AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: risperidone
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: Htr2c
UniProt: P08909 (5HT2C_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.84
Assay: Displacement of [3H]mesulergine from 5HT2C receptor in rat cerebral cortex after 15 mins by liquid scintillation counting analysis
Drug: risperidone
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: Q64264 (5HT1A_MOUSE)
Organism: Mus musculus
Activity: IC50 = 6.37
Assay: Inhibitory activity against serotonin 5-hydroxytryptamine 1A receptor from mice.
Drug: risperidone
Target: Histamine H1 receptor (GPCR)
Gene: Hrh1
UniProt: P31390 (HRH1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.1
Assay: Displacement of [3H]mepyramine from H1R in rat brain
Drug: risperidone
Target: D(3) dopamine receptor (GPCR)
Gene: Drd3
UniProt: P19020 (DRD3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.01
Assay: Displacement of [3H]7-OH-DPAT from dopamine D3 receptor in rat olfactory tubercle after 60 mins by liquid scintillation counting analysis
Drug: risperidone
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: Htr6
UniProt: P31388 (5HT6R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.4
Action type: ANTAGONIST
Drug: risperidone
Target: Transporter (Transporter)
Gene: NET
UniProt: Q63380 (Q63380_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.55
Assay: Binding affinity to rat NET
Drug: risperidone
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.96
Assay: Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Drug: risperidone
Target: Multidrug and toxin extrusion protein 1 (Transporter)
Gene: SLC47A1
UniProt: Q96FL8 (S47A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.8
Assay: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Drug: risperidone
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 = 6.47
Assay: The binding affinity was measured on serotonin 5-hydroxytryptamine 1 receptor in rat brain tissue
Drug: risperidone
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 = 9.85
Assay: Ability to displace [3H]ketanserin from serotonergic 5-hydroxytryptamine 2 receptor
Drug: risperidone
Target: Serotonin 2 (5-HT2) receptor (GPCR)
Gene: Htr2c|Htr2a|Htr2b
UniProt: P34968|P35363|Q02152 (5HT2C_MOUSE|5HT2A_MOUSE|5HT2B_MOUSE)
Organism: Mus musculus
Activity: IC50 = 8.82
Assay: Inhibitory activity against serotonin 5-hydroxytryptamine 2 receptor from mice.
Drug: risperidone
Target: Histone H1.0 (Nuclear other)
Gene: H1F0
UniProt: P07305 (H10_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.85
Assay: Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
Drug: ritodrine
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.62
Action type: AGONIST
Drug: ritodrine
Target: Beta-3 adrenergic receptor (GPCR)
Gene: ADRB3
UniProt: P13945 (ADRB3_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.72
Drug: ritonavir
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.575
Assay: DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine)
Drug: ritonavir
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.55
Drug: ritonavir
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.83
Drug: ritonavir
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.301
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: ritonavir
Target: Nuclear receptor subfamily 1 group I member 2 (Nuclear hormone receptor)
Gene: NR1I2
UniProt: O75469 (NR1I2_HUMAN)
Organism: Homo sapiens
Drug: ritonavir
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.263
Assay: DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine)
Drug: ritonavir
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.796
Assay: DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: ritonavir
Target: Vasopressin V1a receptor (GPCR)
Gene: AVPR1A
UniProt: P37288 (V1AR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.303
Assay: DRUGMATRIX: Vasopressin V1A radioligand binding (ligand: [125I] PhenylacetylTyr(Me)PheGlnAsnArgProArgTyr)
Drug: ritonavir
Target: Gag-Pol polyprotein (Polyprotein)
Gene: gag-pol
UniProt: P03367 (POL_HV1BR)
Organism: Human immunodeficiency virus type 1 group M subtype B (isolate BRU/LAI)
Activity: Ki = 9.23
Drug: ritonavir
Target: Thromboxane-A synthase (Enzyme)
Gene: TBXAS1
UniProt: P24557 (THAS_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.119
