AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: metergoline
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.8
Action type: ANTAGONIST
Drug: metergoline
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.3
Assay: Evaluated for the binding affinity to porcine choroid plexus at 5-hydroxytryptamine 2C receptor binding site by using [3H]-MES as a radioligand.
Drug: metergoline
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.4
Action type: ANTAGONIST
Drug: metergoline
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.2
Assay: Displacement of [3H]5CT from 5HT7 receptor
Drug: metergoline
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.124
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: metergoline
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.583
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: metergoline
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.319
Assay: DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug: metergoline
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.018
Assay: DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug: metergoline
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.2
Action type: ANTAGONIST
Drug: metergoline
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.2
Action type: ANTAGONIST
Drug: metergoline
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.569
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: metergoline
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.301
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: metergoline
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: metergoline
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.42
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: metergoline
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P22303 (ACES_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.872
Assay: DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine)
Drug: metergoline
Target: 5-hydroxytryptamine receptor 5A (GPCR)
Gene: HTR5A
UniProt: P47898 (5HT5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.2
Action type: ANTAGONIST
Drug: metergoline
Target: 5-hydroxytryptamine receptor 1F (GPCR)
Gene: HTR1F
UniProt: P30939 (5HT1F_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.5
Action type: ANTAGONIST
Drug: metergoline
Target: 5-hydroxytryptamine receptor 1E (GPCR)
Gene: HTR1E
UniProt: P28566 (5HT1E_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.1
Action type: ANTAGONIST
Drug: metergoline
Target: Substance-K receptor (GPCR)
Gene: TACR2
UniProt: P21452 (NK2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.867
Assay: DRUGMATRIX: Tachykinin NK2  radioligand binding (ligand: [3H] SR-48968)
Drug: metergoline
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.839
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: metergoline
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.6
Assay: Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug: metergoline
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.02
Drug: metergoline
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.22
Assay: Evaluated for the binding affinity to hippocampus striatal membranes at 5-hydroxytryptamine 1A receptor binding site by using [3H]-8-OH- DPAT as a radioligand.
Drug: metergoline
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32305 (5HT7R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.2
Assay: Binding affinity towards 5-hydroxytryptamine 7 receptor
Drug: metergoline
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32304 (5HT7R_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.5
Action type: ANTAGONIST
Drug: metergoline
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: Htr6
UniProt: P31388 (5HT6R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.5
Action type: ANTAGONIST
Drug: metergoline
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 = 7.7
Assay: Evaluated for binding affinity towards rat cortical membranes at 5-hydroxytryptamine 1 receptor binding site by using [3H]-5-HT as a radioligand.
Drug: metergoline
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 = 9.52
Assay: Binding affinity to rat cortical membranes at 5-hydroxytryptamine 2 (5-HT2) receptor using [3H]KET as a radioligand
Drug: metformin
Target: 5'-AMP-activated protein kinase subunit beta-1 (Kinase)
Gene: PRKAB1
UniProt: Q9Y478 (AAKB1_HUMAN)
Organism: Homo sapiens
Drug: metformin
Target: Dipeptidyl peptidase 4 (Enzyme)
