AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: tacrine
Target: Cholinesterase (Enzyme)
Gene: BCHE
UniProt: P06276 (CHLE_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.301
Action type: INHIBITOR
Drug: tacrolimus
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Drug: tacrolimus
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Assay: DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin)
Drug: tacrolimus
Target: Interleukin-5 (Cytokine)
Gene: IL5
UniProt: P05113 (IL5_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 10.22
Drug: tacrolimus
Target: Interferon gamma (Cytokine)
Gene: IFNG
UniProt: P01579 (IFNG_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 10.22
Drug: tacrolimus
Target: Peptidyl-prolyl cis-trans isomerase FKBP1A (Enzyme)
Gene: FKBP1A
UniProt: P62942 (FKB1A_HUMAN)
Organism: Homo sapiens
Activity: Kd = 9.398
Action type: INHIBITOR
Drug: tacrolimus
Target: Interleukin-2 (Cytokine)
Gene: IL2
UniProt: P60568 (IL2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.72
Drug: tacrolimus
Target: Serine/threonine-protein phosphatase 2B catalytic subunit gamma isoform (Enzyme)
Gene: PPP3CC
UniProt: P48454 (PP2BC_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.456
Drug: tacrolimus
Target: Serine/threonine-protein kinase mTOR (Kinase)
Gene: MTOR
UniProt: P42345 (MTOR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.02
Assay: Inhibitory activity against macrophilin (FKBP-12)
Drug: tacrolimus
Target: Serine/threonine-protein phosphatase 2B catalytic subunit alpha isoform (Enzyme)
Gene: PPP3CA
UniProt: Q08209 (PP2BA_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.7
Assay: Binding affinity to protein phosphatase, calcineurin (CN) was determined
Drug: tacrolimus
Target: Peptidyl-prolyl cis-trans isomerase FKBP1B (Enzyme)
Gene: FKBP1B
UniProt: P68106 (FKB1B_HUMAN)
Organism: Homo sapiens
Activity: Kd = 9.4
Drug: tacrolimus
Target: Peptidyl-prolyl cis-trans isomerase FKBP5 (Enzyme)
Gene: FKBP5
UniProt: Q13451 (FKBP5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.1
Assay: Binding affinity to human FKBP51 by competitive fluorescence polarization assay
Drug: tacrolimus
Target: Splicing factor 3B subunit 3 (Nuclear other)
Gene: SF3B3
UniProt: Q15393 (SF3B3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.96
Assay: Inhibition of SAP130 mediated cell growth in human WiDr cells
Drug: tacrolimus
Target: Peptidyl-prolyl cis-trans isomerase FKBP10 (Enzyme)
Gene: FKBP10
UniProt: Q96AY3 (FKB10_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.02
Drug: tadalafil
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4
Assay: Inhibition of human ERG channel in HEK293 cells by voltage-clamp method
Drug: tadalafil
Target: cGMP-specific 3',5'-cyclic phosphodiesterase (Enzyme)
Gene: PDE5A
UniProt: O76074 (PDE5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8
Action type: INHIBITOR
Assay: Inhibition of human phosphodiesterase 5
Drug: tadalafil
Target: Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A (Enzyme)
Gene: PDE11A
UniProt: Q9HCR9 (PDE11_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.48
Assay: Inhibition of human phosphodiesterase 11
Drug: tadalafil
Target: Acetylcholinesterase (Enzyme)
Gene: Ache
UniProt: P37136 (ACES_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.58
Assay: Inhibition of AChE from rat cortex by Ellman's method
Drug: tadalafil
Target: cGMP-specific 3',5'-cyclic phosphodiesterase (Enzyme)
Gene: Pde5a
UniProt: O54735 (PDE5A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.3
Assay: Inhibition of phosphodiesterase 5 in rat fetal lung fibroblast (RFL-6) cells
Drug: tadalafil
Target: cGMP-specific 3',5'-cyclic phosphodiesterase (Enzyme)
Gene: PDE5A
UniProt: Q28156 (PDE5A_BOVIN)
Organism: Bos taurus
Activity: IC50 = 8.48
Assay: Inhibition of bovine PDE5 after 24 hrs by HTRF
Drug: tadalafil
Target: Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha (Enzyme)
Gene: PDE6A
UniProt: P11541 (PDE6A_BOVIN)
Organism: Bos taurus
Activity: IC50 = 5.52
Assay: Inhibition of bovine retina PDE6
Drug: tadalafil
Target: Phosphodiesterase 6 (Enzyme)
Gene: PDE6D|PDE6A|PDE6G|PDE6B|PDE6C|PDE6H
UniProt: O43924|P16499|P18545|P35913|P51160|Q13956 (PDE6D_HUMAN|PDE6A_HUMAN|CNRG_HUMAN|PDE6B_HUMAN|PDE6C_HUMAN|CNCG_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.01
Assay: Inhibition of human phosphodiesterase 6
Drug: tadalafil
Target: Phosphodiesterase 6 (Enzyme)
Gene: PDE6G|PDE6A|PDE6C|PDE6H|PDE6B|PDE6D
UniProt: P04972|P11541|P16586|P22571|P23439|Q95142 (CNRG_BOVIN|PDE6A_BOVIN|PDE6C_BOVIN|CNCG_BOVIN|PDE6B_BOVIN|PDE6D_BOVIN)
