AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: methylergometrine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.268
Action type: ANTAGONIST
Assay: DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug: methylergometrine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.559
Assay: DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
Drug: methylergometrine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.225
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: methylergometrine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.633
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
Drug: methylergometrine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.4
Action type: AGONIST
Drug: methylergometrine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.1
Action type: PARTIAL AGONIST
Assay: Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug: methylergometrine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.3
Action type: AGONIST
Drug: methylergometrine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.928
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: methylergometrine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.678
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: methylergometrine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.244
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: methylergometrine
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.699
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: methylergometrine
Target: 5-hydroxytryptamine receptor 1F (GPCR)
Gene: HTR1F
UniProt: P30939 (5HT1F_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.5
Action type: ANTAGONIST
Drug: methylergometrine
Target: 5-hydroxytryptamine receptor 1E (GPCR)
Gene: HTR1E
UniProt: P28566 (5HT1E_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.2
Action type: ANTAGONIST
Drug: methylergometrine
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.033
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug: methylergometrine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.39
Drug: methylergometrine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: Htr2a
UniProt: P14842 (5HT2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.9
Action type: AGONIST
Drug: methylergometrine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: Htr2c
UniProt: P08909 (5HT2C_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.9
Action type: AGONIST
Drug: naltrexone
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.38
Action type: ANTAGONIST
Drug: naltrexone
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: naltrexone
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.93
Action type: ANTAGONIST
Drug: naltrexone
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.99
Action type: ANTAGONIST
Drug: naltrexone
Target: Neuronal acetylcholine receptor subunit alpha-7 (Ion channel)
Gene: CHRNA7
UniProt: P36544 (ACHA7_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.6
Assay: Blockage of Nicotinic acetylcholine receptor alpha-7 noncompetitively in hippocampal primary cultures
Drug: naltrexone
Target: Mu-type opioid receptor (GPCR)
Gene: Oprm1
UniProt: P33535 (OPRM_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.34
Assay: Displacement of [3H]DAMGO from mu opioid receptor in rat brain homogenate after 1 hr by liquid scintillation counting
Drug: naltrexone
Target: Mu-type opioid receptor (GPCR)
Gene: Oprm1
UniProt: P42866 (OPRM_MOUSE)
Organism: Mus musculus
Activity: Ki = 9.58
Assay: Displacement of [3H]DAMGO from mouse mu opioid receptor in whole brain without cerebellum
Drug: naltrexone
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P97266 (OPRM_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 9.77
Assay: Binding affinity towards Opioid receptor mu 1 of guinea pig brain membranes using radioligand 0.25 nM [3H]DAMGO
Drug: naltrexone
Target: Delta-type opioid receptor (GPCR)
Gene: Oprd1
UniProt: P32300 (OPRD_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.91
Assay: Displacement of [3H]DPDPE from mouse delta opioid receptor in whole brain without cerebellum
Drug: naltrexone
Target: Delta-type opioid receptor (GPCR)
Gene: Oprd1
UniProt: P33533 (OPRD_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.32
Assay: In vito concentration required to displace [3H]DADLE (Kd = 12.2 nM and concentration is 2.1 nM) from low affinity delta-site in rat brain membranes.
