LFS1 (Q2LFS1_9INFA)
Organism: Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1))
Activity: Ki = 8.31
Assay: Inhibition of Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1)) neuraminidase by Michaelis-Menten equation analysis
Drug: oseltamivir
Target: Neuraminidase (Enzyme)
UniProt: C4LRQ6 (C4LRQ6_9INFA)
Organism: Influenza A virus (A/duck/Laos/25/2006(H5N1))
Activity: Ki = 8.96
Assay: Inhibition of Influenza A virus (A/duck/Laos/25/2006(H5N1)) neuraminidase by Michaelis-Menten equation analysis
Drug: oseltamivir
Target: Neuraminidase (Enzyme)
UniProt: Q20MD3 (Q20MD3_9INFA)
Organism: Influenza A virus (A/udorn/1972(H3N2))
Activity: IC50 = 8.54
Drug: oseltamivir
Target: Neuraminidase (Enzyme)
UniProt: P03470 (NRAM_I33A0)
Organism: Influenza A virus (strain A/Wilson-Smith/1933 H1N1)
Activity: IC50 = 6.32
Drug: oseltamivir
Target: Neuraminidase (Enzyme)
UniProt: Q194T1 (Q194T1_9INFA)
Organism: Influenza A virus (A/RI/5+/1957(H2N2))
Activity: IC50 = 6.1
Assay: Inhibition of Influenza A virus (A/RI/5+/1957(H2N2)) recombinant neuraminidase using MUNANA as substrate after 30 mins
Drug: oseltamivir
Target: Neuraminidase (Enzyme)
UniProt: P03469 (NRAM_I77AB)
Organism: Influenza A virus (strain A/USSR/90/1977 H1N1)
Activity: IC50 = 8.86
Drug: oseltamivir
Target: Neuraminidase (Enzyme)
UniProt: Q07599 (NRAM_I63A3)
Organism: Influenza A virus (strain A/Duck/Ukraine/1/1963 H3N8)
Activity: IC50 = 8.05
Assay: Inhibition of Influenza A virus A/goose/Jiangsu/1306/2014(H5N8) neuraminidase N8 using fluorogenic MUNANA as substrate preincubated for 10 mins followed by substrate addition measured after 40 to 60 mins by fluorescence-based assay
Drug: oseltamivir
Target: Neuraminidase (Enzyme)
UniProt: P03471 (NRAM_I71A1)
Organism: Influenza A virus
Activity: IC50 = 9.96
Assay: Inhibition of influenza A virus H3N2 clinical isolate neuraminidase using NA-Fluor MUNANA as substrate preincubated for 20 to 30 mins followed by substrate addition and measured for 60 mins by fluorescence assay
Drug: oseltamivir
Target: Neuraminidase (Enzyme)
UniProt: Q6XV28 (NRAM_I77AG)
Organism: Influenza A virus
Activity: IC50 = 7.82
Assay: Inhibition of Influenza A virus A/duck/Guangdong/674/2014(H5N6) neuraminidase N6 using fluorogenic MUNANA as substrate preincubated for 10 mins followed by substrate addition measured after 40 to 60 mins by fluorescence-based assay
Drug: oteracil
Target: Uridine 5'-monophosphate synthase (Enzyme)
Gene: UMPS
UniProt: P11172 (UMPS_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action
Drug: ouabain
Target: Sodium/potassium-transporting ATPase subunit alpha-2 (Ion channel)
Gene: ATP1A2
UniProt: D2WKD8 (AT1A2_PIG)
Organism: Sus scrofa
Activity: IC50 = 6.169
Assay: DRUGMATRIX: ATPase, Na+/K+ enzyme inhibition (substrate: ATP)
Drug: ouabain
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.009
Drug: ouabain
Target: Sodium/potassium-transporting ATPase subunit alpha-1 (Transporter)
Gene: ATP1A1
UniProt: P05023 (AT1A1_HUMAN)
Organism: Homo sapiens
Drug: ouabain
Target: Signal transducer and activator of transcription 3 (Transcription factor)
Gene: STAT3
UniProt: P40763 (STAT3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.94
Assay: PUBCHEM_BIOASSAY: Dose response cell-based assay to measure STAT3 inhibition. (Class of assay: confirmatory) [Related pubchem assays: 920, 1317, 1265, 1308, 862 ]
Drug: oxacillin
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.85
Drug: oxacillin
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.02
Drug: oxacillin
Target: Penicillin-binding protein 1A (Enzyme)
Gene: pbpA
UniProt: Q8XJ01 (PBPA_CLOPE)
Organism: Clostridium perfringens (strain 13 / Type A)
Drug: oxacillin
Target: Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A (Enzyme)
Gene: PDE11A
UniProt: Q9HCR9 (PDE11_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.04
Drug: oxacillin
Target: Penicillin-binding protein (Enzyme)
Gene: pbp4|mecA|pbpA|PBP2|pbpF
UniProt: P72355|Q53707|Q53725|Q53729|Q9XDB3 (P72355_STAAU|Q53707_STAAU|Q53725_STAAU|Q53729_STAAU|Q9XDB3_STAAU)
Organism: Staphylococcus aureus
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2362972; PROTEIN FAMILY
Drug: oxametacin
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.55
Assay: Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production
Drug: oxametacin
Target: Arachidonate 5-lipoxygenase (Enzyme)
Gene: Alox5
UniProt: P12527 (LOX5_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.12
