AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: flumazenil
Target: GABA-A receptor; alpha-1/beta-2/gamma-2 (Ion channel)
Gene: Gabrg2|Gabra1|Gabrb2
UniProt: P18508|P62813|P63138 (GBRG2_RAT|GBRA1_RAT|GBRB2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.3
Assay: Binding affinity for rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells
Drug: flumazenil
Target: GABA-A receptor alpha-6/beta-3/gamma-2 (Ion channel)
Gene: GABRG2|GABRB3|GABRA6
UniProt: P18507|P28472|Q16445 (GBRG2_HUMAN|GBRB3_HUMAN|GBRA6_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.83
Action type: ALLOSTERIC ANTAGONIST
Drug: flumazenil
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
Activity: Ki = 9.05
Assay: Displacement of [3H]flumazenil from bovine benzodiazepine receptor GABA-A channel of brain membranes
Drug: flumetasone pivalate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Drug: flunarizine
Target: Cannabinoid receptor 1 (GPCR)
Gene: CNR1
UniProt: P21554 (CNR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.621
Assay: DRUGMATRIX: Cannabinoid CB1 radioligand binding (ligand: [3H] SR141716A)
Drug: flunarizine
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.62
Assay: Binding affinity against mu opioid receptor using [3H]DAMGO
Drug: flunarizine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.713
Assay: DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug: flunarizine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.932
Assay: DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
Drug: flunarizine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.662
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: flunarizine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: flunarizine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.304
Assay: DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole)
Drug: flunarizine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.577
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: flunarizine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.877
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: flunarizine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.612
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
Drug: flunarizine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.936
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: flunarizine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.16
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: flunarizine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.455
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: flunarizine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.063
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: flunarizine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.481
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: flunarizine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.745
Assay: DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug: flunarizine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.151
Assay: DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: flunarizine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.504
Assay: DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: flunarizine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.103
Assay: DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: flunarizine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.1
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: flunarizine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.495
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: flunarizine
Target: Sodium channel protein type 1 subunit alpha (Ion channel)
Gene: SCN1A
UniProt: P35498 (SCN1A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.2
Drug: flunarizine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.333
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: flunarizine
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.532
Assay: DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
Drug: flunarizine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.357
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: flunarizine
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.02
Assay: Binding affinity against opioid receptor kappa 1 by using [3H]U-69593 as radioligand
Drug: flunarizine
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.44
Assay: Binding affinity against delta opiate receptor using [3H]DPDPE
Drug: flunarizine
Target: Voltage-dependent N-type calcium channel subunit alpha-1B (Ion channel)
Gene: CACNA1B
UniProt: Q00975 (CAC1B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.78
Assay: Inhibition of calcium channel Cav2.2 in IMR32 cells
Drug: flunarizine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.218
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: flunarizine
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.42
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: flunarizine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.96
Drug: flunarizine
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.64
Assay: Inhibition of [3H]raclopride binding to Dopamine receptor D2 of rat striatum membranes
Drug: flunarizine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.37
Drug: flunarizine
Target: Sodium channel protein type 2 subunit alpha (Ion channel)
Gene: Scn2a
UniProt: P04775 (SCN2A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.31
Assay: Inhibitory activity against type IIA sodium channel in CNaIIA-1 cell line expressed in CHO cells
Drug: flunarizine
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: Ki = 7.28
Assay: Inhibition of [3H]- batrachotoxin binding to sodium channel in rat neocortical membrane
Drug: flunarizine
Target: CAAX prenyl protease 2 (Enzyme)
Gene: RCE1
UniProt: Q9Y256 (FACE2_HUMAN)
Organism: Homo sapiens
Activity: AC50 = 4.15
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: flunarizine
Target: CAAX prenyl protease 2 (Enzyme)
Gene: RCE1
UniProt: Q03530 (RCE1_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: AC50 = 5.46
Assay: Active
Drug: flunarizine
Target: Potassium channel subfamily K member 2 (Ion channel)
Gene: Kcnk2
UniProt: Q8HY88 (Q8HY88_BOVIN)
Organism: Bos taurus
Activity: IC50 = 5.6
Assay: Activation of bovine TREK1 expressed in AZT cells assessed as reduction in channel currents
Drug: flunarizine
Target: Voltage-dependent T-type calcium channel subunit alpha-1G (Ion channel)
Gene: CACNA1G
UniProt: O43497 (CAC1G_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.28
Action type: BLOCKER
Assay: Inhibition of T-type Cav3.1 channel
Drug: flunarizine
Target: Voltage-dependent T-type calcium channel subunit alpha-1H (Ion channel)
Gene: CACNA1H
UniProt: O95180 (CAC1H_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.44
Action type: BLOCKER
Assay: Inhibition of T-type Cav3.2 channel
Drug: flunarizine
Target: Voltage-dependent T-type calcium channel subunit alpha-1I (Ion channel)
Gene: CACNA1I
UniProt: Q9P0X4 (CAC1I_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.08
Action type: BLOCKER
Assay: Inhibition of T-type Cav3.3 channel
Drug: flunisolide
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 9.1
Action type: AGONIST
Drug: flunisolide
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 7.328
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: flunitrazepam
Target: Gamma-aminobutyric acid receptor subunit alpha-1 (Ion channel)
Gene: GABRA1
UniProt: P14867 (GBRA1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.28
Action type: ALLOSTERIC MODULATOR
Assay: Assay using recombinant GABA<sub>A</sub> channels with subunit composition; &alpha;1&beta;3&gamma;2.