Gene: DPP4
UniProt: P27487 (DPP4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.54
Assay: Inhibition of DPP4
Drug: metformin
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 2.697
Drug: metformin
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 3.401
Drug: metformin
Target: Solute carrier family 22 member 3 (Transporter)
Gene: SLC22A3
UniProt: O75751 (S22A3_HUMAN)
Organism: Homo sapiens
Activity: Km = 2.499
Drug: metformin
Target: Mitochondrial complex I (NADH dehydrogenase) (Enzyme)
Gene: NDUFS8|NDUFA4|NDUFAB1|NDUFA1|NDUFS4|NDUFB5|NDUFB3|NDUFC1|NDUFA2|NDUFS5|NDUFS7|NDUFS2|NDUFS6|NDUFB1|NDUFS3|NDUFB6|NDUFA3|NDUFB4|NDUFB8|NDUFB2|NDUFA7|NDUFC2|NDUFA10|NDUFB10|MT-ND1|MT-ND2|MT-ND3|MT-ND4L|MT-ND4|MT-ND5|MT-ND6|NDUFB7|NDUFV2|NDUFS1|NDUFV1|NDUFA8|NDUFV3|NDUFA6|NDUFA5|NDUFA9|NDUFA11|NDUFAF2|NDUFAF3|NDUFA4L2|NDUFB11|NDUFAF4|NDUFA13|NDUFA12|NDUFAF1|NDUFB9
UniProt: O00217|O00483|O14561|O15239|O43181|O43674|O43676|O43677|O43678|O43920|O75251|O75306|O75380|O75438|O75489|O95139|O95167|O95168|O95169|O95178|O95182|O95298|O95299|O96000|P03886|P03891|P03897|P03901|P03905|P03915|P03923|P17568|P19404|P28331|P49821|P51970|P56181|P56556|Q16718|Q16795|Q86Y39|Q8N183|Q9BU61|Q9NRX3|Q9NX14|Q9P032|Q9P0J0|Q9UI09|Q9Y375|Q9Y6M9 (NDUS8_HUMAN|NDUA4_HUMAN|ACPM_HUMAN|NDUA1_HUMAN|NDUS4_HUMAN|NDUB5_HUMAN|NDUB3_HUMAN|NDUC1_HUMAN|NDUA2_HUMAN|NDUS5_HUMAN|NDUS7_HUMAN|NDUS2_HUMAN|NDUS6_HUMAN|NDUB1_HUMAN|NDUS3_HUMAN|NDUB6_HUMAN|NDUA3_HUMAN|NDUB4_HUMAN|NDUB8_HUMAN|NDUB2_HUMAN|NDUA7_HUMAN|NDUC2_HUMAN|NDUAA_HUMAN|NDUBA_HUMAN|NU1M_HUMAN|NU2M_HUMAN|NU3M_HUMAN|NU4LM_HUMAN|NU4M_HUMAN|NU5M_HUMAN|NU6M_HUMAN|NDUB7_HUMAN|NDUV2_HUMAN|NDUS1_HUMAN|NDUV1_HUMAN|NDUA8_HUMAN|NDUV3_HUMAN|NDUA6_HUMAN|NDUA5_HUMAN|NDUA9_HUMAN|NDUAB_HUMAN|MIMIT_HUMAN|NDUF3_HUMAN|NUA4L_HUMAN|NDUBB_HUMAN|NDUF4_HUMAN|NDUAD_HUMAN|NDUAC_HUMAN|CIA30_HUMAN|NDUB9_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2363065; PROTEIN COMPLEX
Drug: methacholine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.638
Drug: methacholine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.23
Assay: Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M2
Drug: methacholine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action; CHEMBL245; SINGLE PROTEIN
Drug: methacholine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.8
Assay: Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4
Drug: methacholine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: Chrm2
UniProt: P10980 (ACM2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.23
Assay: Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M2 in rat cerebral cortical membranes
Drug: methacholine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: Chrm1
UniProt: P08482 (ACM1_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 6.4
Action type: AGONIST
Drug: methacholine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: Chrm3
UniProt: P08483 (ACM3_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 6.92
Action type: AGONIST
Drug: methacholine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: Chrm4
UniProt: P08485 (ACM4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.8
Assay: Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug: metacycline
Target: DNA repair protein RAD52 homolog (Nuclear other)
Gene: RAD52
UniProt: P43351 (RAD52_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.7
Assay: Inhibition of RAD52 (unknown origin) assessed as reduction in RAD52-ssDNA interaction using Cy3-dT30-Cy5 ssDNA by FRET assay
Drug: methadone
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.78
Action type: AGONIST
Drug: methadone
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.01
Assay: Inhibitory concentration against potassium channel HERG
Drug: methadone
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.29
Assay: Binding affinity against opioid receptor kappa 1 using [3H]- U-69,593 radioligand
Drug: methadone
Target: Glutamate receptor ionotropic, NMDA 3A (Ion channel)
Gene: GRIN3A
UniProt: Q8TCU5 (NMD3A_HUMAN)
Organism: Homo sapiens
Drug: methadone
Target: Neuronal acetylcholine receptor subunit alpha-10 (Ion channel)
Gene: CHRNA10
UniProt: Q9GZZ6 (ACH10_HUMAN)
Organism: Homo sapiens
Drug: methadone
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.96
Assay: Binding affinity against delta-opiate receptor (human) using [3H]-DPDPE radioligand
Drug: methadone
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: IC50 = 7.29
