AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: sertindole
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.57
Assay: Inhibition of human cloned ERG expressed in CHO cells assessed as inhibition of potassium channel current by automated patch clamp assay
Drug: sertindole
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.19
Assay: Inhibition of human ABCB1-mediated rhodamine 123 efflux in mouse L5178 cells expressing human MDR1 after 20 mins by FACS analysis
Drug: sertindole
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.48
Assay: Ability to displace [3H]5-CT (2.0 nM) from HeLa cells of human 5-hydroxytryptamine 1A receptor
Drug: sertindole
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.3
Assay: Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug: sertindole
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.553
Drug: sertindole
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.745
Drug: sertindole
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.347
Drug: sertindole
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.59
Assay: Ability to displace [3H]spiperone (0.3 nM) from CHO cells of human Dopamine receptor D3
Drug: sertindole
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.29
Assay: Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
Drug: sertindole
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.57
Drug: sertindole
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.25
Assay: Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
Drug: sertindole
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.2
Action type: ANTAGONIST
Drug: sertindole
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.347
Drug: sertindole
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.96
Assay: Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug: sertindole
Target: 5-hydroxytryptamine receptor 1F (GPCR)
Gene: HTR1F
UniProt: P30939 (5HT1F_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.4
Action type: ANTAGONIST
Drug: sertindole
Target: 5-hydroxytryptamine receptor 1E (GPCR)
Gene: HTR1E
UniProt: P28566 (5HT1E_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.4
Action type: ANTAGONIST
Drug: sertindole
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.47
Assay: Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes
Drug: sertindole
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: Adra1d
UniProt: P23944 (ADA1D_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.18
Assay: Displacement of [3H]prazosin (0.3 nM) from rat Alpha-1D adrenergic receptor expressed in CHO cells
Drug: sertindole
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.35
Assay: Displacement of [3H]spiperone (0.5 nM) from rat corpus striatum dopamine D2 receptor
Drug: sertindole
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: Htr2a
UniProt: P14842 (5HT2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.7
Assay: Displacement of [3H]ketanserin (0.5 nM) from rat cerebral cortex 5-hydroxytryptamine 2A receptors
Drug: sertindole
Target: D(1A) dopamine receptor (GPCR)
Gene: Drd1
UniProt: P18901 (DRD1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.92
Assay: Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
Drug: sertindole
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: Htr2c
UniProt: P08909 (5HT2C_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.29
Assay: Displacement of [3H]mesulergine (0.5 nM) from rat 5-hydroxytryptamine 2C receptor expressed in SR-3T3 cells
Drug: sertindole
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P18130 (ADA1A_BOVIN)
Organism: Bos taurus
Activity: Ki = 9.43
Assay: Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
Drug: sertindole
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P18841 (ADA1B_MESAU)
Organism: Mesocricetus auratus
Activity: Ki = 9.48
Assay: Displacement of [3H]prazosin (0.5 nM) from hamster Alpha-1B adrenergic receptor expressed in rat-1 cells
Drug: sertindole
Target: Adrenergic receptor alpha-1 (GPCR)
Gene: Adra1b|Adra1d|Adra1a
UniProt: P15823|P23944|P43140 (ADA1B_RAT|ADA1D_RAT|ADA1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.85
Assay: Ability to displace [3H]prazosin (0.25 nM) from whole brain of rat alpha-1 adrenergic receptor
Drug: sertindole
Target: Serotonin 2 (5-HT2) receptor (GPCR)
Gene: Htr2c|Htr2a|Htr2b
UniProt: P08909|P14842|P30994 (5HT2C_RAT|5HT2A_RAT|5HT2B_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 9.41
Assay: Displacement of [3H]ketanserin from 5-hydroxytryptamine 2 receptor from rat cortical membranes.