Organism: Bos taurus
Activity: IC50 = 5.29
Assay: Inhibition of bovine retina PDE6 (Phosphodiesterase 6)
Drug: talbutal
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: talinolol
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.62
Assay: Binding affinity to beta1 adrenergic receptor (unknown origin) by radioligand binding assay
Drug: talinolol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.05
Assay: Binding affinity to beta2 adrenergic receptor (unknown origin) by radioligand binding assay
Drug: talinolol
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Drug: talinolol
Target: Bifunctional epoxide hydrolase 2 (Enzyme)
Gene: EPHX2
UniProt: P34913 (HYES_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.55
Assay: Inhibition of recombinant human full length soluble epoxide hydrolase (1 to 555 residues) expressed in Escherichia coli BL21(DE3) using non-fluorescent PHOME as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by fluorescence based assay
Drug: talipexole
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.309
Drug: talipexole
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.915
Drug: talipexole
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.77
Drug: talipexole
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.69
Drug: talipexole
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.481
Drug: talipexole
Target: D(1B) dopamine receptor (GPCR)
Gene: DRD5
UniProt: P21918 (DRD5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.46
Drug: talipexole
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.695
Drug: talipexole
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.48
Drug: talipexole
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.9
Drug: talipexole
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.41
Drug: talipexole
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.24
Assay: In vitro binding affinity to rat striatal Dopamine receptor D2 was determined using the agonist [3H]quinpirole to label the high affinity state (D2 high)
Drug: talipexole
Target: Adrenergic receptor alpha-2 (GPCR)
Gene: Adra2b|Adra2c|Adra2a
UniProt: P19328|P22086|P22909 (ADA2B_RAT|ADA2C_RAT|ADA2A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.6
Assay: Binding affinity against Alpha-2 adrenergic receptor is the ability to inhibit the specific [3H]clonidine binding (0.4 nM) to rat isolated brain membranes by 50% was reported; 2.5*10e-8
Drug: taltirelin
Target: Thyrotropin-releasing hormone receptor (GPCR)
Gene: TRHR
UniProt: P34981 (TRFR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.5
Action type: AGONIST
Drug: tamoxifen
Target: Sodium/potassium-transporting ATPase subunit alpha-2 (Ion channel)
Gene: ATP1A2
UniProt: D2WKD8 (AT1A2_PIG)
Organism: Sus scrofa
Activity: IC50 = 4.807
Assay: DRUGMATRIX: ATPase, Na+/K+ enzyme inhibition (substrate: ATP)
Drug: tamoxifen
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.001
Assay: DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug: tamoxifen
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.46
Drug: tamoxifen
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.357
Assay: DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid)
Drug: tamoxifen
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.146
Assay: DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine)
Drug: tamoxifen
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.372
Assay: DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug: tamoxifen
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.335
Assay: DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
Drug: tamoxifen
Target: Adenosine receptor A2a (GPCR)
Gene: ADORA2A
UniProt: P29274 (AA2AR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.4
Assay: DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA)
Drug: tamoxifen
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.139
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: tamoxifen
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.5
Drug: tamoxifen
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.8
Assay: Inhibition of human ERG
Drug: tamoxifen
Target: 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase (Enzyme)
Gene: EBP
UniProt: Q15125 (EBP_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.301
Drug: tamoxifen
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7
Drug: tamoxifen
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.907
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: tamoxifen
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.836