Assay: Tested for inhibition of 5-Lipoxygenase (ARBL) in calcium-stimulated rat basophilic leukemia cells(RBL-1)
Drug: oxametacin
Target: Cyclooxygenase (Enzyme)
Gene: Ptgs2|Ptgs1
UniProt: P35355|Q63921 (PGH2_RAT|PGH1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.96
Assay: Tested for inhibition of cyclooxygenase (ARBC) in calcium-stimulated rat basophilic leukemia cells(RBL-1)
Drug: oxandrolone
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Drug: oxaprozin
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.44
Action type: INHIBITOR
Drug: oxaprozin
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.068
Action type: INHIBITOR
Assay: DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid)
Drug: oxaprozin
Target: fMet-Leu-Phe receptor (GPCR)
Gene: FPR1
UniProt: P21462 (FPR1_HUMAN)
Organism: Homo sapiens
Drug: oxaprozin
Target: Bifunctional epoxide hydrolase 2 (Enzyme)
Gene: EPHX2
UniProt: P34913 (HYES_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.3
Action type: INHIBITOR
Assay: Inhibition of sEH's phosphatase activity <i>in vitro</i> using bacterially-expressed recombinant N-terminal domain of sEH.
Drug: oxaprozin
Target: Complement C5 (Secreted)
Gene: C5
UniProt: P01031 (CO5_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.19
Assay: Binding affinity to human C5a assessed as dissociation constant after 1 hr by circular dichroism analysis
Drug: oxaprozin
Target: Complement C5 (Unclassified)
Gene: C5
UniProt: P01031 (CO5_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.19
Assay: Binding affinity to human C5a assessed as dissociation constant after 1 hr by circular dichroism analysis
Drug: oxaprozin
Target: Serine hydroxymethyltransferase, mitochondrial (Enzyme)
Gene: SHMT2
UniProt: P34897 (GLYM_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.71
Assay: Inhibition of His-tagged human recombinant SHMT2 expressed in Escherichia coli BLR(DE3) assessed as reduction in NADPH level using L-serine, THF and NADP+ incubated for 5 mins by SHMT2-MTHFD coupled reaction based fluorescence assay
Drug: oxatomide
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.056
Drug: oxatomide
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.148
Drug: oxatomide
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.203
Drug: oxatomide
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.13
Drug: oxatomide
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P31389 (HRH1_CAVPO)
Organism: Cavia porcellus
Activity: IC50 = 8.05
Assay: Inhibitory activity against Tritiated [3H]- mepyramine binding to Histamine H1 receptor in guinea pig cerebral cortex
Drug: oxatomide
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.699
Action type: ANTAGONIST
Drug: oxazepam
Target: GABA-A receptor alpha-1/beta-3/gamma-2 (Ion channel)
Gene: GABRA1|GABRG2|GABRB3
UniProt: P14867|P18507|P28472 (GBRA1_HUMAN|GBRG2_HUMAN|GBRB3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.745
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: oxcarbazepine
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: oxyphencyclimine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Assay: Mechanism of Action; CHEMBL216; SINGLE PROTEIN
Drug: oxyphencyclimine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Assay: Mechanism of Action; CHEMBL245; SINGLE PROTEIN
Drug: oxprenolol
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.11
Action type: ANTAGONIST
Drug: oxprenolol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8
Action type: ANTAGONIST
Drug: oxprenolol
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.54
Assay: Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Drug: oxprenolol
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.03
Drug: oxybutynin
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.991
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: oxybutynin
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.589
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: oxybutynin
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.298
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: oxybutynin
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.837
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: oxybutynin
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.09
Action type: ANTAGONIST
Assay: Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M2 receptor expressed in Sf9 cells