AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: ribavirin
Target: Adenosine receptor A1 (GPCR)
Gene: ADORA1
UniProt: P30542 (AA1R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.13
Assay: Displacement of [3H]N6-R-phenylisopropyladenosine from human A1A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay
Drug: ribavirin
Target: Adenosine kinase (Kinase)
Gene: ADK
UniProt: P55263 (ADK_HUMAN)
Organism: Homo sapiens
Drug: ribavirin
Target: Ectonucleotide pyrophosphatase/phosphodiesterase family member 1 (Enzyme)
Gene: ENPP1
UniProt: P22413 (ENPP1_HUMAN)
Organism: Homo sapiens
Drug: ribavirin
Target: Cytosolic purine 5'-nucleotidase (Enzyme)
Gene: NT5C2
UniProt: P49902 (5NTC_HUMAN)
Organism: Homo sapiens
Drug: ribavirin
Target: Inosine-5'-monophosphate dehydrogenase 1 (Enzyme)
Gene: IMPDH1
UniProt: P20839 (IMDH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Action type: INHIBITOR
Assay: <i>In vitro</i> inhibition of IMPDH (isoform not specified, human and mouse assayed)
Drug: ribavirin
Target: Inosine-5'-monophosphate dehydrogenase 2 (Enzyme)
Gene: IMPDH2
UniProt: P12268 (IMDH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Action type: INHIBITOR
Assay: <i>In vitro</i> inhibition of IMPDH (isoform not specified, human and mouse assayed)
Drug: ribavirin
Target: DNA topoisomerase 1 (Enzyme)
Gene: TOP1
UniProt: P11387 (TOP1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.18
Assay: Inhibition of human topoisomerase 1 activity assessed as DNA triplex formation and presence of supercoiled DNA by microplate assay
Drug: ribavirin
Target: NS5B protein (Enzyme)
Gene: NS5B
UniProt: Q8JXU8 (Q8JXU8_9HEPC)
Organism: Hepatitis C virus
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL5375; SINGLE PROTEIN
Drug: rifabutin
Target: DNA-directed RNA polymerase subunit beta (Enzyme)
Gene: rpoB
UniProt: P9WGY9 (RPOB_MYCTU)
Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)
Activity: Ki = 8
Drug: rifabutin
Target: Bacterial DNA-directed RNA polymerase (Enzyme)
Gene: rpoA|rpoZ|rpoC|rpoB
UniProt: P0A7Z4|P0A800|P0A8T7|P0A8V2 (RPOA_ECOLI|RPOZ_ECOLI|RPOC_ECOLI|RPOB_ECOLI)
Organism: Escherichia coli (strain K12)
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2364672; PROTEIN COMPLEX
Drug: rifampicin
Target: Nuclear receptor subfamily 1 group I member 2 (Nuclear hormone receptor)
Gene: NR1I2
UniProt: O75469 (NR1I2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.64
Assay: Activation of PXR in human DPX2 cells after 24 hrs by luciferase reporter gene assay
Drug: rifampicin
Target: Enoyl-[acyl-carrier-protein] reductase [NADH] (Enzyme)
Gene: inhA
UniProt: P9WGR1 (INHA_MYCTU)
Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)
Activity: IC50 = 7.52
Drug: rifampicin
Target: Bile salt export pump (Transporter)
Gene: ABCB11
UniProt: O95342 (ABCBB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.95
Drug: rifampicin
Target: Caspase-1 (Enzyme)
Gene: CASP1
UniProt: P29466 (CASP1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.08
Assay: DRUGMATRIX: Protease, Caspase 1 enzyme inhibition (substrate: Ac-YVAD-AMC)
Drug: rifampicin
Target: Solute carrier organic anion transporter family member 1B1 (Transporter)
Gene: SLCO1B1
UniProt: Q9Y6L6 (SO1B1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.96
Action type: INHIBITOR
Assay: Inhibition of atorvastatin transport by OATP1B1.
