AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: aspartic acid
Target: Aspartate aminotransferase, cytoplasmic (Enzyme)
Gene: GOT1
UniProt: P17174 (AATC_HUMAN)
Organism: Homo sapiens
Drug: aspartic acid
Target: Aspartoacylase (Enzyme)
Gene: ASPA
UniProt: P45381 (ACY2_HUMAN)
Organism: Homo sapiens
Drug: aspartic acid
Target: Asparagine synthetase [glutamine-hydrolyzing] (Enzyme)
Gene: ASNS
UniProt: P08243 (ASNS_HUMAN)
Organism: Homo sapiens
Drug: aspartic acid
Target: Argininosuccinate synthase (Enzyme)
Gene: ASS1
UniProt: P00966 (ASSY_HUMAN)
Organism: Homo sapiens
Drug: aspartic acid
Target: Aminoacylase-1 (Enzyme)
Gene: ACY1
UniProt: Q03154 (ACY1_HUMAN)
Organism: Homo sapiens
Drug: aspartic acid
Target: Aspartate aminotransferase, mitochondrial (Enzyme)
Gene: GOT2
UniProt: P00505 (AATM_HUMAN)
Organism: Homo sapiens
Drug: aspartic acid
Target: Aspartate--tRNA ligase, cytoplasmic (Enzyme)
Gene: DARS
UniProt: P14868 (SYDC_HUMAN)
Organism: Homo sapiens
Drug: aspartic acid
Target: Aspartyl/asparaginyl beta-hydroxylase (Enzyme)
Gene: ASPH
UniProt: Q12797 (ASPH_HUMAN)
Organism: Homo sapiens
Drug: aspartic acid
Target: Excitatory amino acid transporter 1 (Transporter)
Gene: SLC1A3
UniProt: P43003 (EAA1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.03
Assay: Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method
Drug: aspartic acid
Target: Excitatory amino acid transporter 2 (Transporter)
Gene: SLC1A2
UniProt: P43004 (EAA2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.5
Assay: Inhibition of human EAAT2 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method
Drug: aspartic acid
Target: Excitatory amino acid transporter 3 (Transporter)
Gene: SLC1A1
UniProt: P43005 (EAA3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.71
Assay: Inhibition of human EAAT3 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method
Drug: aspartic acid
Target: Calcium-binding mitochondrial carrier protein Aralar2 (Transporter)
Gene: SLC25A13
UniProt: Q9UJS0 (CMC2_HUMAN)
Organism: Homo sapiens
Drug: aspartic acid
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: IC50 = 5.79
Assay: Compound was evaluated for the inhibition of [3H]-CGS-19,755 binding at N-methyl-D-aspartate glutamate receptor
Drug: aspartic acid
Target: Excitatory amino acid transporter 4 (Transporter)
Gene: Slc1a6
UniProt: O35921 (EAA4_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.96
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: aspartic acid
Target: Glutamate transporter homolog (Transporter)
UniProt: O59010 (GLT_PYRHO)
Organism: Pyrococcus horikoshii
Activity: Kd = 9
Assay: Binding affinity to Pyrococcus horikoshii sodium-coupled aspartate transporter L130W mutant fluorescence-based assay in presence of NaCl
Drug: latanoprost
Target: Prostaglandin E2 receptor EP1 subtype (GPCR)
Gene: PTGER1
UniProt: P34995 (PE2R1_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.757
Drug: latanoprost
Target: Prostaglandin E2 receptor EP3 subtype (GPCR)
Gene: PTGER3
UniProt: P43115 (PE2R3_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.187
Drug: latanoprost
Target: Prostaglandin F2-alpha receptor (GPCR)
Gene: PTGFR
UniProt: P43088 (PF2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.3
Action type: AGONIST
Drug: latanoprost
Target: Prostaglandin F2-alpha receptor (GPCR)
Gene: PTGFR
UniProt: P37289 (PF2R_BOVIN)
Organism: Bos taurus
Activity: Ki = 7.01
Assay: Displacement of [3H]PGF2 alpha from FP receptor in bovine corpus luteum membrane
Drug: leflunomide
Target: Sodium/nucleoside cotransporter 1 (Transporter)
Gene: SLC28A1
UniProt: O00337 (S28A1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.287
Assay: DRUGMATRIX: Sodium/nucleoside co-transporter radioligand binding (ligand: nitrobenzylthioinosine)
Drug: leflunomide
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.338
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: leflunomide
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.64
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: leflunomide
Target: Dihydroorotate dehydrogenase (quinone), mitochondrial (Enzyme)
Gene: DHODH
UniProt: Q02127 (PYRD_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5
Action type: INHIBITOR
Assay: Immunosuppressive activity expressed as ability to inhibit human recombinant dihydroorotate dehydrogenase (DHODH)
Drug: leflunomide