Drug: flunitrazepam
Target: Gamma-aminobutyric acid receptor subunit alpha-2 (Ion channel)
Gene: GABRA2
UniProt: P47869 (GBRA2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.28
Action type: ALLOSTERIC MODULATOR
Assay: Assay using recombinant GABA<sub>A</sub> channels with subunit composition; &alpha;2&beta;1&gamma;2.
Drug: flunitrazepam
Target: Gamma-aminobutyric acid receptor subunit alpha-3 (Ion channel)
Gene: GABRA3
UniProt: P34903 (GBRA3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.8
Action type: ALLOSTERIC MODULATOR
Assay: Assay using recombinant GABA<sub>A</sub> channels with subunit composition; &alpha;3&beta;1&gamma;2.
Drug: flunitrazepam
Target: Gamma-aminobutyric acid receptor subunit alpha-5 (Ion channel)
Gene: GABRA5
UniProt: P31644 (GBRA5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.26
Action type: ALLOSTERIC MODULATOR
Assay: Assay using recombinant GABA<sub>A</sub> channels with subunit composition; &alpha;5&beta;1&gamma;2.
Drug: flunitrazepam
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: Ki = 8.699
Drug: flunitrazepam
Target: GABA-A receptor alpha-2/beta-3/gamma-2 (Ion channel)
Gene: GABRG2|GABRB3|GABRA2
UniProt: P18507|P28472|P47869 (GBRG2_HUMAN|GBRB3_HUMAN|GBRA2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.699
Drug: flunitrazepam
Target: GABA-A receptor alpha-3/beta-3/gamma-2 (Ion channel)
Gene: GABRG2|GABRB3|GABRA3
UniProt: P18507|P28472|P34903 (GBRG2_HUMAN|GBRB3_HUMAN|GBRA3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.347
Drug: flunitrazepam
Target: GABA-A receptor alpha-5/beta-3/gamma-2 (Ion channel)
Gene: GABRG2|GABRB3|GABRA5
UniProt: P18507|P28472|P31644 (GBRG2_HUMAN|GBRB3_HUMAN|GBRA5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.84
Drug: flunitrazepam
Target: GABA-A receptor alpha-1/beta-2/gamma-3 (Ion channel)
Gene: GABRA1|GABRB2|GABRG3
UniProt: P14867|P47870|Q99928 (GBRA1_HUMAN|GBRB2_HUMAN|GBRG3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.457
Drug: flunitrazepam
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: Ki = 8.47
Drug: flunitrazepam
Target: GABA-A receptor; anion channel (Ion channel)
Gene: Gabrp|Gabrb1|Gabrd|Gabrg2|Gabra5|Gabra3|Gabrg1|Gabra2|Gabra4|Gabrg3|Gabra6|Gabra1|Gabrb3|Gabrb2|Gabrq|Gabre
UniProt: O09028|P15431|P18506|P18508|P19969|P20236|P23574|P23576|P28471|P28473|P30191|P62813|P63079|P63138|Q91ZM7|Q9ES14 (GBRP_RAT|GBRB1_RAT|GBRD_RAT|GBRG2_RAT|GBRA5_RAT|GBRA3_RAT|GBRG1_RAT|GBRA2_RAT|GBRA4_RAT|GBRG3_RAT|GBRA6_RAT|GBRA1_RAT|GBRB3_RAT|GBRB2_RAT|Q91ZM7_RAT|GBRE_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.82
Assay: Displacement of [3H]diazepam from GABA-A Benzodiazepine receptor of rat forebrain
Drug: flunitrazepam
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: Ki = 8.824
Drug: flunitrazepam
Target: GABA A receptor alpha-3/beta-2/gamma-3 (Ion channel)
Gene: GABRA3|GABRB2|GABRG3
UniProt: P34903|P47870|Q99928 (GBRA3_HUMAN|GBRB2_HUMAN|GBRG3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.5
Drug: flunitrazepam
Target: GABA A receptor alpha-5/beta-3/gamma-3 (Ion channel)
Gene: GABRB3|GABRA5|GABRG3
UniProt: P28472|P31644|Q99928 (GBRB3_HUMAN|GBRA5_HUMAN|GBRG3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.42
Drug: flunitrazepam
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: Ki = 9
Drug: flunitrazepam
Target: GABA A receptor alpha-5/beta-2/gamma-3 (Ion channel)
Gene: GABRA5|GABRB2|GABRG3
UniProt: P31644|P47870|Q99928 (GBRA5_HUMAN|GBRB2_HUMAN|GBRG3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.42
Drug: fluocinolone acetonide
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.848
Action type: AGONIST
Assay: DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
Drug: fluocinolone acetonide
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 8.475
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: fluocinonide
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.622
Action type: AGONIST
Assay: DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
Drug: fluocinonide
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 8.538
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: fluorescein
Target: Cytochrome P450 2C19 (Enzyme)
Gene: CYP2C19
UniProt: P33261 (CP2CJ_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.042
Assay: DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: fluorescein
Target: Protein arginine N-methyltransferase 1 (Enzyme)
Gene: PRMT1
UniProt: Q99873 (ANM1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.12
Assay: Inhibition of human recombinant GST-PRMT1 expressed in BL21 cells
Drug: fluorescein
Target: Solute carrier family 22 member 6 (Transporter)
Gene: Slc22a6
UniProt: Q8VC69 (S22A6_MOUSE)
Organism: Mus musculus