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: tamoxifen
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.158
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
Drug: tamoxifen
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.863
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: tamoxifen
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.877
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: tamoxifen
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.618
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: tamoxifen
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.98
Assay: Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug: tamoxifen
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.794
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: tamoxifen
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.439
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: tamoxifen
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.034
Assay: DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug: tamoxifen
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.167
Assay: DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: tamoxifen
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.557
Assay: DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: tamoxifen
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.201
Assay: DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: tamoxifen
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.173
Assay: DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: tamoxifen
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.731
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: tamoxifen
Target: Aldehyde oxidase (Enzyme)
Gene: AOX1
UniProt: Q06278 (AOXA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.658
Drug: tamoxifen
Target: Beta-3 adrenergic receptor (GPCR)
Gene: ADRB3
UniProt: P13945 (ADRB3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.238
Assay: DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug: tamoxifen
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.835
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: tamoxifen
Target: Adenosine receptor A1 (GPCR)
Gene: ADORA1
UniProt: P30542 (AA1R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.858
Assay: DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX)
Drug: tamoxifen
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.679
Assay: DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
Drug: tamoxifen
Target: Nuclear receptor subfamily 1 group I member 2 (Nuclear hormone receptor)
Gene: NR1I2
UniProt: O75469 (NR1I2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.456
Drug: tamoxifen
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.407
Assay: DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug: tamoxifen
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.611
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: tamoxifen
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.204
Assay: DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine)
Drug: tamoxifen
Target: Estrogen receptor (Nuclear hormone receptor)
Gene: ESR1
UniProt: P03372 (ESR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.51
Action type: MODULATOR
Assay: Displacement of [2,4,6,7-3H]estradiol from human ERalpha expressed in HeLa cells after 18 hrs by liquid scintillation counting
Drug: tamoxifen
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.89
Drug: tamoxifen
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.328
Assay: DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole)
Drug: tamoxifen
Target: Estrogen receptor beta (Nuclear hormone receptor)
Gene: ESR2
UniProt: Q92731 (ESR2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.91
Drug: tamoxifen
Target: G-protein coupled estrogen receptor 1 (GPCR)
Gene: GPER1
UniProt: Q99527 (GPER1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.5
Drug: tamoxifen
Target: Estrogen-related receptor gamma (Nuclear hormone receptor)
Gene: ESRRG
UniProt: P62508 (ERR3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.1
Drug: tamoxifen
Target: Epidermal growth factor receptor (Kinase)
Gene: EGFR
UniProt: P00533 (EGFR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.449
Assay: DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: tamoxifen
Target: Substance-P receptor (GPCR)
Gene: TACR1
UniProt: P25103 (NK1R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.069
Assay: DRUGMATRIX: Tachykinin NK1 radioligand binding (ligand: [3H] Substance P)