Assay: Displacement of [3H]naloxone from Sprague-Dawley rat cerebellum opioid receptor assessed as relative receptor affinity by scintillation counting
Drug: acetylmethadol
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.66
Assay: Inhibitory concentration against potassium channel HERG
Drug: acetylmethadol
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action
Drug: methamphetamine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.383
Drug: methamphetamine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.08
Assay: Binding affinity towards sigma opioid receptor in guinea pig cerebral homogenate using [3H]DTG as radioligand
Drug: methamphetamine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.133
Action type: INHIBITOR
Drug: methamphetamine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki  7.91
Action type: INHIBITOR
Drug: methamphetamine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5
Drug: methamphetamine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.128
Drug: methamphetamine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.09
Drug: methamphetamine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.611
Action type: INHIBITOR
Drug: methamphetamine
Target: Trace amine-associated receptor 1 (GPCR)
Gene: TAAR1
UniProt: Q96RJ0 (TAAR1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.89
Action type: AGONIST
Assay: Activation of human TAAR1 expressed in human HEK293T cells assessed as cAMP accumulation after 10 mins by BRET assay
Drug: methamphetamine
Target: Synaptic vesicular amine transporter (Transporter)
Gene: Slc18a2
UniProt: Q01827 (VMAT2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.61
Assay: Inhibition of VMAT2-mediated [3H]-dopamine uptake in rat striata isolated synaptic vesicles by liquid scintillation spectroscopy
Drug: methamphetamine
Target: Trace amine-associated receptor 1 (GPCR)
Gene: TAAR1
UniProt: Q8HZ64 (TAAR1_MACMU)
Organism: Macaca mulatta
Activity: EC50 = 5.28
Assay: Activation of rhesus monkey TAAR1 expressed in RD-HGA16 cells co-expressing Gq protein assessed as cAMP accumulation by fluorescence plate reader
Drug: methamphetamine
Target: Trace amine-associated receptor 1 (GPCR)
Gene: Taar1
UniProt: Q923Y9 (TAAR1_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 6.88
Assay: Activation of rat wild type TAAR1 expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay
Drug: methamphetamine
Target: Trace amine-associated receptor 1 (GPCR)
Gene: Taar1
UniProt: Q923Y8 (TAAR1_MOUSE)
Organism: Mus musculus
Activity: EC50 = 7.15
Assay: Activation of mouse TAAR1 expressed in human HEK293 cells assessed as accumulation of cAMP after 15 mins
Drug: methanthelinium
Target: Muscarinic acetylcholine receptor (GPCR)
Gene: CHRM2|CHRM4|CHRM5|CHRM1|CHRM3
UniProt: P08172|P08173|P08912|P11229|P20309 (ACM2_HUMAN|ACM4_HUMAN|ACM5_HUMAN|ACM1_HUMAN|ACM3_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Drug: methapyrilene
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.36
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: methapyrilene
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.975
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: methapyrilene
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.86
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: methapyrilene
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.745
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: methapyrilene
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.27
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: methapyrilene
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.409
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: methapyrilene
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.843
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: methapyrilene
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.82
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: methapyrilene
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.745
Assay: DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug: methapyrilene
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.939
Assay: DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: methapyrilene
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.228
Assay: DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: methapyrilene
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.63
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: methapyrilene
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.66