Assay: DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2)
Drug: ritonavir
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.47
Assay: Inhibition of human OCT1-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Drug: ritonavir
Target: Substance-K receptor (GPCR)
Gene: TACR2
UniProt: P21452 (NK2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.058
Assay: DRUGMATRIX: Tachykinin NK2  radioligand binding (ligand: [3H] SR-48968)
Drug: ritonavir
Target: Cytochrome P450 3A5 (Enzyme)
Gene: CYP3A5
UniProt: P20815 (CP3A5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.92
Action type: INHIBITOR
Drug: ritonavir
Target: Pol polyprotein (Enzyme)
Gene: pol
UniProt: Q72874 (Q72874_9HIV1)
Organism: Human immunodeficiency virus 1
Activity: Ki = 10.82
Action type: INHIBITOR
Assay: Inhibition constant of ritonavir towards HIV protease was determined
Drug: ritonavir
Target: UDP-glucuronosyltransferase 1-1 (Enzyme)
Gene: UGT1A1
UniProt: P22309 (UD11_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.77
Action type: INHIBITOR
Drug: ritonavir
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.61
Assay: Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Drug: ritonavir
Target: Multidrug and toxin extrusion protein 1 (Transporter)
Gene: SLC47A1
UniProt: Q96FL8 (S47A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.1
Assay: Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis
Drug: ritonavir
Target: Multidrug and toxin extrusion protein 2 (Transporter)
Gene: SLC47A2
UniProt: Q86VL8 (S47A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.36
Assay: Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay
Drug: ritonavir
Target: Protease (Enzyme)
Gene: protease
UniProt: Q9YQ12 (Q9YQ12_9HIV1)
Organism: Human immunodeficiency virus 1
Activity: Ki = 10.47
Assay: Inhibition of HIV1 protease
Drug: rivastigmine
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P22303 (ACES_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.43
Action type: INHIBITOR
Assay: Inhibition of human erythrocytes BChE
Drug: rivastigmine
Target: Cholinesterase (Enzyme)
Gene: BCHE
UniProt: P06276 (CHLE_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.52
Action type: INHIBITOR
Assay: Inhibition of human recombinant butyrylcholinesterase
Drug: rivastigmine
Target: Acetylcholinesterase (Enzyme)
Gene: Ache
UniProt: P21836 (ACES_MOUSE)
Organism: Mus musculus
Activity: IC50 = 5.95
Assay: Inhibition of Swiss albino mouse RBC AChE after 30 mins by Ellman method
Drug: rivastigmine
Target: Butyrylcholinesterase; Protein Bche (Enzyme)
Gene: Bche
UniProt: Q9JKC1 (Q9JKC1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.46
Assay: In vitro inhibitory concentration against butyrylcholinesterase was determined using rat serum homogenate
Drug: rivastigmine
Target: Acetylcholinesterase (Enzyme)
Gene: Ache
UniProt: P37136 (ACES_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.74
Assay: In vitro inhibitory concentration against rat cortex acetylcholinesterase
Drug: rivastigmine
Target: Acetylcholinesterase (Enzyme)
Gene: ache
UniProt: O42275 (ACES_ELEEL)
Organism: Electrophorus electricus
Activity: IC50 = 5.38
Assay: Inhibition of electric eel AChE preincubated for 5 mins by Ellman's method
Drug: rivastigmine
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P23795 (ACES_BOVIN)
Organism: Bos taurus
Activity: IC50 = 6.21
Assay: Inhibition of bovine AChE after 120 mins by Ellman's method
Drug: rivastigmine
Target: Cholinesterase (Enzyme)
Gene: Bche
UniProt: Q03311 (CHLE_MOUSE)
Organism: Mus musculus
Activity: IC50 = 5.8
Assay: Inhibition of mouse serum BChE
Drug: rivastigmine
Target: Butyrylcholinesterase (Enzyme)
Gene: BCHE
UniProt: Q9N1N9 (Q9N1N9_HORSE)
Organism: Equus caballus
Activity: IC50 = 6.8
Assay: Inhibition of equine BuChE after 120 mins by Ellman's method
Drug: rivastigmine
Target: Cholinesterase (Enzyme)
Gene: BCHE
UniProt: P81908 (CHLE_HORSE)
Organism: Equus caballus
Activity: IC50 = 6.08
Assay: Inhibition of horse serum BChE preincubated for 5 mins by Ellman's method
Drug: rizatriptan
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.85
Assay: In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1A receptor
Drug: rizatriptan
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.1
Assay: Binding activity against 5-hydroxytryptamine 2C receptor from human brain cortex using [3H]mesulergine as radioligand.