Drug: rifampicin
Target: Lanosterol 14-alpha demethylase (Enzyme)
Gene: CYP51A1
UniProt: Q16850 (CP51A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.52
Assay: Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay
Drug: rifampicin
Target: DNA-directed RNA polymerase subunit beta (Enzyme)
Gene: rpoB
UniProt: P0A8V2 (RPOB_ECOLI)
Organism: Escherichia coli (strain K12)
Action type: INHIBITOR
Drug: rifampicin
Target: Arachidonate 15-lipoxygenase (Enzyme)
Gene: ALOX15
UniProt: P12530 (LOX15_RABIT)
Organism: Oryctolagus cuniculus
Activity: IC50 = 5.53
Assay: DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid)
Drug: rifampicin
Target: Solute carrier organic anion transporter family member 1A2 (Transporter)
Gene: SLCO1A2
UniProt: P46721 (SO1A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.29
Action type: INHIBITOR
Drug: rifampicin
Target: Solute carrier organic anion transporter family member 1B3 (Transporter)
Gene: SLCO1B3
UniProt: Q9NPD5 (SO1B3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.8
Action type: INHIBITOR
Drug: rifampicin
Target: Bile salt export pump (Transporter)
Gene: Abcb11
UniProt: O70127 (ABCBB_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.46
Drug: rifampicin
Target: Glutathione S-transferase omega-1 (Unclassified)
Gene: GSTO1
UniProt: P78417 (GSTO1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.12
Assay: Inhibition of GSTO1-1 (unknown origin) by enzymatic assay
Drug: rifapentine
Target: Bacterial DNA-directed RNA polymerase (Enzyme)
Gene: rpoA|rpoZ|rpoC|rpoB
UniProt: P0A7Z4|P0A800|P0A8T7|P0A8V2 (RPOA_ECOLI|RPOZ_ECOLI|RPOC_ECOLI|RPOB_ECOLI)
Organism: Escherichia coli (strain K12)
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2364672; PROTEIN COMPLEX
Drug: rifaximin
Target: Nuclear receptor subfamily 1 group I member 2 (Nuclear hormone receptor)
Gene: NR1I2
UniProt: O75469 (NR1I2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.66
Assay: Transactivation of human PXR expressed in HepG2 cells after 18 hrs by luciferase reporter gene assay
Drug: rifaximin
Target: Bacterial DNA-directed RNA polymerase (Enzyme)
Gene: rpoA|rpoZ|rpoC|rpoB
UniProt: P0A7Z4|P0A800|P0A8T7|P0A8V2 (RPOA_ECOLI|RPOZ_ECOLI|RPOC_ECOLI|RPOB_ECOLI)
Organism: Escherichia coli (strain K12)
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2364672; PROTEIN COMPLEX
Drug: rilmenidine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.44
Assay: Displacement of [3H]RX821001 from human alpha2A adrenoceptor expressed in CHO cells after 60 mins by gamma counter
Drug: rilmenidine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.05
Drug: rilmenidine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.37
Assay: Displacement of [3H]RX821001 from human alpha2B adrenoceptor expressed in CHO cells after 60 mins by gamma counter
Drug: rilmenidine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.9
Assay: Displacement of [3H]RX821001 from human alpha2C adrenoceptor expressed in CHO cells after 60 mins by gamma counter
Drug: rilmenidine
Target: Nischarin (Membrane receptor)
Gene: NISCH
UniProt: Q9Y2I1 (NISCH_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.23
Assay: Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR
Drug: rilmenidine
Target: Nischarin (Unclassified)
Gene: Nisch
UniProt: Q4G017 (NISCH_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.95
Assay: Displacement of [3H]paraiodoclonidine from imidazoline I1 receptor in rat PC12 cells after 30 mins by gamma counter
Drug: riluzole
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: riluzole
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.3
Action type: BLOCKER
Assay: Inhibition of currents via human Kv11.1 (hERG) channels expressed in HEK293 cells in whole-cell patch-clamp experiments.
Drug: riluzole
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.765
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: riluzole
Target: Intermediate conductance calcium-activated potassium channel protein 4 (Ion channel)
Gene: KCNN4
UniProt: O15554 (KCNN4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.7
Action type: ACTIVATOR
Drug: riluzole
Target: Glutamate receptor ionotropic, NMDA 3A (Ion channel)
Gene: GRIN3A
UniProt: Q8TCU5 (NMD3A_HUMAN)
Organism: Homo sapiens
Drug: riluzole
Target: Small conductance calcium-activated potassium channel protein 3 (Ion channel)
Gene: KCNN3
UniProt: Q9UGI6 (KCNN3_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.9
Action type: ACTIVATOR
Drug: riluzole
Target: Pteridine reductase 1 (Enzyme)
Gene: PTR1
UniProt: Q01782 (PTR1_LEIMA)
Organism: Leishmania major
Activity: Ki = 5.4
Assay: Inhibition of Leishmania major PTR1 by Lineweaver-Burk analysis
Drug: riluzole
Target: Small conductance calcium-activated potassium channel protein 1 (Ion channel)
Gene: KCNN1
UniProt: Q92952 (KCNN1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.68
Action type: ACTIVATOR
Drug: riluzole
Target: Short transient receptor potential channel 5 (Ion channel)
Gene: TRPC5
UniProt: Q9UL62 (TRPC5_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.04
Action type: ACTIVATOR
Drug: riluzole
Target: Small conductance calcium-activated potassium channel protein 2 (Ion channel)
Gene: Kcnn2
UniProt: P70604 (KCNN2_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 4.89
Action type: ACTIVATOR
Drug: rimantadine
Target: Matrix protein 2 (Ion channel)
Gene: M
UniProt: P21430 (M2_I60A0)
Organism: Influenza A virus (strain A/Ann Arbor/6/1960 H2N2)
Drug: rimantadine
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.36
Assay: Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Drug: rimantadine
Target: Multidrug and toxin extrusion protein 1 (Transporter)
Gene: SLC47A1
UniProt: Q96FL8 (S47A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.14
Assay: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Drug: rimantadine
Target: Matrix protein 2 (Ion channel)
Gene: M
UniProt: P63231 (M2_I72A2)
Organism: Influenza A virus (strain A/Udorn/307/1972 H3N2)
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2052; SINGLE PROTEIN
Drug: rimantadine
Target: Polymerase acidic protein (Enzyme)
Gene: PA
UniProt: P03433 (PA_I34A1)
Organism: Influenza A virus (strain A/Puerto Rico/8/1934 H1N1)
Activity: IC50 = 4.96
Assay: Inhibition of Influenza A virus (A/Puerto Rico/8/34(H1N1)) PA endonuclease infected in MDCK cells assessed as reduction in virus titer treated with cells for 1 hr prior to viral infection for 1 hr followed by compound washout and subsequent compound addition measured after 48 hrs by hemagglutination test
Drug: rimantadine
Target: Polymerase acidic protein (Unclassified)
Gene: PA
UniProt: P03433 (PA_I34A1)
Organism: Influenza A virus (strain A/Puerto Rico/8/1934 H1N1)
Activity: IC50 = 4.96
Assay: Inhibition of Influenza A virus (A/Puerto Rico/8/34(H1N1)) PA endonuclease infected in MDCK cells assessed as reduction in virus titer treated with cells for 1 hr prior to viral infection for 1 hr followed by compound washout and subsequent compound addition measured after 48 hrs by hemagglutination test
Drug: rimantadine
Target: Matrix protein 2 (Unclassified)
Gene: M
UniProt: P05778 (M2_I000F)
Organism: Influenza A virus
Activity: Kd = 7.8
Assay: Binding affinity to Influenza A Weybridge(H7N7) virus Matrix protein 2 by spectrophotometry
Drug: rimantadine
Target: Matrix protein 2 (Unclassified)
Gene: M
UniProt: P0DOF8 (M2_I72A8)
Organism: Influenza A virus
Activity: Kd = 6.29
Assay: Binding affinity to Influenza A virus A/Udorn/72 wild-type M2 proton channel by isothermal calorimetric titration
Drug: rimexolone
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: ripazepam
Target: GABA-A receptor; anion channel (Ion channel)
Gene: Gabrp|Gabrb1|Gabrd|Gabrg2|Gabra5|Gabra3|Gabrg1|Gabra2|Gabra4|Gabrg3|Gabra6|Gabra1|Gabrb3|Gabrb2|Gabrq|Gabre
UniProt: O09028|P15431|P18506|P18508|P19969|P20236|P23574|P23576|P28471|P28473|P30191|P62813|P63079|P63138|Q91ZM7|Q9ES14 (GBRP_RAT|GBRB1_RAT|GBRD_RAT|GBRG2_RAT|GBRA5_RAT|GBRA3_RAT|GBRG1_RAT|GBRA2_RAT|GBRA4_RAT|GBRG3_RAT|GBRA6_RAT|GBRA1_RAT|GBRB3_RAT|GBRB2_RAT|Q91ZM7_RAT|GBRE_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.17
Assay: Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor in synaptic membranes of rat cerebral cortex
Drug: risedronic acid
Target: Farnesyl pyrophosphate synthase (Enzyme)
Gene: FDPS
UniProt: P14324 (FPPS_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.44
Action type: INHIBITOR
Assay: Inhibition of human recombinant FPPS expressed in Escherichia coli BL21 after 10 mins
Drug: risedronic acid
Target: Farnesyl pyrophosphate synthase (Enzyme)
UniProt: Q0GKD7 (Q0GKD7_LEIDO)
Organism: Leishmania donovani
Activity: Ki = 7.77
Assay: Binding affinity towards Farnesyl diphosphate synthase from leishmania major
Drug: risedronic acid
Target: Farnesyl diphosphate synthase (Enzyme)
Gene: FPPS
UniProt: Q197X6 (Q197X6_TOXGO)
Organism: Toxoplasma gondii
Activity: IC50 = 7.13
Assay: Inhibition of Toxoplasma gondii FPPS after 30 mins using [14C]IPP by scintillation counting
Drug: risedronic acid
Target: Farnesyl diphosphate synthase (Enzyme)
UniProt: Q8WS26 (Q8WS26_TRYCR)
Organism: Trypanosoma cruzi
Activity: IC50 = 7.57
Assay: Inhibition of Trypanosoma cruzi FPPS after 30 mins using [14C]IPP by scintillation counting
Drug: levisoprenaline
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.1
Assay: Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
Drug: levisoprenaline
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 10.3
Assay: Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
Drug: levisoprenaline
Target: Beta-3 adrenergic receptor (GPCR)
Gene: ADRB3
UniProt: P13945 (ADRB3_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.4
Assay: Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
Drug: levisoprenaline
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P04274 (ADRB2_MESAU)
Organism: Mesocricetus auratus
Activity: Ki = 6.87
Assay: Displacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells
Drug: levisoprenaline
Target: Beta-1 adrenergic receptor (GPCR)
Gene: Adrb1
UniProt: P34971 (ADRB1_MOUSE)
Organism: Mus musculus
Activity: Ki = 6.66
Assay: Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay
Drug: risperidone
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.301
Drug: risperidone
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.301
Drug: risperidone
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.68
Assay: Binding affinity against dopamine receptor D1
Drug: risperidone
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.49
Action type: ANTAGONIST
Drug: risperidone
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8
Drug: risperidone
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.37
Assay: Binding affinity measured at the sigma receptor by the inhibition of [3H]-3-PPP binding to guinea pig cerebellum using unlabeled 3-PPP for nonspecific binding.
Drug: risperidone
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.788
Drug: risperidone
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.85
Assay: Binding affinity to human SERT
Drug: risperidone
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.443
Drug: risperidone
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.364
Action type: ANTAGONIST
Drug: risperidone
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.42
Drug: risperidone
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.7
Action type: ANTAGONIST
Drug: risperidone
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.65
Assay: Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug: risperidone
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.47
Drug: risperidone
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.553
Drug: risperidone
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.77
Drug: risperidone
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.07
Action type: ANTAGONIST
Drug: risperidone
Target: D(1B) dopamine receptor (GPCR)
Gene: DRD5
UniProt: P21918 (DRD5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.023
Drug: risperidone
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.481
Drug: risperidone
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.921
Drug: risperidone
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.55
Assay: Binding affinity to human cloned muscarinic M1 receptor
Drug: risperidone
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.432
Drug: risperidone
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5
Drug: risperidone
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.538
Drug: risperidone
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.49
Action type: ANTAGONIST
Drug: risperidone
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.6
Action type: ANTAGONIST
Drug: risperidone
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.495
Drug: risperidone
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.278
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: risperidone
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8
Action type: ANTAGONIST
Drug: risperidone
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.4
Action type: ANTAGONIST
Drug: risperidone
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.48
Drug: risperidone
Target: Glycine receptor subunit alpha-1 (Ion channel)
Gene: GLRA1
UniProt: P23415 (GLRA1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.49
Drug: risperidone
Target: 5-hydroxytryptamine receptor 5A (GPCR)
Gene: HTR5A
UniProt: P47898 (5HT5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.687
Drug: risperidone
Target: 5-hydroxytryptamine receptor 1F (GPCR)
Gene: HTR1F
UniProt: P30939 (5HT1F_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.9
Action type: ANTAGONIST
Drug: risperidone
Target: 5-hydroxytryptamine receptor 1E (GPCR)
Gene: HTR1E
UniProt: P28566 (5HT1E_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.9
Action type: ANTAGONIST
Drug: risperidone
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.967
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: risperidone
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.89
Assay: Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
Drug: risperidone
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P31389 (HRH1_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 7.66
Assay: Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
Drug: risperidone
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.74
Assay: Ability to displace [3H]spiperone from D2 dopamine receptor isolated from the striata of male Wistar rats
Drug: risperidone
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.89
Assay: Ability to displace [3H]-8-OH-DPAT from serotonergic 5-hydroxytryptamine 1A receptor
Drug: risperidone
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: Htr2a
UniProt: P14842 (5HT2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.82
Assay: Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat cortex by scintillation spectrometry
Drug: risperidone
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32305 (5HT7R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.85
Assay: Binding affinity towards rat 5-hydroxytryptamine 7 receptor
Drug: risperidone
Target: Beta-1 adrenergic receptor (GPCR)
Gene: Adrb1
UniProt: P18090 (ADRB1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.66
Assay: Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
Drug: risperidone
Target: D(1A) dopamine receptor (GPCR)
Gene: Drd1
UniProt: P18901 (DRD1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.66
Assay: Affinity for Dopamine receptor D1
Drug: risperidone
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: Adra2a
UniProt: P22909 (ADA2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.6
Assay: Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
Drug: risperidone
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61168 (DRD2_MOUSE)
Organism: Mus musculus
Activity: IC50 = 7.64
Assay: Inhibition of mouse Dopamine receptor D2