Drug: naltrexone
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41144 (OPRK_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 9.51
Assay: Binding affinity towards guinea pig Opioid receptor kappa 1 using radioligand [3H]U-69593
Drug: naltrexone
Target: Neuronal acetylcholine receptor subunit alpha-4 (Ion channel)
Gene: Chrna4
UniProt: P09483 (ACHA4_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.51
Assay: Blockage of Nicotinic acetylcholine receptor alpha4-beta2 noncompetitively in acute hippocampal slices
Drug: naltrexone
Target: Kappa-type opioid receptor (GPCR)
Gene: Oprk1
UniProt: P34975 (OPRK_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.97
Assay: Displacement of [3H]U69593 from kappa opioid receptor in rat brain homogenate after 1 hr by liquid scintillation counting
Drug: naltrexone
Target: Kappa-type opioid receptor (GPCR)
Gene: Oprk1
UniProt: P33534 (OPRK_MOUSE)
Organism: Mus musculus
Activity: Ki = 8.84
Assay: Displacement of [3H]-diprenorphine from mouse kappa opioid receptor expressed in CHO cells after 1.5 hrs
Drug: naltrexone
Target: Opioid receptor (GPCR)
Gene: Oprd1|Oprm1|Oprk1|Sigmar1
UniProt: P33533|P33535|P34975|Q9R0C9 (OPRD_RAT|OPRM_RAT|OPRK_RAT|SGMR1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.26
Assay: Inhibition of [3H]diprenorphine binding to rat brain membrane opioid receptors;(T= total opioid receptor family)
Drug: naltrexone
Target: Opioid receptors; mu and delta (GPCR)
Gene: Oprd1|Oprm1
UniProt: P32300|P42866 (OPRD_MOUSE|OPRM_MOUSE)
Organism: Mus musculus
Activity: Ki = 9.06
Assay: Displacement of [3H]-DAMGO from mouse MOR/DOR expressed in HEK293 cells
Drug: methylparaben
Target: Carbonic anhydrase 2 (Enzyme)
Gene: CA2
UniProt: P00918 (CAH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.47
Assay: Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by CO2 hydration stopped-flow assay
Drug: methylparaben
Target: Carbonic anhydrase 1 (Enzyme)
Gene: CA1
UniProt: P00915 (CAH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.59
Assay: Inhibition of human carbonic anhydrase 1 preincubated for 15 mins by CO2 hydration stopped-flow assay
Drug: methylparaben
Target: Carbonic anhydrase 9 (Enzyme)
Gene: CA9
UniProt: Q16790 (CAH9_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.26
Assay: Inhibition of human carbonic anhydrase 9 preincubated for 15 mins by CO2 hydration stopped-flow assay
Drug: methylparaben
Target: Carbonic anhydrase 12 (Enzyme)
Gene: CA12
UniProt: O43570 (CAH12_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.09
Assay: Inhibition of human carbonic anhydrase 12 preincubated for 15 mins by CO2 hydration stopped-flow assay
Drug: methylparaben
Target: Carbonic anhydrase 7 (Enzyme)
Gene: CA7
UniProt: P43166 (CAH7_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.11
Assay: Inhibition of human carbonic anhydrase 7 preincubated for 15 mins by CO2 hydration stopped-flow assay
Drug: methylparaben
Target: Carbonic anhydrase 14 (Enzyme)
Gene: CA14
UniProt: Q9ULX7 (CAH14_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.39
Assay: Inhibition of human carbonic anhydrase 14 preincubated for 15 mins by CO2 hydration stopped-flow assay
Drug: methylphenidate
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.252
Drug: methylphenidate
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.19
Assay: Displacement of [125I]RTI-55 from human SERT expressing HEK293 cells
Drug: methylphenidate
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.18
Action type: INHIBITOR
Assay: Displacement of [125I]RTI-55 from human NET expressing HEK293 cells
Drug: methylphenidate
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.615
Drug: methylphenidate
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.068
Drug: methylphenidate
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.96
Action type: INHIBITOR
Assay: Displacement of [125I]RTI-55 from human DAT expressing HEK293 cells
Drug: methylphenidate
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: Slc6a3
UniProt: P23977 (SC6A3_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.08
Assay: Tested for the ability to bind stereoselectively and enantioselectively to the dopamine transporter (DAT); Value ranges from 34 - 83 nM
Drug: methylprednisolone
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.5
Action type: AGONIST
Drug: methylprednisolone
Target: Annexin A1 (Cytosolic other)
Gene: ANXA1
UniProt: P04083 (ANXA1_HUMAN)
Organism: Homo sapiens
Drug: methylprednisolone
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.75
Assay: DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
Drug: methylprednisolone
Target: Short transient receptor potential channel 5 (Ion channel)
Gene: TRPC5
UniProt: Q9UL62 (TRPC5_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.92
Action type: ACTIVATOR
Assay: Measuring intracellular calcium elevation in HEK293 cells expressing hTRPC5.