Target: Cytochrome P450 1A2 (Enzyme)
Gene: CYP1A2
UniProt: P05177 (CP1A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.301
Assay: DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: leflunomide
Target: Amine oxidase [flavin-containing] A (Enzyme)
Gene: MAOA
UniProt: P21397 (AOFA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.684
Assay: DRUGMATRIX: Monoamine Oxidase MAO-A enzyme inhibition (substrate: Kynuramine)
Drug: leflunomide
Target: Dihydroorotate dehydrogenase (quinone), mitochondrial (Enzyme)
Gene: Dhodh
UniProt: Q63707 (PYRD_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.05
Assay: Inhibitory concentration tested against enzyme dihydroorotate dehydrogenase in rat
Drug: leflunomide
Target: Dihydroorotate dehydrogenase (quinone), mitochondrial (Enzyme)
Gene: Dhodh
UniProt: O35435 (PYRD_MOUSE)
Organism: Mus musculus
Activity: IC50 = 7.52
Assay: Inhibitory concentration tested on enzyme dihydroorotate dehydrogenase in mouse
Drug: letrozole
Target: Aromatase (Enzyme)
Gene: CYP19A1
UniProt: P11511 (CP19A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.22
Action type: INHIBITOR
Drug: letrozole
Target: Cytochrome P450 11B1, mitochondrial (Enzyme)
Gene: CYP11B1
UniProt: P15538 (C11B1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.58
Assay: Inhibition of human CYP11B1 expressed in hamster V79MZh cells using [1,2-3H]-11-deoxy-corticosterone as substrate
Drug: letrozole
Target: Cytochrome P450 11B2, mitochondrial (Enzyme)
Gene: CYP11B2
UniProt: P19099 (C11B2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.85
Assay: Inhibition of human CYP11B2 expressed in hamster V79MZh cells using [1,2-3H]-11-deoxy-corticosterone as substrate
Drug: leucine
Target: Large neutral amino acids transporter small subunit 1 (Transporter)
Gene: SLC7A5
UniProt: Q01650 (LAT1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.07
Assay: Cis-inhibition of human LAT1 expressed in TREx HEK293 cells at 200 uM assessed as inhibition of [3H]-gabapentin uptake preincubated for 3 mins at 37 degC followed by washing with choline buffer and measured after 3 hrs by scintillation counting analysis relative to BCH
Drug: leuprorelin
Target: Gonadotropin-releasing hormone receptor (GPCR)
Gene: GNRHR
UniProt: P30968 (GNRHR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.523
Action type: AGONIST
Drug: leuprorelin
Target: Gonadotropin-releasing hormone receptor (GPCR)
Gene: Gnrhr
UniProt: P30969 (GNRHR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 9.3
Assay: The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
Drug: levallorphan
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.32
Action type: ANTAGONIST
Assay: Displacement of [125I]-IBOxyA from MOR-1 expressed in CHO cells
Drug: levallorphan
Target: Mu-type opioid receptor (GPCR)
Gene: Oprm1
UniProt: P33535 (OPRM_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 9.2
Assay: Displacement of [3H]-dihydromorphine from mu opioid receptor in rat cerebral cortex by liquid scintillation counting
Drug: levallorphan
Target: Acetylcholinesterase (Enzyme)
Gene: ache
UniProt: O42275 (ACES_ELEEL)
Organism: Electrophorus electricus
Activity: Ki = 4.92
Assay: Inhibition of electric eel AChE by Ellman's method
Drug: levallorphan
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 = 9.27
Assay: Inhibition of [3H]naloxone binding to opioid receptor in presence of NaCl
Drug: levamisole
Target: Acetylcholine receptor subunit alpha-type unc-63 (Ion channel)
Gene: unc-63
UniProt: Q9N587 (ACH6_CAEEL)
Organism: Caenorhabditis elegans
Drug: levamisole
Target: Alkaline phosphatase, tissue-nonspecific isozyme (Enzyme)
Gene: ALPL
UniProt: P05186 (PPBT_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.8
Assay: Inhibition of TNSALP
Drug: levamisole
Target: Nicotinic acetylcholine receptor alpha subunit (Ion channel)
UniProt: O96760 (O96760_ASCSU)
Organism: Ascaris suum
Action type: AGONIST
Assay: Mechanism of Action; CHEMBL1884; SINGLE PROTEIN
Drug: levamisole
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.568
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: levamisole
Target: Alkaline phosphatase, tissue-nonspecific isozyme (Enzyme)
Gene: ALPL
UniProt: P09487 (PPBT_BOVIN)
Organism: Bos taurus
Activity: IC50 = 4.72
Drug: levamisole
Target: Intestinal-type alkaline phosphatase (Enzyme)
Gene: ALPI
