AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: terconazole
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.511
Assay: DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: terconazole
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.718
Assay: DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: terconazole
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.504
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: terconazole
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.215
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: terconazole
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.362
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: terconazole
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.27
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: terconazole
Target: Lanosterol 14-alpha demethylase (Enzyme)
Gene: ERG11
UniProt: P10613 (CP51_CANAL)
Organism: Candida albicans (strain SC5314 / ATCC MYA-2876)
Action type: INHIBITOR
Drug: terconazole
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P22303 (ACES_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.666
Assay: DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine)
Drug: terconazole
Target: Tyrosine-protein kinase Fyn (Kinase)
Gene: FYN
UniProt: P06241 (FYN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.963
Assay: DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: terconazole
Target: Lanosterol 14-alpha demethylase (Enzyme)
Gene: CYP51A1
UniProt: Q16850 (CP51A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.52
Assay: Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay
Drug: terconazole
Target: Heme oxygenase 2 (Enzyme)
Gene: Hmox2
UniProt: P23711 (HMOX2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.3
Assay: Inhibition of rat brain microsome HO-2 preincubated for 10 mins followed by beta-NADPH addition and measured after 15 mins by gas chromatography
Drug: terconazole
Target: Arachidonate 15-lipoxygenase (Enzyme)
Gene: ALOX15
UniProt: P12530 (LOX15_RABIT)
Organism: Oryctolagus cuniculus
Activity: IC50 = 5.612
Assay: DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid)
Drug: terconazole
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.102
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: terconazole
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.389
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug: terconazole
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.71
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: terconazole
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.88
Drug: terfenadine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.874
Assay: DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug: terfenadine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.687
Assay: DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
Drug: terfenadine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.252
Drug: terfenadine
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.854
Drug: terfenadine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.719
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: terfenadine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.137
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: terfenadine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.523
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: terfenadine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.19
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: terfenadine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.218
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: terfenadine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.292
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: terfenadine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.699
Action type: ANTAGONIST
Drug: terfenadine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.54
Assay: Compound is evaluated for in vitro receptor binding affinity against Muscarinic acetylcholine receptor M1
Drug: terfenadine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.264
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: terfenadine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.693
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: terfenadine
Target: Epidermal growth factor receptor (Kinase)
Gene: EGFR
UniProt: P00533 (EGFR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.448
Assay: DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: terfenadine
Target: C-C chemokine receptor type 5 (GPCR)
Gene: CCR5
UniProt: P51681 (CCR5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.07
Assay: DRUGMATRIX: Chemokine CCR5 radioligand binding (ligand: [125I] MIP-1alpha)
Drug: terfenadine
Target: Tyrosine-protein kinase Fyn (Kinase)
Gene: FYN
UniProt: P06241 (FYN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.213
Assay: DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: terfenadine
Target: Cytochrome P450 2J2 (Enzyme)
Gene: CYP2J2
UniProt: P51589 (CP2J2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.09
Assay: Inhibition of human recombinant CYP2J2 expressed in baculovirus-infected Sf9 insect cells
Drug: terfenadine
Target: Substance-K receptor (GPCR)
Gene: TACR2
UniProt: P21452 (NK2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.05
Assay: DRUGMATRIX: Tachykinin NK2  radioligand binding (ligand: [3H] SR-48968)
Drug: terfenadine
Target: Potassium voltage-gated channel subfamily H member 1 (Ion channel)
Gene: KCNH1
UniProt: O95259 (KCNH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.8
Action type: BLOCKER
Drug: terfenadine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.734
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: terfenadine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P31389 (HRH1_CAVPO)
Organism: Cavia porcellus
Activity: Kd = 7.45
Assay: Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.
