AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: glutamic acid
Target: Metabotropic glutamate receptor 8 (GPCR)
Gene: Grm8
UniProt: P70579 (GRM8_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.47
Drug: glutamic acid
Target: Metabotropic glutamate receptor 8 (GPCR)
Gene: Grm8
UniProt: P47743 (GRM8_MOUSE)
Organism: Mus musculus
Activity: EC50 = 7.66
Drug: glutamic acid
Target: Metabotropic glutamate receptor 5 (GPCR)
Gene: Grm5
UniProt: P31424 (GRM5_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 5.36
Drug: glutamic acid
Target: Metabotropic glutamate receptor 1 (GPCR)
Gene: Grm1
UniProt: P23385 (GRM1_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 5
Drug: glutamic acid
Target: Metabotropic glutamate receptor 2 (GPCR)
Gene: Grm2
UniProt: P31421 (GRM2_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 5.4
Drug: glutamic acid
Target: Metabotropic glutamate receptor 3 (GPCR)
Gene: Grm3
UniProt: P31422 (GRM3_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 5.52
Drug: glutamic acid
Target: Glutamate racemase (Enzyme)
Gene: murI
UniProt: P56068 (MURI_HELPY)
Organism: Helicobacter pylori (strain ATCC 700392 / 26695)
Activity: Ki = 5.24
Assay: Inhibition of Helicobacter pylori glutamate racemase
Drug: glutamic acid
Target: Excitatory amino acid transporter 4 (Transporter)
Gene: Slc1a6
UniProt: O35921 (EAA4_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.89
Assay: Inhibition of rat EAAT4 expressed in tsA201 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method
Drug: glutamine
Target: Amino acid transporter (Transporter)
Gene: Slc1a5
UniProt: Q9Z1J7 (Q9Z1J7_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.57
Assay: Inhibition of ASCT2 in rat hippocampal astrocytes at high affinity component 1 assessed as reduction in [3H]-D-serine uptake after 5 mins by beta counting analysis
Drug: glutathione
Target: Glutathione S-transferase kappa 1 (Enzyme)
Gene: GSTK1
UniProt: Q9Y2Q3 (GSTK1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.7
Assay: Affinity towards recombinant Glutathione S-transferase (GST) Enzyme.
Drug: glutethimide
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
Action type: POSITIVE MODULATOR
Drug: glibenclamide
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.13
Assay: Inhibition of human ERG potassium channel
Drug: glibenclamide
Target: Bile salt export pump (Transporter)
Gene: ABCB11
UniProt: O95342 (ABCBB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.28
Drug: glibenclamide
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.795
Action type: INHIBITOR
Assay: DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: glibenclamide
Target: Peroxisome proliferator-activated receptor gamma (Nuclear hormone receptor)
Gene: PPARG
UniProt: P37231 (PPARG_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.18
Assay: Binding affinity to PPARgamma (unknown origin) by TR-FRET assay
Drug: glibenclamide
Target: Cystic fibrosis transmembrane conductance regulator (Ion channel)
Gene: CFTR
UniProt: P13569 (CFTR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.66
Action type: BLOCKER
Drug: glibenclamide
Target: Sulfonylurea receptor 2, Kir6.2 (Ion channel)
Gene: ABCC9|KCNJ11
UniProt: O60706|Q14654 (ABCC9_HUMAN|KCJ11_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.21
Action type: BLOCKER
Drug: glibenclamide
Target: Bile salt export pump (Transporter)
Gene: Abcb11
UniProt: O70127 (ABCBB_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.55
Drug: glibenclamide
Target: ATP-sensitive inward rectifier potassium channel 11 (Ion channel)
Gene: Kcnj11
UniProt: Q61743 (KCJ11_MOUSE)
Organism: Mus musculus
Activity: IC50 = 5.7
Action type: BLOCKER
Drug: glibenclamide
Target: NACHT, LRR and PYD domains-containing protein 3 (Unclassified)
Gene: NLRP3
UniProt: Q96P20 (NLRP3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.92
Assay: Inhibition of NLRP3 in LPS activated human monocytes after 30 mins by ELISA analysis in presence of ATP
Drug: glibenclamide
Target: CDGSH iron-sulfur domain-containing protein 1 (Unclassified)
Gene: CISD1