Drug: sertindole
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.35
Action type: ANTAGONIST
Assay: Displacement of [3H]prozosin from human cloned dopamine D2 receptor expressed in CHO cells
Drug: sertindole
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.22
Action type: ANTAGONIST
Assay: Binding affinity towards Serotonin 5-hydroxytryptamine 2A receptor
Drug: sertindole
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.7
Action type: INVERSE AGONIST
Assay: Displacement of [3H]prozosin from human cloned 5HT2C receptor expressed in CHO cells
Drug: sertraline
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.965
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: sertraline
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.24
Assay: Binding affinity to sigma 1 receptor
Drug: sertraline
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.167
Assay: DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole)
Drug: sertraline
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 9.54
Action type: INHIBITOR
Assay: Equilibrium dissociation constant (KD) for Competitive binding between [3H]- imipramine and the compound at human transporter-hSERT
Drug: sertraline
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.38
Drug: sertraline
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.106
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: sertraline
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.666
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: sertraline
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.246
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: sertraline
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.863
Drug: sertraline
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.082
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: sertraline
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.128
Drug: sertraline
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.678
Drug: sertraline
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.886
Drug: sertraline
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.854
Drug: sertraline
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.721
Drug: sertraline
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.187
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: sertraline
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.6
Drug: sertraline
Target: Cytochrome P450 2C19 (Enzyme)
Gene: CYP2C19
UniProt: P33261 (CP2CJ_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Assay: DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: sertraline
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.475
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: sertraline
Target: Melanocortin receptor 5 (GPCR)
Gene: MC5R
UniProt: P33032 (MC5R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.365
Assay: DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug: sertraline
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.885
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: sertraline
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: Slc6a4
UniProt: P31652 (SC6A4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.07
Assay: Inhibition the uptake of tritiated serotonin (5-HT) by the serotonin transporter SERT in rat synaptosomes
Drug: sertraline
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: Slc6a3
UniProt: P23977 (SC6A3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.11
Assay: Inhibition of the uptake of tritiated dopamine (DA) in rat synaptosomes
Drug: sertraline
Target: Transporter (Transporter)
Gene: Slc6a2
UniProt: Q9WTR4 (Q9WTR4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.8
Assay: Inhibition of uptake of tritiated norepinephrine (NE) in rat synaptosomes
Drug: sertraline
Target: Transcriptional activator protein luxR (Unclassified)
Gene: luxR
UniProt: P12746 (LUXR_ALIFS)
Organism: Aliivibrio fischeri
Activity: IC50 = 4.57
Assay: Inhibition of LuxR-dependent quorum sensing in Vibrio fischeri assessed as reduction of 3-oxo-C6-HSL-induced bioluminescence intensity
Drug: setastine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Assay: Mechanism of Action
Drug: sevoflurane
Target: Glycine receptor subunit alpha-1 (Ion channel)
Gene: GLRA1
UniProt: P23415 (GLRA1_HUMAN)
Organism: Homo sapiens
Action type: POSITIVE MODULATOR
Drug: sevoflurane
Target: Potassium channel subfamily K member 2 (Ion channel)
Gene: KCNK2
UniProt: O95069 (KCNK2_HUMAN)
Organism: Homo sapiens
Action type: OPENER
Assay: Mechanism of Action; CHEMBL2321615; SINGLE PROTEIN
Drug: sevoflurane
Target: Potassium channel subfamily K member 3 (Ion channel)
Gene: KCNK3
UniProt: O14649 (KCNK3_HUMAN)
Organism: Homo sapiens
Action type: OPENER
Assay: Mechanism of Action; CHEMBL2321613; SINGLE PROTEIN
Drug: sevoflurane
Target: Potassium channel subfamily K member 9 (Ion channel)