Drug: rizatriptan
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.1
Assay: Binding activity against 5-hydroxytryptamine 2C receptor from pig cortex membrane using [3H]mesulergine as radioligand.
Drug: rizatriptan
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.9
Action type: AGONIST
Drug: rizatriptan
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.9
Action type: AGONIST
Drug: rizatriptan
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.854
Drug: rizatriptan
Target: 5-hydroxytryptamine receptor 1F (GPCR)
Gene: HTR1F
UniProt: P30939 (5HT1F_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.8
Action type: AGONIST
Drug: rizatriptan
Target: 5-hydroxytryptamine receptor 1E (GPCR)
Gene: HTR1E
UniProt: P28566 (5HT1E_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.8
Action type: AGONIST
Drug: rizatriptan
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: Htr2a
UniProt: P14842 (5HT2A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.2
Assay: Binding activity against 5-hydroxytryptamine 2C receptor from pig cortex membrane using [3H]mesulergine as radioligand.
Drug: rizatriptan
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P79400 (5HT1D_PIG)
Organism: Sus scrofa
Activity: IC50 = 7.3
Assay: Binding activity against 5-hydroxytryptamine 2C receptor from human brain cortex using [3H]mesulergine as radioligand.
Drug: rizatriptan
Target: Serotonin 3 (5-HT3) receptor (Ion channel)
Gene: Htr3a|Htr3b
UniProt: P35563|Q9JJ16 (5HT3A_RAT|5HT3B_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.4
Assay: Binding activity radioligand.
Drug: rocuronium
Target: Acetylcholine receptor (Ion channel)
Gene: CHRNA1|CHRNB1|CHRND
UniProt: P02708|P11230|Q07001 (ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.77
Action type: ANTAGONIST
Drug: rocuronium
Target: Acetylcholine receptor; alpha1/beta1/delta/gamma (Ion channel)
Gene: CHRNA1|CHRNG|CHRNB1|CHRND
UniProt: P02708|P07510|P11230|Q07001 (ACHA_HUMAN|ACHG_HUMAN|ACHB_HUMAN|ACHD_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.09
Assay: GRAC: human AChR-alpha1 commonly used antagonist
Drug: rofecoxib
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.51
Action type: INHIBITOR
Drug: rofecoxib
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.77
Assay: In vitro potency against human Prostaglandin G/H synthase 1 in U937 microsomes.
Drug: rofecoxib
Target: Prostaglandin E2 receptor EP2 subtype (GPCR)
Gene: PTGER2
UniProt: P43116 (PE2R2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.466
Drug: rofecoxib
Target: Cytochrome c oxidase subunit 2 (Enzyme)
Gene: MT-CO2
UniProt: P00403 (COX2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.52
Assay: Inhibition of human COX2 assessed as reduction in PGF2alpha production by ELISA
Drug: rofecoxib
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: Ptgs2
UniProt: Q05769 (PGH2_MOUSE)
Organism: Mus musculus
Activity: IC50 = 7.92
Assay: In vitro inhibitory activity against Prostaglandin G/H synthase 2 in murine J774 cells
Drug: rofecoxib
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P05979 (PGH1_SHEEP)
Organism: Ovis aries
Activity: IC50 = 4.63
Assay: Inhibition of sheep COX1 by spectrophotometry
Drug: rofecoxib
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: O62698 (PGH2_BOVIN)
Organism: Bos taurus
Activity: IC50 = 6.37
Assay: In vitro inhibitory activity against prostaglandin G/H synthase 2 (COX-2)
Drug: rofecoxib
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: Ptgs2
UniProt: P35355 (PGH2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.12
Assay: In vitro inhibitory concentration against rat Prostaglandin G/H synthase 2
Drug: rofecoxib
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: Ptgs1
UniProt: Q63921 (PGH1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.94
Assay: In vitro inhibitory concentration against rat prostaglandin G/H synthase 1
Drug: rofecoxib
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P79208 (PGH2_SHEEP)
Organism: Ovis aries
Activity: IC50 = 6.52
Assay: Inhibition of ovine COX2
Drug: rolitetracycline
Target: Insulin-degrading enzyme (Enzyme)
Gene: IDE