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: methapyrilene
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.56
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: methaqualone
Target: GABA-A receptor alpha-1/beta-2/gamma-2 (Ion channel)
Gene: GABRA1|GABRG2|GABRB2
UniProt: P14867|P18507|P47870 (GBRA1_HUMAN|GBRG2_HUMAN|GBRB2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.41
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: methaqualone
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
Activity: EC50 = 4.52
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: methaqualone
Target: GABA A receptor alpha-2/beta-2/gamma-2 (Ion channel)
Gene: GABRG2|GABRA2|GABRB2
UniProt: P18507|P47869|P47870 (GBRG2_HUMAN|GBRA2_HUMAN|GBRB2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.61
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: methaqualone
Target: GABA A receptor alpha-3/beta-2/gamma-2 (Ion channel)
Gene: GABRG2|GABRA3|GABRB2
UniProt: P18507|P34903|P47870 (GBRG2_HUMAN|GBRA3_HUMAN|GBRB2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.31
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: methaqualone
Target: GABA A receptor alpha-4/beta-2/delta (Ion channel)
Gene: GABRD|GABRB2|GABRA4
UniProt: O14764|P47870|P48169 (GBRD_HUMAN|GBRB2_HUMAN|GBRA4_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.17
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: methaqualone
Target: GABA A receptor alpha-5/beta-2/gamma-2 (Ion channel)
Gene: GABRG2|GABRA5|GABRB2
UniProt: P18507|P31644|P47870 (GBRG2_HUMAN|GBRA5_HUMAN|GBRB2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.56
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: methaqualone
Target: GABA A receptor alpha-4/beta-3/delta (Ion channel)
Gene: GABRA4|GABRB3|GABRD
UniProt: P48169|P28472|O14764 (GBRA4_HUMAN|GBRB3_HUMAN|GBRD_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 3.91
Action type: AGONIST
Drug: methaqualone
Target: GABA-A receptor alpha-6/beta-2 (Ion channel)
Gene: GABRA6|GABRB2
UniProt: Q16445|P47870 (GBRA6_HUMAN|GBRB2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.13
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: methaqualone
Target: GABA-A receptor alpha-6/beta-2/delta (Ion channel)
Gene: GABRB2|GABRA6|GABRD
UniProt: P47870|Q16445|O14764 (GBRB2_HUMAN|GBRA6_HUMAN|GBRD_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.44
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: methaqualone
Target: GABA-A receptor alpha-6/beta-3/delta (Ion channel)
Gene: GABRD|GABRB3|GABRA6
UniProt: O14764|P28472|Q16445 (GBRD_HUMAN|GBRB3_HUMAN|GBRA6_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.5
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: metharbital
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: methazolamide
Target: Carbonic anhydrase 2 (Enzyme)
Gene: CA2
UniProt: P00918 (CAH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.05
Action type: INHIBITOR
Assay: Inhibitory activity against human carbonic anhydrase II
Drug: methazolamide
Target: Carbonic anhydrase 1 (Enzyme)
Gene: CA1
UniProt: P00915 (CAH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.85
Action type: INHIBITOR
Assay: Inhibition of human carbonic anhydrase 1-catalyzed CO2 hydration preincubated for 10 mins by stopped-flow assay
Drug: methazolamide
Target: Carbonic anhydrase 4 (Enzyme)
Gene: CA4
UniProt: P22748 (CAH4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.62
Action type: INHIBITOR
Assay: Inhibition of cloned isozyme, human carbonic anhydrase IV
Drug: methazolamide
Target: Carbonic anhydrase 9 (Enzyme)
Gene: CA9
UniProt: Q16790 (CAH9_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.57
Assay: Inhibitory activity against human carbonic anhydrase IX (hCA IX) by using CO2 hydrase assay method
Drug: methazolamide
Target: Carbonic anhydrase 12 (Enzyme)
Gene: CA12
UniProt: O43570 (CAH12_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.47
Assay: Ki value against human carbonic anhydrase XII (hCA XII)
Drug: methazolamide
Target: Carbonic anhydrase 5A, mitochondrial (Enzyme)
Gene: CA5A
UniProt: P35218 (CAH5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.19
Assay: Inhibitory activity against human recombinant mitochondrial isozyme CA VA
Drug: methazolamide
Target: Carbonic anhydrase 5B, mitochondrial (Enzyme)
Gene: CA5B
UniProt: Q9Y2D0 (CAH5B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.21
Assay: Inhibitory activity against human recombinant mitochondrial isozyme CA VB