Gene: KCNK9
UniProt: Q9NPC2 (KCNK9_HUMAN)
Organism: Homo sapiens
Action type: OPENER
Assay: Mechanism of Action; CHEMBL2321614; SINGLE PROTEIN
Drug: sevoflurane
Target: Potassium channel subfamily K member 10 (Ion channel)
Gene: KCNK10
UniProt: P57789 (KCNKA_HUMAN)
Organism: Homo sapiens
Action type: OPENER
Assay: Mechanism of Action; CHEMBL2331041; SINGLE PROTEIN
Drug: sevoflurane
Target: Potassium channel subfamily K member 18 (Ion channel)
Gene: KCNK18
UniProt: Q7Z418 (KCNKI_HUMAN)
Organism: Homo sapiens
Action type: OPENER
Assay: Mechanism of Action; CHEMBL2331042; SINGLE PROTEIN
Drug: sevoflurane
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: sibutramine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.526
Action type: INHIBITOR
Drug: sibutramine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.263
Action type: INHIBITOR
Drug: sibutramine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.962
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: sibutramine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Drug: sibutramine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.026
Action type: INHIBITOR
Drug: sibutramine
Target: Potassium voltage-gated channel subfamily D member 3 (Ion channel)
Gene: KCND3
UniProt: Q9UK17 (KCND3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.7
Drug: sibutramine
Target: Cytochrome P450 2B6 (Enzyme)
Gene: CYP2B6
UniProt: P20813 (CP2B6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.79
Action type: INHIBITOR
Drug: sibutramine
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.538
Drug: sibutramine
Target: Potassium voltage-gated channel subfamily D member 3 (Ion channel)
Gene: Kcnd3
UniProt: Q62897 (KCND3_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.7
Action type: BLOCKER
Drug: sildenafil
Target: Adenosine receptor A2a (GPCR)
Gene: ADORA2A
UniProt: P29274 (AA2AR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.7
Assay: Displacement of [3H]ZM241385 from human AA2AR expressed in HEK293T cells after 2 hrs by liquid scintillation counter
Drug: sildenafil
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.48
Assay: Inhibition of human Potassium channel HERG expressed in mammalian cells
Drug: sildenafil
Target: Adenosine receptor A1 (GPCR)
Gene: ADORA1
UniProt: P30542 (AA1R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.06
Assay: DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX)
Drug: sildenafil
Target: Multidrug resistance-associated protein 5 (Transporter)
Gene: ABCC5
UniProt: O15440 (MRP5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.92
Assay: Inhibition of ABCC5 in human erythrocytes assessed as inhibition of ATP-mediated [3H]cGMP uptake in inside-out vesicles after 60 mins by liquid scintillation counting
Drug: sildenafil
Target: cGMP-specific 3',5'-cyclic phosphodiesterase (Enzyme)
Gene: PDE5A
UniProt: O76074 (PDE5A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9
Action type: INHIBITOR
Drug: sildenafil
Target: Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha (Enzyme)
Gene: PDE6A
UniProt: P16499 (PDE6A_HUMAN)
Organism: Homo sapiens
Drug: sildenafil
Target: Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A (Enzyme)
Gene: PDE11A
UniProt: Q9HCR9 (PDE11_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.64
Assay: Inhibition of human phosphodiesterase 11
Drug: sildenafil
Target: cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (Enzyme)
Gene: PDE10A
UniProt: Q9Y233 (PDE10_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.51
Assay: Inhibitory concentration against human phosphodiesterase 10
Drug: sildenafil
Target: cAMP-specific 3',5'-cyclic phosphodiesterase 4D (Enzyme)
Gene: PDE4D
UniProt: Q08499 (PDE4D_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.7
Assay: Inhibition of human PDE4D
Drug: sildenafil
Target: cGMP-dependent 3',5'-cyclic phosphodiesterase (Enzyme)
Gene: PDE2A
UniProt: O00408 (PDE2A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.2
Drug: sildenafil
Target: High affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7A (Enzyme)
Gene: PDE7A
UniProt: Q13946 (PDE7A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.33
Assay: Inhibition of human recombinant PDE7A1 at 1 uM by [3H]cGMP based tritium scintillation proximity assay
Drug: sildenafil
Target: Cone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha' (Enzyme)
Gene: PDE6C
UniProt: P51160 (PDE6C_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.41
Assay: Inhibition of human recombinant PDE6C at 1 uM by [3H]cGMP based tritium scintillation proximity assay
Drug: sildenafil
Target: High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A (Enzyme)
Gene: PDE9A
UniProt: O76083 (PDE9A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.47
Assay: Inhibition of Phosphodiesterase 9
Drug: sildenafil
Target: High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A (Enzyme)
Gene: PDE8A