UniProt: P14735 (IDE_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4
Assay: Inhibition of human recombinant IDE expressed in Escherichia coli BL21 (DE3) cells using ATTO 655- Cys-Lys-Leu-Val-Phe-Phe-Ala-Glu-Asp-Trp as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by spectrophotometric analysis
Drug: rolitetracycline
Target: Integrase (Enzyme)
UniProt: Q76353 (Q76353_9HIV1)
Organism: Human immunodeficiency virus 1
Activity: IC50 = 4.55
Assay: Inhibition of HIV1 recombinant integrase 3'-processing activity
Drug: rolitetracycline
Target: DNA repair protein RAD52 homolog (Nuclear other)
Gene: RAD52
UniProt: P43351 (RAD52_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.54
Assay: Inhibition of RAD52 (unknown origin) assessed as reduction in RAD52-ssDNA interaction using Cy3-dT30-Cy5 ssDNA by FRET assay
Drug: ropinirole
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.49
Drug: ropinirole
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.14
Action type: AGONIST
Drug: ropinirole
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.73
Drug: ropinirole
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.54
Drug: ropinirole
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.85
Assay: Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
Drug: ropinirole
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.42
Drug: ropinirole
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.82
Drug: ropinirole
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.12
Drug: ropinirole
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.43
Action type: AGONIST
Drug: ropinirole
Target: D(1B) dopamine receptor (GPCR)
Gene: DRD5
UniProt: P21918 (DRD5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.38
Drug: ropinirole
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.86
Drug: ropinirole
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.92
Drug: ropinirole
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.07
Action type: AGONIST
Drug: ropinirole
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.57
Assay: Displacement of [3H]spiperone from rat D2 receptor expressed in HEK293 cells
Drug: ropinirole
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P20288 (DRD2_BOVIN)
Organism: Bos taurus
Activity: IC50 = 5.17
Assay: Displacement of [3H]spiroperidol from homogenized bovine pituitary Dopamine receptor D2
Drug: ropinirole
Target: D(3) dopamine receptor (GPCR)
Gene: Drd3
UniProt: P19020 (DRD3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.53
Assay: Displacement of [3H]spiperone from rat D3 receptor expressed in HEK293 cells
Drug: ropivacaine
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.56
Action type: BLOCKER
Drug: ropivacaine
Target: Sodium channel protein type 1 subunit alpha (Ion channel)
Gene: SCN1A
UniProt: P35498 (SCN1A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: ropivacaine
Target: Sodium channel protein type 2 subunit alpha (Ion channel)
Gene: SCN2A
UniProt: Q99250 (SCN2A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: ropivacaine
Target: Sodium channel protein type 3 subunit alpha (Ion channel)
Gene: SCN3A
UniProt: Q9NY46 (SCN3A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: ropivacaine
Target: Sodium channel protein type 4 subunit alpha (Ion channel)
Gene: SCN4A
UniProt: P35499 (SCN4A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: ropivacaine
Target: Sodium channel protein type 8 subunit alpha (Ion channel)
Gene: SCN8A
UniProt: Q9UQD0 (SCN8A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: ropivacaine
Target: Sodium channel protein type 9 subunit alpha (Ion channel)
Gene: SCN9A
UniProt: Q15858 (SCN9A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: ropivacaine
Target: Sodium channel protein type 10 subunit alpha (Ion channel)
Gene: SCN10A
UniProt: Q9Y5Y9 (SCNAA_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: ropivacaine
Target: Potassium channel subfamily K member 3 (Ion channel)
Gene: KCNK3
UniProt: O14649 (KCNK3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.28
Assay: Inhibition of human TASK1 expressed in Xenopus oocytes by whole cell voltage clamp assay
Drug: rosiglitazone