UniProt: P09923 (PPBI_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.69
Assay: Inhibition of human IAP using CDP-star as substrate pretreated for 10 mins followed by substrate addition measured after 10 mins by spectrophotometric method
Drug: levamfetamine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.33
Assay: Binding affinity towards sigma opioid receptor in guinea pig cerebral homogenate using [3H]DTG as radioligand
Drug: levamfetamine
Target: Trace amine-associated receptor 1 (GPCR)
Gene: TAAR1
UniProt: Q96RJ0 (TAAR1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.6
Assay: Activation of human TAAR1 expressed in human HEK293T cells assessed as cAMP accumulation after 10 mins by BRET assay
Drug: levamfetamine
Target: Trace amine-associated receptor 1 (GPCR)
Gene: TAAR1
UniProt: Q8HZ64 (TAAR1_MACMU)
Organism: Macaca mulatta
Activity: EC50 = 5.73
Assay: Activation of rhesus monkey TAAR1 expressed in RD-HGA16 cells co-expressing Gq protein assessed as cAMP accumulation by fluorescence plate reader
Drug: levamfetamine
Target: Trace amine-associated receptor 1 (GPCR)
Gene: Taar1
UniProt: Q923Y9 (TAAR1_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 7.47
Assay: Activation of rat wild type TAAR1 expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay
Drug: levamfetamine
Target: Trace amine-associated receptor 1 (GPCR)
Gene: Taar1
UniProt: Q923Y8 (TAAR1_MOUSE)
Organism: Mus musculus
Activity: EC50 = 7.19
Assay: Activation of mouse TAAR1 expressed in human HEK293 cells assessed as accumulation of cAMP after 15 mins
Drug: levamfetamine
Target: Serotonin (5-HT) receptor (GPCR)
Gene: Htr2c|Htr2a|Htr1a|Htr1b|Htr1d|Htr1f|Htr2b|Htr6|Htr7|Htr5a|Htr5b|Htr3a|Htr4|Htr3b
UniProt: P08909|P14842|P19327|P28564|P28565|P30940|P30994|P31388|P32305|P35364|P35365|P35563|Q62758|Q9JJ16 (5HT2C_RAT|5HT2A_RAT|5HT1A_RAT|5HT1B_RAT|5HT1D_RAT|5HT1F_RAT|5HT2B_RAT|5HT6R_RAT|5HT7R_RAT|5HT5A_RAT|5HT5B_RAT|5HT3A_RAT|5HT4R_RAT|5HT3B_RAT)
Organism: Rattus norvegicus
Activity: Kd = 5.16
Assay: Affinity against 5-hydroxytryptamine receptors in rat fundus model
Drug: levetiracetam
Target: Sodium channel protein type 1 subunit alpha (Ion channel)
Gene: SCN1A
UniProt: P35498 (SCN1A_HUMAN)
Organism: Homo sapiens
Drug: levetiracetam
Target: Voltage-dependent T-type calcium channel subunit alpha-1G (Ion channel)
Gene: CACNA1G
UniProt: O43497 (CAC1G_HUMAN)
Organism: Homo sapiens
Drug: levetiracetam
Target: Carbonic anhydrase 1 (Enzyme)
Gene: CA1
UniProt: P00915 (CAH1_HUMAN)
Organism: Homo sapiens
Drug: levetiracetam
Target: Synaptic vesicle glycoprotein 2A (Unclassified)
Gene: Sv2a
UniProt: Q02563 (SV2A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.1
Action type: INHIBITOR
Assay: <i>In vitro</i> inhibitory activity against [<sup>3</sup>H](2S)-2-[4-(3-azidophenyl)-2-oxopyrrolidin-1-yl]butanamide binding to levetiracetam binding site, in rat brain homogenate
Drug: levetiracetam
Target: Synaptic vesicle glycoprotein 2A (Transporter)
Gene: SV2A
UniProt: Q7L0J3 (SV2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.1
Action type: MODULATOR
Assay: Mechanism of Action; CHEMBL1998; SINGLE PROTEIN
Drug: levocabastine
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Drug: levocabastine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.279
Action type: ANTAGONIST
Drug: levocabastine
Target: Neurotensin receptor type 2 (GPCR)
Gene: NTSR2
UniProt: O95665 (NTR2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.8
Action type: AGONIST
Drug: levocabastine
Target: Neurotensin receptor 2 (GPCR)
Gene: Ntsr2
UniProt: Q63384 (NTR2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.48
Assay: Displacement of [125I]NT at rat NTS2 overexpressed in CHOK1 cells after 30 mins by gamma counting
Drug: levocabastine
Target: Neurotensin receptor type 2 (GPCR)
Gene: Ntsr2
UniProt: P70310 (NTR2_MOUSE)
Organism: Mus musculus
Activity: IC50 = 8.7
Action type: AGONIST
Drug: levocetirizine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.95
Action type: ANTAGONIST
Drug: levodopa
Target: Large neutral amino acids transporter small subunit 1 (Transporter)
Gene: SLC7A5
UniProt: Q01650 (LAT1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4
Assay: Inhibition of LAT1-mediated [14C]-L-leucine uptake in human MCF7 cells after 5 mins by liquid scintillation counting method
Drug: levodopa
Target: Epidermal growth factor receptor (Kinase)
Gene: EGFR
UniProt: P00533 (EGFR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.541
Assay: DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: levodopa
Target: Tyrosine-protein kinase Lck (Kinase)
Gene: LCK
UniProt: P06239 (LCK_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.428
Assay: DRUGMATRIX: Protein Tyrosine Kinase, LCK enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: levodopa
Target: Tyrosine-protein kinase Fyn (Kinase)
Gene: FYN
UniProt: P06241 (FYN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.668
Assay: DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: levodopa
Target: Arachidonate 15-lipoxygenase (Enzyme)
Gene: ALOX15
UniProt: P12530 (LOX15_RABIT)
Organism: Oryctolagus cuniculus
Activity: IC50 = 5.646
Assay: DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid)
Drug: levodopa
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Drug: levodopa
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Drug: levofloxacin
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 3.04
Drug: levofloxacin
Target: DNA gyrase subunit A (Enzyme)
Gene: gyrA
UniProt: P9WG47 (GYRA_MYCTU)
Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)
Activity: IC50 = 4.28
Assay: Inhibition of DNA supercoiling activity of wild type Mycobacterium tuberculosis DNA gyrase A
Drug: levofloxacin
Target: Multidrug and toxin extrusion protein 1 (Transporter)
Gene: SLC47A1
UniProt: Q96FL8 (S47A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.75
Assay: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Drug: levofloxacin
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: levofloxacin
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: levofloxacin
Target: CAAX prenyl protease 2 (Enzyme)
Gene: RCE1
UniProt: Q9Y256 (FACE2_HUMAN)
Organism: Homo sapiens
Activity: AC50 = 4.39
Assay: PUBCHEM_BIOASSAY: Human Ras-Converting Enzyme Inhibition Assay Measured in Biochemical System Using Plate Reader - 2034-04_Inhibitor_Dose_CherryPick_Activity. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID2618]
Drug: levomethadyl acetate
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Drug: levomethadyl acetate
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.66
Drug: levonorgestrel
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.225
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: levonorgestrel
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.167
Assay: DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
Drug: levonorgestrel
Target: Estrogen receptor (Nuclear hormone receptor)
Gene: ESR1
UniProt: P03372 (ESR1_HUMAN)
Organism: Homo sapiens
Drug: levonorgestrel
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Activity: ED50 = 12.796
Action type: AGONIST
Drug: levonorgestrel
Target: Sex hormone-binding globulin (Secreted)
Gene: SHBG
UniProt: P04278 (SHBG_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.91
Assay: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin
Drug: levonorgestrel
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.37
Assay: DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
Drug: levonorgestrel
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 9.339
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: levorphanol
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.68
Action type: AGONIST
Assay: Inhibition of [3H]-DAMGO binding to Opioid receptor mu 1 of Chinese hamster ovary membrane
Drug: levorphanol
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.64
Assay: Inhibition of [3H]U-69593 binding to Opioid receptor kappa 1 of Chinese hamster ovary membrane
Drug: levorphanol
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.38
Assay: Inhibition of [3H]naltrindole binding to opioid receptor delta 1 of Chinese hamster ovary membrane
Drug: levorphanol
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.1
Assay: Inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis
Drug: levorphanol
Target: Mu-type opioid receptor (GPCR)
Gene: Oprm1
UniProt: P42866 (OPRM_MOUSE)
Organism: Mus musculus
Activity: Ki = 9.52
Assay: Binding affinity for mouse opioid receptor mu
Drug: levorphanol
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P97266 (OPRM_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 9.68
Assay: Binding affinity against opioid receptor mu 1 using [3H]DAMGO as radioligand in guinea pig brain membranes.