UniProt: Q9NZ45 (CISD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.78
Assay: Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis
Drug: glibenclamide
Target: Peroxisome proliferator-activated receptor gamma (Nuclear other)
Gene: PPARG
UniProt: P37231 (PPARG_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.18
Assay: Binding affinity to PPARgamma (unknown origin) by TR-FRET assay
Drug: glibenclamide
Target: Sur1-Trpm4; Sulfonylurea receptor 1 - Transient receptor potential melastatin 4 (Ion channel)
Gene: Abcc8|Trpm4
UniProt: Q09429|Q9ESQ5 (ABCC8_RAT|TRPM4_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 7.32
Action type: INHIBITOR
Assay: activity measured in native reactive (type R1) rat astrocytes
Drug: glibenclamide
Target: Sulfonylurea receptor 1, Kir6.2 (Ion channel)
Gene: ABCC8|KCNJ11
UniProt: Q09428|Q14654 (ABCC8_HUMAN|KCJ11_HUMAN)
Organism: Homo sapiens
Activity: Kd = 9.523
Action type: BLOCKER
Assay: [86]Rb+ efflux in RINm5F insulinoma cells
Drug: glycine
Target: Glutamate receptor ionotropic, NMDA 1 (Ion channel)
Gene: Grin1
UniProt: P35439 (NMDZ1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.6
Assay: In vitro inhibitory activity to inhibit [3H]glycine binding to NMDA receptor
Drug: glycine
Target: Sodium- and chloride-dependent glycine transporter 1 (Transporter)
Gene: SLC6A9
UniProt: P48067 (SC6A9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.5
Assay: Inhibition of GlyT1 (unknown origin) assessed as inhibition of [14C]glycine uptake
Drug: glycine
Target: Glutamate NMDA receptor (Ion channel)
Gene: Grin1|Grin2a|Grin2b|Grin2c|Grin2d|Grin3b|Grin3a
UniProt: P35439|Q00959|Q00960|Q00961|Q62645|Q8VHN2|Q9R1M7 (NMDZ1_RAT|NMDE1_RAT|NMDE2_RAT|NMDE3_RAT|NMDE4_RAT|NMD3B_RAT|NMD3A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.77
Assay: Affinity for the glycine binding site of NMDA receptor by inhibition of [3H]5,7-dichlorokynurenic acid ([3H]DCKA) binding to rat brain synaptic membrane
Drug: glycine
Target: Olfactory receptor 51E2 (GPCR)
Gene: OR51E2
UniProt: Q9H255 (O51E2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.24
Assay: Agonist activity at PSGR/OR51E2 (unknown origin) expressed in human Hana3A cells co-transfected with CRE-Luc by luciferase reporter gene assay
Drug: glycyrrhizic acid
Target: Corticosteroid 11-beta-dehydrogenase isozyme 2 (Enzyme)
Gene: HSD11B2
UniProt: P80365 (DHI2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.4
Assay: Inhibition of human 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay
Drug: glycyrrhizic acid
Target: Corticosteroid 11-beta-dehydrogenase isozyme 1 (Enzyme)
Gene: HSD11B1
UniProt: P28845 (DHI1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.22
Assay: Inhibition of human 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay
Drug: glycyrrhizic acid
Target: Corticosteroid 11-beta-dehydrogenase isozyme 1 (Enzyme)
Gene: Hsd11b1
UniProt: P50172 (DHI1_MOUSE)
Organism: Mus musculus
Activity: IC50 = 8.52
Assay: Inhibition of mouse 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay
Drug: glycyrrhizic acid
Target: High mobility group protein B1 (Nuclear other)
Gene: HMGB1
UniProt: P09429 (HMGB1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.06
Assay: Binding affinity to recombinant HMGB1 B box region (90 to 175 residues) (unknown origin) expressed Escherichia coli after 5 mins by fluorescence-based assay
Drug: goserelin
Target: Lutropin-choriogonadotropic hormone receptor (GPCR)
Gene: LHCGR
UniProt: P22888 (LSHR_HUMAN)
Organism: Homo sapiens
Drug: goserelin
Target: Gonadotropin-releasing hormone receptor (GPCR)
Gene: GNRHR
UniProt: P30968 (GNRHR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action; CHEMBL1855; SINGLE PROTEIN
Drug: gossypol
Target: Estrogen receptor (Nuclear hormone receptor)
Gene: ESR1
UniProt: P03372 (ESR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.59
Assay: PUBCHEM_BIOASSAY: Estrogen Receptor-alpha Coactivator Binding Inhibitors Dose Response Confirmation. (Class of assay: confirmatory) [Related pubchem assays: 629 (Primary screen preceding this dose response confirmation assay.)]