UniProt: O60658 (PDE8A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4
Drug: sildenafil
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.094
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: sildenafil
Target: cGMP-specific 3',5'-cyclic phosphodiesterase (Enzyme)
Gene: Pde5a
UniProt: O54735 (PDE5A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.74
Assay: Inhibition of phosphodiesterase 5 in rat fetal lung fibroblast (RFL-6) cells
Drug: sildenafil
Target: Uncharacterized protein (Enzyme)
Gene: PDE3B
UniProt: E1BN64 (E1BN64_BOVIN)
Organism: Bos taurus
Activity: IC50 = 5.04
Assay: Inhibition of bovine aorta PDE3 (Phosphodiesterase 3)
Drug: sildenafil
Target: cGMP-specific 3',5'-cyclic phosphodiesterase (Enzyme)
Gene: PDE5A
UniProt: Q28156 (PDE5A_BOVIN)
Organism: Bos taurus
Activity: IC50 = 8.22
Assay: Inhibition of bovine aorta PDE5 (Phosphodiesterase 5)
Drug: sildenafil
Target: Cone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha' (Enzyme)
Gene: PDE6C
UniProt: P16586 (PDE6C_BOVIN)
Organism: Bos taurus
Activity: IC50 = 7.48
Assay: Inhibition of bovine cone PDE6
Drug: sildenafil
Target: Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha (Enzyme)
Gene: PDE6A
UniProt: P11541 (PDE6A_BOVIN)
Organism: Bos taurus
Activity: IC50 = 6.85
Assay: Inhibition of bovine retina PDE6
Drug: sildenafil
Target: Indoleamine 2,3-dioxygenase 2 (Enzyme)
Gene: Ido2
UniProt: Q8R0V5 (I23O2_MOUSE)
Organism: Mus musculus
Activity: IC50 = 5.35
Assay: Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
Drug: sildenafil
Target: cGMP-specific 3',5'-cyclic phosphodiesterase (Enzyme)
Gene: PDE5A
UniProt: O77746 (PDE5A_CANFA)
Organism: Canis familiaris
Activity: IC50 = 9
Assay: Inhibitory activity against phosphodiesterase 5 (PDE5) isolated from canine lung
Drug: sildenafil
Target: Phosphodiesterase 3 (Enzyme)
Gene: PDE3B|PDE3A
UniProt: Q13370|Q14432 (PDE3B_HUMAN|PDE3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.15
Assay: Inhibitory concentration against phosphodiesterase 3 from human platelet
Drug: sildenafil
Target: Phosphodiesterase 4 (Enzyme)
Gene: PDE4A|PDE4B|PDE4C|PDE4D
UniProt: P27815|Q07343|Q08493|Q08499 (PDE4A_HUMAN|PDE4B_HUMAN|PDE4C_HUMAN|PDE4D_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.11
Assay: Inhibition of human recombinant PDE4 (Phosphodiesterase 4)
Drug: sildenafil
Target: Phosphodiesterase 4 (Enzyme)
Gene: Pde4d|Pde4c|Pde4b|Pde4a
UniProt: P14270|P14644|P14646|P54748 (PDE4D_RAT|PDE4C_RAT|PDE4B_RAT|PDE4A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.34
Assay: Inhibitory concentration against phosphodiesterase 4 (PDE4) from rat kidney
Drug: sildenafil
Target: Phosphodiesterase 1 (Enzyme)
Gene: PDE1A|PDE1B|PDE1C
UniProt: P54750|Q01064|Q14123 (PDE1A_HUMAN|PDE1B_HUMAN|PDE1C_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.57
Assay: Inhibitory activity against phosphodiesterase-1 (PDE1) isolated from canine lung
Drug: sildenafil
Target: Phosphodiesterase 1 (Enzyme)
Gene: PDE1A|PDE1B
UniProt: P14100|Q01061 (PDE1A_BOVIN|PDE1B_BOVIN)
Organism: Bos taurus
Activity: IC50 = 6.4
Assay: Inhibition of Phosphodiesterase 1
Drug: sildenafil
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 = 7.7
Assay: Inhibition of phosphodiesterase 6 from bovine retina
Drug: sildenafil
Target: Phosphodiesterase 1 (Enzyme)
Gene: Pde1b|Pde1c|Pde1a
UniProt: Q01066|Q63421|Q9EPR9 (PDE1B_RAT|PDE1C_RAT|Q9EPR9_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.59
Assay: Inhibition of Phosphodiesterase 1 from rat liver
Drug: sildenafil
Target: Solute carrier organic anion transporter family member 1B3 (Transporter)
Gene: SLCO1B3
UniProt: Q9NPD5 (SO1B3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.1
Action type: INHIBITOR
Drug: sildenafil
Target: Phosphodiesterase 2A (Enzyme)
Gene: PDE2A
UniProt: P14099 (PDE2A_BOVIN)
Organism: Bos taurus
Activity: IC50 = 4.37
Assay: Inhibitory activity against phosphodiesterase-2 (PDE2) isolated from bovine adrenal gland
Drug: silymarin
Target: Urokinase-type plasminogen activator (Enzyme)
Gene: PLAU
UniProt: P00749 (UROK_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.68
Assay: Inhibition of urokinase amidolytic activity (unknown origin)
Drug: silymarin
Target: Carbonic anhydrase 2 (Enzyme)
Gene: CA2
UniProt: P00918 (CAH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.6
Assay: Inhibition of human carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration method
Drug: silymarin
Target: Carbonic anhydrase 1 (Enzyme)
Gene: CA1
UniProt: P00915 (CAH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.83
Assay: Inhibition of human carbonic anhydrase 1 after 15 mins by stopped flow CO2 hydration method
Drug: silymarin
Target: Carbonic anhydrase 4 (Enzyme)
Gene: CA4
UniProt: P22748 (CAH4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.05
Assay: Inhibition of human carbonic anhydrase 4 after 15 mins by stopped flow CO2 hydration method