Drug: levorphanol
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41144 (OPRK_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 8.64
Assay: Binding affinity against opioid receptor kappa 1 using [3H]-U-69,593 as radioligand in guinea pig brain membranes.
Drug: levorphanol
Target: Acetylcholinesterase (Enzyme)
Gene: ache
UniProt: O42275 (ACES_ELEEL)
Organism: Electrophorus electricus
Activity: Ki = 4.6
Assay: Inhibition of electric eel AChE by Ellman's method
Drug: levorphanol
Target: Kappa-type opioid receptor (GPCR)
Gene: Oprk1
UniProt: P33534 (OPRK_MOUSE)
Organism: Mus musculus
Activity: Ki = 8
Assay: Binding affinity for mouse opioid receptor kappa
Drug: levorphanol
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: Sigmar1
UniProt: O55242 (SGMR1_MOUSE)
Organism: Mus musculus
Activity: Ki = 8.72
Assay: Binding affinity for mouse sigma opioid receptor
Drug: levorphanol
Target: Glutamate [NMDA] receptor (Ion channel)
Gene: GRIN2D|GRIN3B|GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN3A
UniProt: O15399|O60391|Q05586|Q12879|Q13224|Q14957|Q8TCU5 (NMDE4_HUMAN|NMD3B_HUMAN|NMDZ1_HUMAN|NMDE1_HUMAN|NMDE2_HUMAN|NMDE3_HUMAN|NMD3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.6
Assay: Binding affinity against dextromethorpin binding site associated with N-methyl-D-aspartate glutamate receptor from guinea pig mitochondriall pellet P2 determined using [3H]1 as radioligand.
Drug: levorphanol
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: IC50 = 5.92
Assay: Binding affinity against PCP binding site associated with N-methyl-D-aspartate glutamate receptor from rat synaptic plasma membrane(SPM) determined using [3H]TCP as radioligand.
Drug: levorphanol
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: EC50 = 9.15
Assay: Binding affinity to opioid receptor in rat brain homogenates
Drug: levorphanol
Target: Sodium channel alpha subunits; brain (Types I, II, III) (Ion channel)
Gene: SCN1A|SCN2A|SCN3A
UniProt: P35498|Q99250|Q9NY46 (SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.6
Assay: Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex
Drug: levosalbutamol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.42
Action type: AGONIST
Assay: Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acid
Drug: levosimendan
Target: cGMP-inhibited 3',5'-cyclic phosphodiesterase A (Enzyme)
Gene: PDE3A
UniProt: Q14432 (PDE3A_HUMAN)
Organism: Homo sapiens
Drug: levosimendan
Target: ATP-sensitive inward rectifier potassium channel 11 (Ion channel)
Gene: KCNJ11
UniProt: Q14654 (KCJ11_HUMAN)
Organism: Homo sapiens
Drug: levosimendan
Target: ATP-sensitive inward rectifier potassium channel 8 (Ion channel)
Gene: KCNJ8
UniProt: Q15842 (KCNJ8_HUMAN)
Organism: Homo sapiens
Drug: levosimendan
Target: Troponin C, slow skeletal and cardiac muscles (Cytosolic other)
Gene: TNNC1
UniProt: P63316 (TNNC1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 3.155
Action type: OPENER
Assay: affinity for the binding of levosimendan to cNTnC-Ca2+-cTnI-(144-163) complex