Drug: gossypol
Target: Beta-lactamase (Enzyme)
Gene: ampC
UniProt: P00811 (AMPC_ECOLI)
Organism: Escherichia coli (strain K12)
Activity: IC50 = 4.34
Assay: Inhibition of Escherichia coli AmpC beta lactamase using relaxed assay conditions in presence of 0.00001% Triton X-100 detergent
Drug: gossypol
Target: Aldose reductase (Enzyme)
Gene: AKR1B1
UniProt: P15121 (ALDR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.3
Assay: The compound was tested for inhibitory activity against Aldose reductase from human placenta
Drug: gossypol
Target: Apoptosis regulator Bcl-2 (Cytosolic other)
Gene: BCL2
UniProt: P10415 (BCL2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.77
Assay: Displacement of FAM-Bim peptide from human Bcl2 by fluorescence polarization assay
Drug: gossypol
Target: Induced myeloid leukemia cell differentiation protein Mcl-1 (Cytosolic other)
Gene: MCL1
UniProt: Q07820 (MCL1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.74
Assay: Displacement of FAM-Bid from human Mcl1 by FP assay
Drug: gossypol
Target: Bcl-2-like protein 1 (Cytosolic other)
Gene: BCL2L1
UniProt: Q07817 (B2CL1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.32
Assay: Displacement of FAM-Bak from human Bcl-xL by FP assay
Drug: gossypol
Target: Malate dehydrogenase, mitochondrial (Enzyme)
Gene: MDH2
UniProt: P00346 (MDHM_PIG)
Organism: Sus scrofa
Activity: IC50 = 5.55
Assay: Inhibition of pig heart mitochondrial MDH
Drug: gossypol
Target: Lactate dehydrogenase (Enzyme)
Gene: LDH
UniProt: Q0PJ46 (Q0PJ46_PLAFA)
Organism: Plasmodium falciparum
Activity: IC50 = 5.58
Assay: Inhibition of Plasmodium falciparum LDH
Drug: gossypol
Target: Malate dehydrogenase (Enzyme)
UniProt: Q6VVP7 (Q6VVP7_PLAFA)
Organism: Plasmodium falciparum
Activity: IC50 = 5.69
Assay: Inhibition of Plasmodium falciparum MDH
Drug: gossypol
Target: Malate dehydrogenase, cytoplasmic (Enzyme)
Gene: MDH1
UniProt: P11708 (MDHC_PIG)
Organism: Sus scrofa
Activity: IC50 = 5.24
Assay: Inhibition of pig cytosolic MDH
Drug: gossypol
Target: L-lactate dehydrogenase A chain (Enzyme)
Gene: LDHA
UniProt: P00338 (LDHA_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.72
Assay: Competitive inhibition of human LDH5 in presence of NADH
Drug: gossypol
Target: Apoptosis regulator Bcl-W (Cytosolic other)
Gene: BCL2L2
UniProt: Q92843 (B2CL2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.75
Assay: Displacement of Flu-Bak peptide from recombinant antiapoptotic Bcl-w protein by fluorescence polarization assay
Drug: gossypol
Target: Kinesin-like protein 1 (Enzyme)
Gene: KIF11
UniProt: P52732 (KIF11_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.97
Assay: Inhibition of human recombinant Eg5 ATPase activity expressed in Escherichia coli after 30 mins by malachite green-based spectrophotometric analysis
Drug: gossypol
Target: Solute carrier family 2, facilitated glucose transporter member 1 (Transporter)
Gene: SLC2A1
UniProt: P11166 (GTR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.7
Assay: Mixed type non-competitive inhibition of glucose displaceable binding of [4-3H]cytochalasin B to GLUT1 in human erythrocyte membranes after 10 mins
Drug: gossypol
Target: DNA-3-methyladenine glycosylase (Enzyme)
Gene: MPG
UniProt: P29372 (3MG_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.52
Drug: gossypol
Target: L-lactate dehydrogenase B chain (Enzyme)
Gene: LDHB
UniProt: P07195 (LDHB_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.85
Assay: Competitive inhibition of human LDH1 in presence of NADH
Drug: granisetron
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.428
Drug: granisetron
Target: 5-hydroxytryptamine receptor 3A (Ion channel)
Gene: HTR3A
UniProt: P46098 (5HT3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.7
Action type: ANTAGONIST
Drug: granisetron
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.37
Assay: Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Drug: granisetron
Target: Multidrug and toxin extrusion protein 1 (Transporter)
Gene: SLC47A1
UniProt: Q96FL8 (S47A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.3