Drug: tamoxifen
Target: Tyrosine-protein kinase Lck (Kinase)
Gene: LCK
UniProt: P06239 (LCK_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.095
Assay: DRUGMATRIX: Protein Tyrosine Kinase, LCK enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: tamoxifen
Target: Tyrosine-protein kinase Fyn (Kinase)
Gene: FYN
UniProt: P06241 (FYN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.923
Assay: DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: tamoxifen
Target: Receptor tyrosine-protein kinase erbB-2 (Kinase)
Gene: ERBB2
UniProt: P04626 (ERBB2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.53
Assay: DRUGMATRIX: Protein Tyrosine Kinase, ERBB2 (HER2) enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: tamoxifen
Target: Thromboxane-A synthase (Enzyme)
Gene: TBXAS1
UniProt: P24557 (THAS_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.038
Assay: DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2)
Drug: tamoxifen
Target: Steroid hormone receptor ERR1 (Nuclear hormone receptor)
Gene: ESRRA
UniProt: P11474 (ERR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.7
Assay: Antagonist activity at ERalpha receptor in human MCF7 cells assessed as inhibition of cell growth after 6 days by crystal violet staining method
Drug: tamoxifen
Target: Substance-K receptor (GPCR)
Gene: TACR2
UniProt: P21452 (NK2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.913
Assay: DRUGMATRIX: Tachykinin NK2  radioligand binding (ligand: [3H] SR-48968)
Drug: tamoxifen
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.821
Assay: DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
Drug: tamoxifen
Target: B2 bradykinin receptor (GPCR)
Gene: BDKRB2
UniProt: P30411 (BKRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.919
Assay: DRUGMATRIX: Bradykinin B2 radioligand binding (ligand: [3H] Bradykinin)
Drug: tamoxifen
Target: Melanocortin receptor 4 (GPCR)
Gene: MC4R
UniProt: P32245 (MC4R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.533
Assay: DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug: tamoxifen
Target: Melanocortin receptor 5 (GPCR)
Gene: MC5R
UniProt: P33032 (MC5R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.604
Assay: DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug: tamoxifen
Target: Melanocortin receptor 3 (GPCR)
Gene: MC3R
UniProt: P41968 (MC3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.761
Assay: DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug: tamoxifen
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.419
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: tamoxifen
Target: Serine/threonine-protein phosphatase 2B catalytic subunit alpha isoform (Enzyme)
Gene: PPP3CA
UniProt: Q08209 (PP2BA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.515
Assay: DRUGMATRIX: Protein Serine/Threonine Phosphatase, PPP3CA (Calcineurin, PP2B) enzyme inhibition (substrate: DiFMUP)
Drug: tamoxifen
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 5.587
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: tamoxifen
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.66
Drug: tamoxifen
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.92
Drug: tamoxifen
Target: C-8 sterol isomerase (Enzyme)
Gene: ERG2
UniProt: P32352 (ERG2_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: Ki = 5.82
Assay: Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand
Drug: tamoxifen
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.061
Drug: tamoxifen
Target: Emopamil-binding protein-like (Enzyme)
Gene: EBPL
UniProt: Q9BY08 (EBPL_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.55
Assay: Binding affinity to emopamil binding protein (unknown origin)
Drug: tamoxifen
Target: Anti-estrogen binding site (AEBS) (Enzyme)
Gene: EBP|DHCR7
UniProt: Q15125|Q9UBM7 (EBP_HUMAN|DHCR7_HUMAN)
Organism: Homo sapiens
Activity: Kd = 9
Assay: Binding affinity towards antiestrogen binding site AEBS
Drug: tamoxifen
Target: Transcriptional activator protein luxR (Unclassified)
Gene: luxR
UniProt: P12746 (LUXR_ALIFS)
Organism: Aliivibrio fischeri
Activity: IC50 = 4.4
Assay: Inhibition of LuxR-dependent quorum sensing in Vibrio fischeri assessed as reduction of 3-oxo-C6-HSL-induced bioluminescence intensity
Drug: tamsulosin
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.89
Assay: Binding affinity towards recombinant human Dopamine receptor D2L was determined using [3H]spiperone as radioligand
Drug: tamsulosin
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.87
Assay: Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand