AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: piroxicam
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P05979 (PGH1_SHEEP)
Organism: Ovis aries
Activity: IC50 = 4.68
Assay: Tested for inhibitory activity against Prostaglandin G/H synthase 1 from ovine
Drug: piroxicam
Target: Cyclooxygenase (Enzyme)
Gene: PTGS1|PTGS2
UniProt: O62664|O62698 (PGH1_BOVIN|PGH2_BOVIN)
Organism: Bos taurus
Activity: IC50 = 4.19
Assay: Inhibition of bovine Prostaglandin G/H synthase after oral administration
Drug: piroxicam
Target: Cyclooxygenase (Enzyme)
Gene: Ptgs2|Ptgs1
UniProt: P35355|Q63921 (PGH2_RAT|PGH1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7
Assay: In vitro inhibitory activity against Prostaglandin G/H synthase in rat neutrophils
Drug: pirprofen
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Drug: pirprofen
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Drug: pitavastatin
Target: 3-hydroxy-3-methylglutaryl-coenzyme A reductase (Enzyme)
Gene: HMGCR
UniProt: P04035 (HMDH_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.168
Action type: INHIBITOR
Drug: pitavastatin
Target: Retinoic acid receptor RXR-alpha (Nuclear hormone receptor)
Gene: RXRA
UniProt: P19793 (RXRA_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.88
Assay: Binding affinity to RXRalpha-LBD (unknown origin) measured up to 120 sec by surface plasma resonance method
Drug: pitavastatin
Target: 3-hydroxy-3-methylglutaryl-coenzyme A reductase (Enzyme)
Gene: Hmgcr
UniProt: P51639 (HMDH_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.98
Assay: Inhibition of Holtzman-Sprague-Dawley rat liver HMG CoA reductase after 30 mins
Drug: pizotifen
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.62
Assay: Binding affinity to dopamine D2 receptor (unknown origin)
Drug: pizotifen
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.4
Action type: ANTAGONIST
Drug: pizotifen
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.12
Assay: Binding affinity to 5-HT2A receptor (unknown origin)
Drug: pizotifen
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.7
Assay: Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
Drug: pizotifen
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.85
Assay: Binding affinity to 5-HT2C receptor (unknown origin)
Drug: pizotifen
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.6
Assay: Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells by liquid scintillation counting analysis
Drug: pizotifen
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.7
Assay: Binding affinity to muscarinic M1 receptor (unknown origin)
Drug: polythiazide
Target: Solute carrier family 12 member 3 (Transporter)
Gene: SLC12A3
UniProt: P55017 (S12A3_HUMAN)
Organism: Homo sapiens
Activity: A2 = 9.09
Action type: INHIBITOR
Drug: pralidoxime
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P22303 (ACES_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.59
Action type: ACTIVATOR
Assay: Binding affinity to sarin-inhibited hemoglobin free human erythrocyte ghost acetylcholinesterase using acetylthiocholineiodide as substrate measured up to 1 hr by Ellman method
Drug: pralmorelin
Target: Growth hormone secretagogue receptor type 1 (GPCR)
Gene: Ghsr
UniProt: O08725 (GHSR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.3
Action type: AGONIST
Drug: pralmorelin
Target: Growth hormone secretagogue receptor type 1 (GPCR)
Gene: GHSR
UniProt: Q92847 (GHSR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Drug: pramipexole
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4
Assay: Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
Drug: pramipexole
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.6
Action type: AGONIST
Drug: pramipexole
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki  7.121
Drug: pramipexole
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.16
Drug: pramipexole
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.93
Assay: Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
Drug: pramipexole
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.925
Drug: pramipexole
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.2
Drug: pramipexole
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.668
Action type: AGONIST
Drug: pramipexole
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.571
Drug: pramipexole
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.455
Drug: pramipexole
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.78
Drug: pramipexole
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki  7.282
Drug: pramipexole
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.31
Action type: AGONIST
Assay: in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
Drug: pramipexole
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.51
Assay: Displacement of [3H]Spiperone from D2 receptor in Sprague-Dawley rat caudate-putamen
Drug: pramipexole
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P20288 (DRD2_BOVIN)
Organism: Bos taurus
Activity: Kd = 8.8
Assay: Binding affinity of compound against Dopamine receptor D2 was measured using [3H]pramipexole in Bovine striatal membranes
Drug: pramipexole
Target: D(3) dopamine receptor (GPCR)
Gene: Drd3
UniProt: P19020 (DRD3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.35
Assay: Displacement of [3H]R(+)-7-OH-DPAT from Sprague-Dawley rat dopamine D3 receptor after 90 mins
Drug: pramlintide
Target: Amylin receptor AMY2 (GPCR)
Gene: CALCR|RAMP2
UniProt: P30988|O60895 (CALCR_HUMAN|RAMP2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.64
Action type: AGONIST
Assay: HEK293S cells
Drug: pramlintide
Target: Amylin receptor AMY1 (GPCR)
Gene: CALCR|RAMP1
UniProt: P30988|O60894 (CALCR_HUMAN|RAMP1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 9.45
Action type: AGONIST
Assay: HEK293S cells
Drug: pramlintide
Target: Amylin receptor AMY3 (GPCR)
Gene: CALCR|RAMP3
UniProt: P30988|O60896 (CALCR_HUMAN|RAMP3_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 9.05
Action type: AGONIST
Assay: HEK293S cells
Drug: pranlukast
Target: Bile acid receptor (Nuclear hormone receptor)
Gene: NR1H4
UniProt: Q96RI1 (NR1H4_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.82
Assay: Partial agonist activity at human full-length FXR expressed in human HeLa cells co-expressing pSG5-RXR measured after 24 hrs by dual-glo luciferase reporter gene assay
Drug: pranlukast
Target: Cysteinyl leukotriene receptor 2 (GPCR)
Gene: CYSLTR2
UniProt: Q9NS75 (CLTR2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.44
Action type: ANTAGONIST
Drug: pranlukast
Target: Cysteinyl leukotriene receptor 1 (GPCR)
Gene: CYSLTR1
UniProt: Q2NNR5 (CLTR1_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 9.1
Assay: In vitro binding of Cysteinyl leukotriene receptor 1 to guinea pig lung membranes
Drug: pranlukast
Target: Cruzipain (Enzyme)
UniProt: P25779 (CYSP_TRYCR)
Organism: Trypanosoma cruzi
Activity: IC50 = 5.15
Assay: Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-100
Drug: pranlukast
Target: Uracil nucleotide/cysteinyl leukotriene receptor (GPCR)
Gene: GPR17
UniProt: Q13304 (GPR17_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.39
Assay: Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay
Drug: pranlukast
Target: Bile acid receptor (Nuclear other)
Gene: NR1H4
UniProt: Q96RI1 (NR1H4_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.82
Assay: Partial agonist activity at human full-length FXR expressed in human HeLa cells co-expressing pSG5-RXR measured after 24 hrs by dual-glo luciferase reporter gene assay
Drug: pranlukast
Target: Cysteinyl leukotriene receptor 1 (GPCR)
Gene: CYSLTR1
UniProt: Q9Y271 (CLTR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 10
Action type: ANTAGONIST
Drug: pranoprofen
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P05979 (PGH1_SHEEP)
Organism: Ovis aries
Activity: IC50 = 5.51
Assay: Inhibitory activity against COX-1 from ram seminal vesicles
Drug: pranoprofen
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: Ptgs1
UniProt: Q63921 (PGH1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.41
Assay: Inhibitory activity against COX-1 from rat peritoneal leukocytes, measured by PGE-2 produced (enzyme immunoassay)
Drug: pravastatin
Target: 3-hydroxy-3-methylglutaryl-coenzyme A reductase (Enzyme)
Gene: HMGCR
UniProt: P04035 (HMDH_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.52
Action type: INHIBITOR
Assay: Tested in vitro for the inhibition of HMG-CoA reductase from partially purified microsomal preparations.