Assay: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Drug: granisetron
Target: Serotonin 3 (5-HT3) receptor (Ion channel)
Gene: Htr3a|Htr3b
UniProt: P35563|Q9JJ16 (5HT3A_RAT|5HT3B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.46
Assay: Ability to displace [3H]granisetron specifically bound to 5-hydroxytryptamine 3 receptor in rat cortical membrane
Drug: granisetron
Target: Neuronal acetylcholine receptor; alpha4/beta2 (Ion channel)
Gene: CHRNB2|CHRNA4
UniProt: P17787|P43681 (ACHB2_HUMAN|ACHA4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.42
Assay: In vitro Binding affinity towards Nicotinic acetylcholine receptor alpha4-beta2 was determined
Drug: granisetron
Target: 5-hydroxytryptamine receptor 3B (Ion channel)
Gene: HTR3B
UniProt: O95264 (5HT3B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.8
Assay: GRAC: human 5-HT3B selective antagonist
Drug: granisetron
Target: Neuronal acetylcholine receptor subunit alpha-3 (Ion channel)
Gene: CHRNA3
UniProt: P32297 (ACHA3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.17
Assay: In vitro Binding affinity towards alpha-3 (PC12) nAChR was determined
Drug: grepafloxacin
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.3
Assay: Inhibitory activity against Potassium channel HERG
Drug: grepafloxacin
Target: DNA topoisomerase 4 (Enzyme)
Gene: parC|parE
UniProt: P72525|Q59961 (PARC_STRPN|PARE_STRPN)
Organism: Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4)
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2363033; PROTEIN COMPLEX
Drug: grepafloxacin
Target: DNA gyrase (Enzyme)
Gene: gyrB|gyrA
UniProt: P0A4L9|P72524 (GYRB_STRPN|GYRA_STRPN)
Organism: Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4)
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2311225; PROTEIN COMPLEX
Drug: griseofulvin
Target: Tubulin beta chain (Structural)
Gene: TUB2
UniProt: P10875 (TBB_CANAX)
Organism: Candida albicans
Drug: griseofulvin
Target: Lanosterol 14-alpha demethylase (Enzyme)
Gene: CYP51A1
UniProt: Q16850 (CP51A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.3
Assay: Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay
Drug: griseofulvin
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.14
Assay: Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
Drug: griseofulvin
Target: Tubulin (Structural)
UniProt: F2SG63|F2SZ02|F2SZD3 (F2SG63_TRIRC|F2SZ02_TRIRC|F2SZD3_TRIRC)
Organism: Trichophyton rubrum (strain ATCC MYA-4607 / CBS 118892)
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2364703; PROTEIN COMPLEX GROUP
Drug: guaiacol
Target: Carbonic anhydrase 2 (Enzyme)
Gene: CA2
UniProt: P00918 (CAH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.53
Assay: Inhibition of human erythrocyte CA2 esterase activity using 4-nitrophenyl acetate substrate
Drug: guaiacol
Target: Carbonic anhydrase 1 (Enzyme)
Gene: CA1
UniProt: P00915 (CAH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.22
Assay: Inhibition of human erythrocyte CA1 esterase activity using 4-nitrophenyl acetate substrate
Drug: guanadrel
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Action type: SUBSTRATE
Drug: guanadrel
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Drug: guanethidine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Drug: guanethidine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Action type: SUBSTRATE
Drug: guanethidine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Drug: guanethidine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Drug: guanethidine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Drug: guanethidine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Drug: guanethidine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Drug: guanfacine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.065
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: guanfacine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.875
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: guanfacine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.119
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: guanfacine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.926