Drug: methylprednisolone acetate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action
Drug: methylprednisolone succinate
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: methyprylon
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 ALLOSTERIC MODULATOR
Drug: methysergide
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.326
Assay: DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug: methysergide
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.57
Assay: DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
Drug: methysergide
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.214
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: methysergide
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.04
Assay: The compound was tested for affinity towards sigma-3 receptor
Drug: methysergide
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.509
Action type: PARTIAL AGONIST
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
Drug: methysergide
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.8
Action type: ANTAGONIST
Drug: methysergide
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.8
Action type: ANTAGONIST
Drug: methysergide
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.663
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: methysergide
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.229
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: methysergide
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.523
Drug: methysergide
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.263
Drug: methysergide
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.213
Drug: methysergide
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.334
Drug: methysergide
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.6
Action type: ANTAGONIST
Drug: methysergide
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.9
Action type: ANTAGONIST
Drug: methysergide
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki  7.054
Drug: methysergide
Target: 5-hydroxytryptamine receptor 5A (GPCR)
Gene: HTR5A
UniProt: P47898 (5HT5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7
Action type: ANTAGONIST
Drug: methysergide
Target: 5-hydroxytryptamine receptor 1F (GPCR)
Gene: HTR1F
UniProt: P30939 (5HT1F_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.2
Action type: ANTAGONIST
Drug: methysergide
Target: 5-hydroxytryptamine receptor 1E (GPCR)
Gene: HTR1E
UniProt: P28566 (5HT1E_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.8
Action type: ANTAGONIST
Drug: methysergide
Target: Induced myeloid leukemia cell differentiation protein Mcl-1 (Cytosolic other)
Gene: MCL1
UniProt: Q07820 (MCL1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.69
Assay: PUBCHEM_BIOASSAY: Fluorescence polarization-based biochemical high throughput dose response assay for inhibitors of myeloid cell leukemia sequence 1 (MCL1) interactions with BIM-BH3 peptide. (Class of assay: confirmatory) [Related pubchem assays: 2090 (Summary AID.), 2057 (Screening assay (MCL1 inhibitors).), 2168 (Screening assay (MCL1 inhibitors).)]
Drug: methysergide
Target: Bcl-2-like protein 1 (Cytosolic other)
Gene: BCL2L1
UniProt: Q07817 (B2CL1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.65
Assay: PUBCHEM_BIOASSAY: Counterscreen for inhibitors of MCL1: fluorescence polarization-based biochemical high throughput dose response assay for inhibitors of BCL2-related protein, long isoform (BCLXL). (Class of assay: confirmatory) [Related pubchem assays: 2129 (Screening assay (BCLXL inhibitors).), 2057 (Screening assay (MCL-1 inhibitors).), 2144 (Summary AID.), 2166 (Screening assay (BCLXL inhibitors).)]
Drug: methysergide
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.967
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug: methysergide
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.27
Drug: methysergide
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: Htr2a
UniProt: P14842 (5HT2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.8
Assay: Binding affinity to 5-hydroxytryptamine 2A receptor from rat cortex assayed using [3H]ketanserin as radioligand.