Drug: pravastatin
Target: 3-hydroxy-3-methylglutaryl-coenzyme A reductase (Enzyme)
Gene: Hmgcr
UniProt: P51639 (HMDH_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.38
Assay: In vitro HMG-CoA reductase inhibitory activity to inhibit sterol synthesis in cell free system in rat
Drug: pravastatin
Target: Solute carrier family 22 member 6 (Transporter)
Gene: Slc22a6
UniProt: O35956 (S22A6_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.28
Assay: Inhibition of rat Oat1 expressed in pig LLC-PK11 cells
Drug: prazepam
Target: GABA-A receptor alpha-1/beta-2/gamma-2 (Ion channel)
Gene: GABRA1|GABRG2|GABRB2
UniProt: P14867|P18507|P47870 (GBRA1_HUMAN|GBRG2_HUMAN|GBRB2_HUMAN)
Organism: Homo sapiens
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: praziquantel
Target: Bile salt export pump (Transporter)
Gene: ABCB11
UniProt: O95342 (ABCBB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.01
Drug: praziquantel
Target: Glutathione S-transferase class-mu 26 kDa isozyme (Enzyme)
UniProt: P08515 (GST26_SCHJA)
Organism: Schistosoma japonicum
Drug: praziquantel
Target: High voltage-activated calcium channel beta subunit CavB1 (Ion channel)
UniProt: Q95US7 (Q95US7_SCHMA)
Organism: Schistosoma mansoni
Action type: BLOCKER
Assay: Mechanism of Action; CHEMBL2363079; SINGLE PROTEIN
Drug: praziquantel
Target: High voltage-activated calcium channel beta subunit CavB2 (Ion channel)
UniProt: Q962H3 (Q962H3_SCHMA)
Organism: Schistosoma mansoni
Action type: BLOCKER
Assay: Mechanism of Action; CHEMBL2363080; SINGLE PROTEIN
Drug: prednicarbate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action; CHEMBL2034; SINGLE PROTEIN
Drug: prednisolone
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.8
Action type: AGONIST
Drug: prednisolone
Target: Annexin A1 (Cytosolic other)
Gene: ANXA1
UniProt: P04083 (ANXA1_HUMAN)
Organism: Homo sapiens
Drug: prednisolone
Target: Mineralocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C2
UniProt: P08235 (MCR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.54
Assay: Displacement of [3H]-aldosterone from human mineralocorticoid receptor expressed in HEK293 cells
Drug: prednisolone
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.6
Assay: Displacement of [3H]-methyltrienolone from human androgen receptor expressed in HEK293 cells
Drug: prednisolone
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.68
Assay: Binding affinity to PR (unknown origin) by FP assay
Drug: prednisolone
Target: Corticosteroid-binding globulin (Secreted)
Gene: SERPINA6
UniProt: P08185 (CBG_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.51
Drug: prednisolone
Target: Interleukin-6 (Cytokine)
Gene: IL6
UniProt: P05231 (IL6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.38
Drug: prednisolone
Target: G-protein coupled bile acid receptor 1 (GPCR)
Gene: GPBAR1
UniProt: Q8TDU6 (GPBAR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.6
Assay: Agonist activity at TGR5 in human whole blood assessed as inhibition of LPS-induced TNF-alpha release
Drug: prednisolone
Target: Fatty acid-binding protein, liver (Unclassified)
Gene: Fabp1
UniProt: P02692 (FABPL_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.58
Assay: Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay
Drug: prednisolone
Target: Glutamine synthetase (Enzyme)
Gene: GLUL
UniProt: P15104 (GLNA_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.49
Assay: Ability to induce human glutamine synthetase in skeletal muscle cells
Drug: prednisolone
Target: Glucocorticoid receptor (Transcription factor)
Gene: Nr3c1
UniProt: P06536 (GCR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.28
Assay: Modulation of glucocorticoid receptor in rat whole blood
Drug: prednisolone
Target: Glucocorticoid receptor (Transcription factor)
Gene: Nr3c1
UniProt: P06537 (GCR_MOUSE)
Organism: Mus musculus
Activity: EC50 = 8.47
Assay: Inhibition of mouse glutamine synthetase by GR-mediated transactivation in C2C12 cells
Drug: prednisolone
Target: Disintegrin and metalloproteinase domain-containing protein 17 (Unclassified)
Gene: ADAM17
UniProt: P78536 (ADA17_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.83
Drug: prednisolone acetate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action; CHEMBL2034; SINGLE PROTEIN
Drug: prednisolone tebutate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.28
Action type: AGONIST
Assay: BindingDB_Patents: Fluorescence Polarization Ligand Binding Assay. The glucocorticoid receptor fluorescence polarization ligand binding (GRFP) assay is used to evaluate direct binding of testing compounds to full-length glucocorticoid (GR) protein. Reagents for this assay are purchased from Invitrogen in a test kit. A fluorescent labeled GR ligand is used as a fluorescent tracer and test compounds compete with the fluorescent tracer for GR binding. The change in polarization value in the presence of test compounds is due to binding of test compounds to GR and is used to determine IC50 and relative binding affinity of test compounds for GR.
Drug: prednisolone tebutate
Target: Mineralocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C2
UniProt: P08235 (MCR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.54
Assay: Displacement of [3H]-aldosterone from human mineralocorticoid receptor expressed in HEK293 cells
Drug: prednisolone tebutate
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.6
Assay: Displacement of [3H]-methyltrienolone from human androgen receptor expressed in HEK293 cells
Drug: prednisolone tebutate
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.68
Assay: Binding affinity to PR (unknown origin) by FP assay
Drug: prednisolone tebutate
Target: Corticosteroid-binding globulin (Secreted)
Gene: SERPINA6
UniProt: P08185 (CBG_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.51
Assay: Binding affinity to human CBG receptor (corticosteroid-binding globulins)
Drug: prednisolone tebutate
Target: Interleukin-6 (Cytokine)
Gene: IL6
UniProt: P05231 (IL6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.38
Assay: Fluorescence Polarization Ligand Binding Assay: The glucocorticoid receptor fluorescence polarization ligand binding (GRFP) assay is used to evaluate direct binding of testing compounds to full-length glucocorticoid (GR) protein. Reagents for this assay are purchased from Invitrogen in a test kit. A fluorescent labeled GR ligand is used as a fluorescent tracer and test compounds compete with the fluorescent tracer for GR binding. The change in polarization value in the presence of test compounds is due to binding of test compounds to GR and is used to determine IC50 and relative binding affinity of test compounds for GR.
Drug: prednisolone tebutate
Target: G-protein coupled bile acid receptor 1 (GPCR)
Gene: GPBAR1
UniProt: Q8TDU6 (GPBAR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.6
Assay: Agonist activity at TGR5 in human whole blood assessed as inhibition of LPS-induced TNF-alpha release
Drug: prednisolone tebutate
Target: Fatty acid-binding protein, liver (Unclassified)
Gene: Fabp1
UniProt: P02692 (FABPL_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.58
Assay: Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay
Drug: prednisolone tebutate
Target: Glutamine synthetase (Enzyme)
Gene: GLUL
UniProt: P15104 (GLNA_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.5
Assay: Ability to induce human glutamine synthetase in skeletal muscle cells
Drug: prednisolone tebutate
Target: Glucocorticoid receptor (Transcription factor)
Gene: Nr3c1
UniProt: P06536 (GCR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.28
Assay: Modulation of glucocorticoid receptor in rat whole blood
Drug: prednisolone tebutate
Target: Glucocorticoid receptor (Transcription factor)
Gene: Nr3c1
UniProt: P06537 (GCR_MOUSE)
Organism: Mus musculus
Activity: EC50 = 8.47
Assay: Inhibition of mouse glutamine synthetase by GR-mediated transactivation in C2C12 cells
Drug: prednisolone tebutate
Target: Disintegrin and metalloproteinase domain-containing protein 17 (Unclassified)
Gene: ADAM17
UniProt: P78536 (ADA17_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.83
Assay: Fluorescence Polarization Ligand Binding Assay: The glucocorticoid receptor fluorescence polarization ligand binding (GRFP) assay is used to evaluate direct binding of testing compounds to full-length glucocorticoid (GR) protein. Reagents for this assay are purchased from Invitrogen in a test kit. A fluorescent labeled GR ligand is used as a fluorescent tracer and test compounds compete with the fluorescent tracer for GR binding. The change in polarization value in the presence of test compounds is due to binding of test compounds to GR and is used to determine IC50 and relative binding affinity of test compounds for GR.
Drug: prednisone
Target: Sodium/nucleoside cotransporter 1 (Transporter)
Gene: SLC28A1
UniProt: O00337 (S28A1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.772
Assay: DRUGMATRIX: Sodium/nucleoside co-transporter radioligand binding (ligand: nitrobenzylthioinosine)
Drug: prednisone
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8
Action type: AGONIST
Drug: prednisone
Target: Annexin A1 (Cytosolic other)
Gene: ANXA1
UniProt: P04083 (ANXA1_HUMAN)
Organism: Homo sapiens
Drug: pregabalin
Target: Large neutral amino acids transporter small subunit 1 (Transporter)
Gene: SLC7A5
UniProt: Q01650 (LAT1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 3.801
Drug: pregabalin
Target: Voltage-dependent calcium channel subunit alpha-2/delta-1 (Ion channel)
Gene: CACNA2D1
UniProt: P54289 (CA2D1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.097
Action type: MODULATOR
Drug: pregabalin
Target: Uncharacterized protein; Voltage-dependent calcium channel alpha-2 delta subunit (Ion channel)
Gene: CACNA2D1
UniProt: O77773 (O77773_PIG)
Organism: Sus scrofa
Activity: IC50 = 7.14
Assay: Displacement of [3H]gabapentin from alpha-2delta calcium channel in pig brain membrane
Drug: pregabalin
Target: Voltage-dependent calcium channel subunit alpha-2/delta-2 (Ion channel)
Gene: CACNA2D2
UniProt: Q9NY47 (CA2D2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.26
Action type: MODULATOR
Drug: pregnenolone succinate
Target: Corticosteroid-binding globulin (Secreted)
Gene: SERPINA6
UniProt: P08185 (CBG_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.23
Drug: pregnenolone succinate
Target: Sex hormone-binding globulin (Secreted)
Gene: SHBG
UniProt: P04278 (SHBG_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.15
Assay: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin
Drug: pregnenolone succinate
Target: Glucose-6-phosphate 1-dehydrogenase (Enzyme)
Gene: G6PD
UniProt: P11413 (G6PD_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.09
Assay: Inhibition of human recombinant N-terminal His tagged G6PD expressed in Escherichia coli JM109 (DE3) cells assessed as production of NADPH after 30 mins by Amplite fluorimetric assay
Drug: prenalterol
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.6
Drug: prenalterol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: Q28044 (ADRB2_BOVIN)
Organism: Bos taurus
Activity: Kd = 5.97
Assay: Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug: prenylamine
Target: Sodium channel alpha subunits; brain (Types I, II, III) (Ion channel)
Gene: SCN1A|SCN2A|SCN3A
UniProt: P35498|Q99250|Q9NY46 (SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.52
Assay: Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex
Drug: prenylamine
Target: Voltage-gated L-type calcium channel (Ion channel)
Gene: Cacna1c|Cacna1d|Cacna1s
UniProt: P22002|P27732|Q02485 (CAC1C_RAT|CAC1D_RAT|CAC1S_RAT)
Organism: Rattus norvegicus
Activity: Kd = 6.68
Assay: Inhibition of [3H]nitrendipine binding to calcium channel of rat brain membranes.
Drug: prenylamine
Target: Calmodulin (Cytosolic other)
Gene: CALM
UniProt: P62157 (CALM_BOVIN)
Organism: Bos taurus
Activity: Kd = 6.3
Assay: Binding affinity to dansylated bovine testes CaM by fluorescence analysis in presence of calcium2+
Drug: pridinol
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.796
Drug: pridinol
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.15
Drug: pridinol
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.194
Drug: pridinol
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.585
Drug: pridinol
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.799