Activity: Ki = 5.53
Assay: Inhibition of mouse Oat1-mediated [3H]PAH uptake in Xenopus oocytes after 1 hr
Drug: fluorescein
Target: Solute carrier family 22 member 20 (Transporter)
Gene: Slc22a20
UniProt: Q80UJ1 (S22AK_MOUSE)
Organism: Mus musculus
Activity: Ki = 4
Assay: Inhibition of mouse Oat6-mediated [3H]ES uptake in Xenopus oocytes after 1 hr
Drug: fluorometholone
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.801
Action type: AGONIST
Assay: DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
Drug: fluorometholone
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.067
Assay: DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
Drug: fluorometholone
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 6.975
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: fluoxetine
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.356
Drug: fluoxetine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.2
Drug: fluoxetine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.07
Assay: The compound was tested for affinity towards sigma-3 receptor
Drug: fluoxetine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.155
Drug: fluoxetine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 9.091
Action type: INHIBITOR
Drug: fluoxetine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.62
Drug: fluoxetine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.61
Drug: fluoxetine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.3
Action type: ANTAGONIST
Drug: fluoxetine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.4
Drug: fluoxetine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.11
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: fluoxetine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.699
Drug: fluoxetine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.156
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: fluoxetine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.699
Drug: fluoxetine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.959
Drug: fluoxetine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.047
Drug: fluoxetine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.569
Drug: fluoxetine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6
Drug: fluoxetine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.538
Drug: fluoxetine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.569
Drug: fluoxetine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.444
Drug: fluoxetine
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.155
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: fluoxetine
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P22303 (ACES_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.89
Assay: Inhibition of AChE
Drug: fluoxetine
Target: Potassium channel subfamily K member 2 (Ion channel)
Gene: KCNK2
UniProt: O95069 (KCNK2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.85
Assay: Inhibition of of human TREK1 expressed in HEK293 cells assessed as reduction in channel currents
Drug: fluoxetine
Target: Histamine H3 receptor (GPCR)
Gene: HRH3
UniProt: Q9Y5N1 (HRH3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.14
Assay: Binding affinity to human histamine H3 receptor
Drug: fluoxetine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: Slc6a4
UniProt: P31652 (SC6A4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.7
Assay: Displacement of [3H]citalopram from serotonin transporter in Sprague-Dawley rat brain after 1 hr by liquid scintillation counting
Drug: fluoxetine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: Slc6a3
UniProt: P23977 (SC6A3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.11
Assay: Displacement of [3H]WIN 35428 from dopamine transporter in Sprague-Dawley rat brain after 1 hr by liquid scintillation counting
Drug: fluoxetine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: Htr2a
UniProt: P14842 (5HT2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.5
Action type: ANTAGONIST
Drug: fluoxetine
Target: Transporter (Transporter)
Gene: Slc6a2
UniProt: Q9WTR4 (Q9WTR4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.84
Assay: Inhibition of [3H]- NE reuptake into rat hippocampal synaptosomes
Drug: fluoxetine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: Slc6a3
UniProt: Q61327 (SC6A3_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.97
Assay: Tested in vitro for serotonin(5-HT) neuronal uptake inhibition
Drug: fluoxetine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: Slc6a2
UniProt: O55192 (SC6A2_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.07
Assay: Tested in vitro for norepinephrine (NE) neuronal uptake inhibition