Action type: AGONIST
Drug: guanfacine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.68
Action type: AGONIST
Drug: guanfacine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.263
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: guanfacine
Target: Nischarin (Membrane receptor)
Gene: NISCH
UniProt: Q9Y2I1 (NISCH_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.72
Assay: Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR
Drug: guanfacine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.87
Drug: guanfacine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.164
Action type: AGONIST
Drug: guanidine
Target: Voltage-gated potassium channel (Ion channel)
Gene: KCNQ3|KCNQ2|KCNH1|KCNA2|KCNA6|KCNA3|KCNA4|KCNA5|KCNC1|KCNQ1|KCNQ4|KCNC4|KCNA1|KCNH2|KCNC3|KCNB1|KCNA10|KCNV1|KCNH5|KCNG3|KCNG4|KCNV2|KCNB2|KCNS1|KCNH8|KCNC2|KCNA7|KCNS3|KCNH6|KCNF1|KCNQ5|KCNH7|KCND1|KCND2|KCNG1|KCNG2|KCND3|KCNH3|KCNS2|KCNH4
UniProt: O43525|O43526|O95259|P16389|P17658|P22001|P22459|P22460|P48547|P51787|P56696|Q03721|Q09470|Q12809|Q14003|Q14721|Q16322|Q6PIU1|Q8NCM2|Q8TAE7|Q8TDN1|Q8TDN2|Q92953|Q96KK3|Q96L42|Q96PR1|Q96RP8|Q9BQ31|Q9H252|Q9H3M0|Q9NR82|Q9NS40|Q9NSA2|Q9NZV8|Q9UIX4|Q9UJ96|Q9UK17|Q9ULD8|Q9ULS6|Q9UQ05 (KCNQ3_HUMAN|KCNQ2_HUMAN|KCNH1_HUMAN|KCNA2_HUMAN|KCNA6_HUMAN|KCNA3_HUMAN|KCNA4_HUMAN|KCNA5_HUMAN|KCNC1_HUMAN|KCNQ1_HUMAN|KCNQ4_HUMAN|KCNC4_HUMAN|KCNA1_HUMAN|KCNH2_HUMAN|KCNC3_HUMAN|KCNB1_HUMAN|KCA10_HUMAN|KCNV1_HUMAN|KCNH5_HUMAN|KCNG3_HUMAN|KCNG4_HUMAN|KCNV2_HUMAN|KCNB2_HUMAN|KCNS1_HUMAN|KCNH8_HUMAN|KCNC2_HUMAN|KCNA7_HUMAN|KCNS3_HUMAN|KCNH6_HUMAN|KCNF1_HUMAN|KCNQ5_HUMAN|KCNH7_HUMAN|KCND1_HUMAN|KCND2_HUMAN|KCNG1_HUMAN|KCNG2_HUMAN|KCND3_HUMAN|KCNH3_HUMAN|KCNS2_HUMAN|KCNH4_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Assay: Mechanism of Action; CHEMBL2362996; PROTEIN FAMILY
Drug: halazepam
Target: GABA-A receptor; anion channel (Ion channel)
Gene: GABRP|GABRD|GABRA1|GABRB1|GABRG2|GABRB3|GABRA5|GABRA3|GABRA2|GABRB2|GABRA4|GABRE|GABRA6|GABRG1|GABRG3|GABRQ
UniProt: O00591|O14764|P14867|P18505|P18507|P28472|P31644|P34903|P47869|P47870|P48169|P78334|Q16445|Q8N1C3|Q99928|Q9UN88 (GBRP_HUMAN|GBRD_HUMAN|GBRA1_HUMAN|GBRB1_HUMAN|GBRG2_HUMAN|GBRB3_HUMAN|GBRA5_HUMAN|GBRA3_HUMAN|GBRA2_HUMAN|GBRB2_HUMAN|GBRA4_HUMAN|GBRE_HUMAN|GBRA6_HUMAN|GBRG1_HUMAN|GBRG3_HUMAN|GBRT_HUMAN)
Organism: Homo sapiens
Action type: POSITIVE ALLOSTERIC MODULATOR
Assay: Mechanism of Action; CHEMBL2093872; PROTEIN COMPLEX GROUP
Drug: ulobetasol propionate
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: halofantrine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.12
Assay: Inhibition of human ERG expressed in CHO cells
Drug: haloperidol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.301
Drug: haloperidol
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.003
Assay: DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine)
Drug: haloperidol
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.82
Drug: haloperidol
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.15
Action type: INVERSE AGONIST
Drug: haloperidol
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.947
Drug: haloperidol
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.92
Drug: haloperidol
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.5
Drug: haloperidol
Target: 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase (Enzyme)
Gene: EBP
UniProt: Q15125 (EBP_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.72
Drug: haloperidol
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.7
Drug: haloperidol
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.74
Assay: Binding affinity to human SERT
Drug: haloperidol
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.74
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: haloperidol
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.55
Assay: Binding affinity for 5-hydroxytryptamine 1A receptor determined using [3H]8-OH-DPAT as radioligand
Drug: haloperidol
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7
Action type: ANTAGONIST
Drug: haloperidol
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.1