Drug: terfenadine
Target: Heat shock protein HSP 90-alpha (Cytosolic other)
Gene: HSP90AA1
UniProt: P07900 (HS90A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.46
Drug: terfenadine
Target: Adrenergic receptor alpha-1 (GPCR)
Gene: ADRA1D|ADRA1A|ADRA1B
UniProt: P25100|P35348|P35368 (ADA1D_HUMAN|ADA1A_HUMAN|ADA1B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.63
Assay: Compound is evaluated for in vitro receptor binding affinity against Alpha-1 adrenergic receptor
Drug: terfenadine
Target: Transcriptional activator protein luxR (Unclassified)
Gene: luxR
UniProt: P12746 (LUXR_ALIFS)
Organism: Aliivibrio fischeri
Activity: IC50 = 4.04
Assay: Inhibition of LuxR-dependent quorum sensing in Vibrio fischeri assessed as reduction of 3-oxo-C6-HSL-induced bioluminescence intensity
Drug: terguride
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.18
Drug: terguride
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki  7.7
Drug: terguride
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki  7.55
Drug: terguride
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.1
Action type: AGONIST
Drug: terguride
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.5
Action type: ANTAGONIST
Drug: terguride
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.5
Action type: AGONIST
Drug: terguride
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.3
Action type: ANTAGONIST
Drug: terguride
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.5
Action type: ANTAGONIST
Drug: terguride
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.4
Action type: ANTAGONIST
Drug: terguride
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9
Action type: AGONIST
Drug: terguride
Target: D(1B) dopamine receptor (GPCR)
Gene: DRD5
UniProt: P21918 (DRD5_HUMAN)
Organism: Homo sapiens
Activity: Ki  7.63
Drug: terguride
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.6
Action type: AGONIST
Drug: terguride
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.8
Action type: AGONIST
Drug: terguride
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.1
Action type: ANTAGONIST
Drug: terguride
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.1
Action type: ANTAGONIST
Drug: terguride
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki  8.41
Drug: terguride
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki  7.46
Drug: terguride
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.4
Assay: In vitro binding activity against dopamine receptor D2 from homogenized rat brain, using [3H]spiperone as the radioligand
Drug: terguride
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.6
Assay: In vitro binding activity against 5-hydroxytryptamine 1A receptor from homogenized rat brain, using [3H]-8-OH-DPAT as the radioligand
Drug: terguride
Target: D(1A) dopamine receptor (GPCR)
Gene: Drd1
UniProt: P18901 (DRD1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.16
Assay: In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
Drug: terguride
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.3
Action type: AGONIST
Drug: terguride
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.2
Action type: ANTAGONIST
Drug: terodiline
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.3
Assay: Inhibitory concentration against IKr potassium channel
Drug: tertatolol
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.087
Drug: tertatolol
Target: Beta-3 adrenergic receptor (GPCR)
Gene: ADRB3
UniProt: P13945 (ADRB3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.6
Action type: ANTAGONIST
Drug: tertatolol
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.11
Assay: The compound was evaluated for binding affinity against 5-hydroxytryptamine 1A receptor in rat hippocampal membranes using [3H]8-OH-DPAT as radioligand in the presence of 1 mM of MnCl2
Drug: tertatolol
Target: Beta-3 adrenergic receptor (GPCR)
Gene: Adrb3
UniProt: P25962 (ADRB3_MOUSE)
Organism: Mus musculus
Activity: Ki = 7
Action type: ANTAGONIST
Drug: tertatolol
Target: Beta-3 adrenergic receptor (GPCR)
Gene: Adrb3
UniProt: P26255 (ADRB3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7
Action type: ANTAGONIST
Drug: testolactone
Target: Aromatase (Enzyme)
Gene: CYP19A1
UniProt: P11511 (CP19A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.46
Action type: INHIBITOR
Drug: testosterone
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.92
Assay: Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand
Drug: testosterone
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.837
Assay: DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
Drug: testosterone
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 9.2
Action type: AGONIST
Drug: testosterone
Target: Aromatase (Enzyme)
Gene: CYP19A1
UniProt: P11511 (CP19A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.22
Assay: Inhibition of human placental aromatase Cytochrome P450 19A1
Drug: testosterone
Target: Corticosteroid-binding globulin (Secreted)
Gene: SERPINA6
UniProt: P08185 (CBG_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.72
Drug: testosterone
Target: Sex hormone-binding globulin (Secreted)
Gene: SHBG
UniProt: P04278 (SHBG_HUMAN)
Organism: Homo sapiens
Activity: Kd = 9.2
Assay: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin
Drug: testosterone
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: testosterone
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.85
Assay: Inhibitory constant against rat prostate cytosol androgen receptor using [3H]mibolerone
Drug: testosterone
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 6.599
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: testosterone
Target: C-8 sterol isomerase (Enzyme)
Gene: ERG2
UniProt: P32352 (ERG2_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: Ki = 5.11
Assay: Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand
Drug: testosterone
Target: Steroid 5-alpha-reductase (Enzyme)
Gene: Srd5a1|Srd5a2
UniProt: P24008|P31214 (S5A1_RAT|S5A2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.72
Assay: In vitro inhibitory activity against rat prostatic steroid 5-alpha-reductase
Drug: testosterone
Target: Constitutive androstane receptor (Nuclear hormone receptor)
Gene: Nr1i3
UniProt: O35627 (NR1I3_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4.52
Assay: Inhibitory concentration against mammalian m-constitutive androstane receptor (mCAR) activity
Drug: testosterone undecanoate
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action; CHEMBL1871; SINGLE PROTEIN
Drug: tetrabenazine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.678
Drug: tetrabenazine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.018
Drug: tetrabenazine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.886
Drug: tetrabenazine
Target: Synaptic vesicular amine transporter (Transporter)
Gene: SLC18A2
UniProt: Q05940 (VMAT2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7
Action type: INHIBITOR
Drug: tetrabenazine
Target: Synaptic vesicular amine transporter (Transporter)
Gene: SLC18A2
UniProt: Q27963 (VMAT2_BOVIN)
Organism: Bos taurus
Activity: Ki = 8.4
Assay: Inhibition of dopamine uptake at VMAT in bovine chromaffin granule ghosts
Drug: tetrabenazine
Target: Synaptic vesicular amine transporter (Transporter)
Gene: Slc18a2
UniProt: Q01827 (VMAT2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.12
Assay: Displacement of [3H]DHTBZ from Sprague-Dawley rat striatum VMAT2 after 1 hr by liquid scintillation counting
Drug: tetrabenazine
Target: Chromaffin granule amine transporter (Transporter)
Gene: SLC18A1
UniProt: P54219 (VMAT1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.7
Action type: INHIBITOR
Drug: tetrabenazine
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 = 4.07
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: tetracaine
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.28
Action type: BLOCKER
Assay: Inhibition of human NaV1.5 alpha subunit expressed in CHOK1 cells at -90 mV holding potential by patch clamp electrophysiological assay
Drug: tetracaine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.153
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: tetracaine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.011
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: tetracaine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.766
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: tetracaine
Target: Sodium channel protein type 2 subunit alpha (Ion channel)
Gene: SCN2A
UniProt: Q99250 (SCN2A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.96
Action type: BLOCKER
Assay: Inhibition of human NaV1.2 alpha subunit expressed in CHOK1 cells at -65 mV holding potential by patch clamp electrophysiological assay
Drug: tetracaine
Target: Sodium channel protein type 8 subunit alpha (Ion channel)
Gene: SCN8A
UniProt: Q9UQD0 (SCN8A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.28
Assay: Inhibition of recombinant human Nav1.6 expressed in HEK293 cells preincubated for 40 mins followed by DiSBAC2 substrate addition measured after 90 mins by FRET assay
Drug: tetracaine
Target: Sodium channel protein type 9 subunit alpha (Ion channel)
Gene: SCN9A
UniProt: Q15858 (SCN9A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.3
Action type: BLOCKER
Assay: Displacement of [3H]BTX from human Nav1.7 expressed in human HEK293 cells after 1 hr by MicroBeta analyzer
Drug: tetracaine
Target: Amine oxidase [flavin-containing] A (Enzyme)
Gene: MAOA
UniProt: P21397 (AOFA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.499
Assay: DRUGMATRIX: Monoamine Oxidase MAO-A enzyme inhibition (substrate: Kynuramine)
Drug: tetracaine
Target: cGMP-gated cation channel alpha-1 (Ion channel)
Gene: CNGA1
UniProt: Q00194 (CNGA1_BOVIN)
Organism: Bos taurus
Activity: Kd = 5.17
Assay: Apparent dissociation constant against Cyclic nucleotide gated channel alpha 1 at +40 mV
Drug: tetracaine
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 = 5.47
Action type: BLOCKER
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: tetracaine
Target: Sodium channel alpha subunits; brain (Types I, II, III) (Ion channel)
Gene: Scn1a|Scn2a|Scn3a
UniProt: P04774|P04775|P08104 (SCN1A_RAT|SCN2A_RAT|SCN3A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.22
Assay: Inhibition of [3H]batrachotoxin binding to rat brain neuronal membranes
Drug: tetracycline
Target: 30S ribosomal protein S4 (Ribosomal protein)
Gene: rpsD
UniProt: P0A7V8 (RS4_ECOLI)
Organism: Escherichia coli (strain K12)
Drug: tetracycline
Target: 30S ribosomal protein S9 (Ribosomal protein)
Gene: rpsI
UniProt: P0A7X3 (RS9_ECOLI)
Organism: Escherichia coli (strain K12)
Drug: sapropterin
Target: Nitric oxide synthase, brain (Enzyme)
Gene: NOS1
UniProt: P29475 (NOS1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.95
Assay: Activity of tetrahydrobiopterin free nNOS
Drug: sapropterin
Target: Phenylalanine-4-hydroxylase (Enzyme)
Gene: PAH
UniProt: P00439 (PH4H_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.4
Action type: ACTIVATOR
Assay: Binding affinity for human PAH.
Drug: tetroxoprim
Target: Dihydrofolate reductase (Enzyme)
Gene: folA
UniProt: P0ABQ4 (DYR_ECOLI)
Organism: Escherichia coli (strain K12)
Activity: Ki = 8.35
Drug: tetroxoprim
Target: Dihydrofolate reductase (Enzyme)
Gene: folA
UniProt: P00381 (DYR_LACCA)
Organism: Lactobacillus casei
Activity: Ki = 6.26
Assay: Inhibitory activity against Lactobacillus casei dihydrofolate reductase
Drug: tetroxoprim
Target: Dihydrofolate reductase (Enzyme)
Gene: dfrA17
UniProt: B0BL08 (B0BL08_ECOLX)
Organism: Escherichia coli
Activity: IC50 = 7.74
Assay: Inhibitory activity against Dihydrofolate reductase of Escherichia coli