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.53
Assay: Inhibition of human ERG expressed in CHO cells by patch clamp assay
Drug: rosiglitazone
Target: Carbonic anhydrase 2 (Enzyme)
Gene: CA2
UniProt: P00918 (CAH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.391
Assay: DRUGMATRIX: Carbonic Anhydrase II enzyme inhibition (substrate: 4-Nitrophenyl acetate (4-NPA))
Drug: rosiglitazone
Target: Bile salt export pump (Transporter)
Gene: ABCB11
UniProt: O95342 (ABCBB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.19
Drug: rosiglitazone
Target: Amine oxidase [flavin-containing] B (Enzyme)
Gene: MAOB
UniProt: P27338 (AOFB_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.38
Assay: Competitive inhibition of human MAOB expressed in Pichia pastoris
Drug: rosiglitazone
Target: Amine oxidase [flavin-containing] A (Enzyme)
Gene: MAOA
UniProt: P21397 (AOFA_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.56
Assay: Competitive inhibition of human MAOA expressed in Pichia pastoris
Drug: rosiglitazone
Target: Peroxisome proliferator-activated receptor alpha (Nuclear hormone receptor)
Gene: PPARA
UniProt: Q07869 (PPARA_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.41
Assay: Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay
Drug: rosiglitazone
Target: Peroxisome proliferator-activated receptor gamma (Nuclear hormone receptor)
Gene: PPARG
UniProt: P37231 (PPARG_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.04
Action type: AGONIST
Drug: rosiglitazone
Target: Retinoic acid receptor RXR-alpha (Nuclear hormone receptor)
Gene: RXRA
UniProt: P19793 (RXRA_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.82
Assay: Binding affinity to RXRalpha-LBD (unknown origin) measured up to 120 sec by surface plasma resonance method
Drug: rosiglitazone
Target: Retinoic acid receptor gamma (Nuclear hormone receptor)
Gene: RARG
UniProt: P13631 (RARG_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5
Assay: Binding affinity against Retinoic acid receptor gamma was determined in vitro by using [3H]ATRA as radioligand
Drug: rosiglitazone
Target: Thromboxane-A synthase (Enzyme)
Gene: TBXAS1
UniProt: P24557 (THAS_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.449
Assay: DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2)
Drug: rosiglitazone
Target: Peroxisome proliferator-activated receptor delta (Nuclear hormone receptor)
Gene: PPARD
UniProt: Q03181 (PPARD_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.44
Assay: In vitro transcription activation on human peroxisome proliferator activated receptor-delta (PPAR delta)
Drug: rosiglitazone
Target: Free fatty acid receptor 1 (GPCR)
Gene: FFAR1
UniProt: O14842 (FFAR1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.6
Action type: AGONIST
Drug: rosiglitazone
Target: Amine oxidase [flavin-containing] B (Enzyme)
Gene: Maob
UniProt: P19643 (AOFB_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.24
Assay: Competitive inhibition of rat MAOB expressed in Pichia pastoris
Drug: rosiglitazone
Target: Amine oxidase [flavin-containing] A (Enzyme)
Gene: Maoa
UniProt: P21396 (AOFA_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.49
Assay: Competitive inhibition of rat MAOA expressed in Pichia pastoris
Drug: rosiglitazone
Target: Peroxisome proliferator-activated receptor alpha (Transcription factor)
Gene: Ppara
UniProt: P23204 (PPARA_MOUSE)
Organism: Mus musculus
Activity: IC50 = 7.1
Assay: Activation of mouse liver PPARalpha
Drug: rosiglitazone
Target: Peroxisome proliferator-activated receptor gamma (Transcription factor)
Gene: Pparg
UniProt: P37238 (PPARG_MOUSE)
Organism: Mus musculus
Activity: EC50 = 7.52
Drug: rosiglitazone
Target: Type-1A angiotensin II receptor (GPCR)
Gene: Agtr1
UniProt: P25095 (AGTRA_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.64
Assay: Displacement of [125I]-SI-Ang-2 from AT1 receptor in Rattus norvegicus Sprague-Dawley (rat) liver membranes after 2 hr
Drug: rosiglitazone
Target: Short transient receptor potential channel 5 (Ion channel)
Gene: TRPC5
UniProt: Q9UL62 (TRPC5_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.51
Action type: ACTIVATOR