Drug: methysergide
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32305 (5HT7R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.9
Assay: Binding affinity towards 5-hydroxytryptamine 7 receptor
Drug: methysergide
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32304 (5HT7R_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.9
Action type: ANTAGONIST
Drug: methysergide
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: Htr6
UniProt: P31388 (5HT6R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.6
Action type: ANTAGONIST
Drug: methysergide
Target: Zinc finger protein mex-5 (Cytosolic other)
Gene: mex-5
UniProt: Q9XUB2 (MEX5_CAEEL)
Organism: Caenorhabditis elegans
Activity: EC50 = 4.91
Assay: Active
Drug: methysergide
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 = 8.28
Assay: Binding affinity which represents concentration giving half-maximal inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2 receptor from rat tissue homogenate
Drug: methysergide
Target: Cytoplasmic zinc-finger protein (Unclassified)
Gene: pos-1
UniProt: G5EF15 (G5EF15_CAEEL)
Organism: Caenorhabditis elegans
Activity: EC50 = 4.99
Assay: Active
Drug: methysergide
Target: 5-hydroxytryptamine receptor 5A (GPCR)
Gene: Htr5a
UniProt: P35364 (5HT5A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.7
Action type: ANTAGONIST
Drug: methysergide
Target: 5-hydroxytryptamine receptor 5A (GPCR)
Gene: Htr5a
UniProt: P30966 (5HT5A_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.2
Action type: ANTAGONIST
Drug: methysergide
Target: 5-hydroxytryptamine receptor 1F (GPCR)
Gene: Htr1f
UniProt: P30940 (5HT1F_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.8
Action type: ANTAGONIST
Drug: methysergide
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.45
Action type: AGONIST
Assay: Displacement of [3H]ketanserin from human 5HT2AR expressed in HEK-293 cells
Drug: methysergide
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.34
Action type: AGONIST
Assay: Displacement of [3H]mesulergine from human HTR2B expressed in CHO-K1 cells
Drug: methysergide
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.34
Action type: AGONIST
Assay: Displacement of [3H]mesulergine from human HTR2B expressed in HEK-293 cells
Drug: metiazinic acid
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P79208 (PGH2_SHEEP)
Organism: Ovis aries
Activity: IC50 = 4.98
Assay: Inhibition of ovine COX2 assessed as reduction in PGH2 production by enzyme immunoassay
Drug: metipranolol
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Assay: Mechanism of Action; CHEMBL213; SINGLE PROTEIN
Drug: metipranolol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Assay: Mechanism of Action; CHEMBL210; SINGLE PROTEIN
Drug: metixene
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Assay: Mechanism of Action; CHEMBL225; SINGLE PROTEIN
Drug: metixene
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Assay: Mechanism of Action; CHEMBL216; SINGLE PROTEIN
Drug: metixene
Target: Cholinesterase (Enzyme)
Gene: BCHE
UniProt: P81908 (CHLE_HORSE)
Organism: Equus caballus
Activity: IC50 = 5.8
Assay: Inhibition of Equine serum BChE using butyrylthiocholine iodide as a substrate after 20 mins by Ellman's assay
Drug: metochalcone
Target: ATP-binding cassette sub-family G member 2 (Transporter)
Gene: ABCG2
UniProt: Q9UNQ0 (ABCG2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.72
Assay: Inhibition of human BCRP expressed in MDCK2 cells assessed as Hoechst 33342 accumulation preincubated for 30 mins by fluorimetry
Drug: metoclopramide
Target: 5-hydroxytryptamine receptor 4 (GPCR)
Gene: HTR4
UniProt: O70528 (5HT4R_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 6.26
Assay: Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
Drug: metoclopramide
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.194
Action type: ANTAGONIST
Drug: metoclopramide
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.991
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: metoclopramide
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.979
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: metoclopramide
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.397
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: metoclopramide
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.904
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: metoclopramide
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.66
Drug: metoclopramide
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Drug: metoclopramide
Target: Aldehyde oxidase (Enzyme)
Gene: AOX1
UniProt: Q06278 (AOXA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.509
Drug: metoclopramide
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.097
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: metoclopramide
Target: 5-hydroxytryptamine receptor 3A (Ion channel)
Gene: HTR3A
UniProt: P46098 (5HT3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.699
Action type: ANTAGONIST
Drug: metoclopramide
Target: 5-hydroxytryptamine receptor 4 (GPCR)
Gene: HTR4
UniProt: Q13639 (5HT4R_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6
Action type: AGONIST