AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: vardenafil
Target: High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A (Enzyme)
Gene: PDE9A
UniProt: O76083 (PDE9A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.34
Assay: Inhibition of Phosphodiesterase 9
Drug: vardenafil
Target: Phosphodiesterase 3 (Enzyme)
Gene: PDE3B|PDE3A
UniProt: Q13370|Q14432 (PDE3B_HUMAN|PDE3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.68
Assay: Inhibition of human phosphodiesterase 3
Drug: vardenafil
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 = 5.35
Assay: Inhibition of human phosphodiesterase 4
Drug: vardenafil
Target: Phosphodiesterase 1 (Enzyme)
Gene: PDE1A|PDE1B
UniProt: P14100|Q01061 (PDE1A_BOVIN|PDE1B_BOVIN)
Organism: Bos taurus
Activity: IC50 = 6.74
Assay: Inhibition of Phosphodiesterase 1
Drug: vasopressin
Target: Vasopressin V1a receptor (GPCR)
Gene: AVPR1A
UniProt: P37288 (V1AR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.59
Action type: AGONIST
Assay: Inhibition of human vasopressin V1a receptor expressed in CHO cells by polarisation binding assay using 96-well plate membranes
Drug: vasopressin
Target: Vasopressin V1b receptor (GPCR)
Gene: AVPR1B
UniProt: P47901 (V1BR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.31
Action type: AGONIST
Assay: Displacement of [3H]-AVP from human vasopressin V1b receptor expressed in CHO cells after 30 mins
Drug: vasopressin
Target: Vasopressin V2 receptor (GPCR)
Gene: AVPR2
UniProt: P30518 (V2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.92
Action type: AGONIST
Assay: Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
Drug: vasopressin
Target: Oxytocin receptor (GPCR)
Gene: OXTR
UniProt: P30559 (OXYR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.78
Assay: Displacement of [3H]-AVP from human oxytocin receptor expressed in CHO cells after 30 mins
Drug: vasopressin
Target: Vasopressin V2 receptor (GPCR)
Gene: AVPR2
UniProt: P32307 (V2R_PIG)
Organism: Sus scrofa
Activity: IC50 = 8.48
Assay: Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
Drug: vasopressin
Target: Oxytocin receptor (GPCR)
Gene: Oxtr
UniProt: P70536 (OXYR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.93
Assay: Displacement of [3H]AVP from rat OT receptor expressed in CHO cells
Drug: vasopressin
Target: Vasopressin V2 receptor (GPCR)
Gene: Avpr2
UniProt: Q00788 (V2R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.35
Assay: Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
Drug: vasopressin
Target: Vasopressin V2 receptor (GPCR)
Gene: AVPR2
UniProt: P48044 (V2R_BOVIN)
Organism: Bos taurus
Activity: Kd = 8.82
Assay: Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
Drug: vasopressin
Target: Vasopressin V1a receptor (GPCR)
Gene: Avpr1a
UniProt: P30560 (V1AR_RAT)
Organism: Rattus norvegicus
Activity: Kd = 9.19
Assay: Binding potency against V1 receptor in rat liver cells
Drug: vasopressin
Target: Vasopressin V1b receptor (GPCR)
Gene: Avpr1b
UniProt: P48974 (V1BR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.54
Assay: Displacement of [3H]AVP from rat vasopressin V1b receptor expressed in At-T20 cells
Drug: vasopressin
Target: Vasopressin V1 receptor (GPCR)
Gene: Avpr1a|Avpr1b
UniProt: P30560|P48974 (V1AR_RAT|V1BR_RAT)
Organism: Rattus norvegicus
Activity: Kd = 9.19
Assay: Compound was evaluated for its dissociation constant (Kd) to rat liver Vasopressin V1 receptor
Drug: vecuronium
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.46
Assay: Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Drug: vecuronium
Target: Multidrug and toxin extrusion protein 1 (Transporter)
Gene: SLC47A1
UniProt: Q96FL8 (S47A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.72
Assay: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Drug: vecuronium
Target: Multidrug and toxin extrusion protein 2 (Transporter)
Gene: SLC47A2
UniProt: Q86VL8 (S47A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.6
Assay: Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Drug: vecuronium
Target: Neuronal acetylcholine receptor; alpha2/beta4 (Ion channel)
Gene: CHRNB4|CHRNA2
UniProt: P30926|Q15822 (ACHB4_HUMAN|ACHA2_HUMAN)
Organism: Homo sapiens
Drug: vecuronium
Target: Acetylcholine receptor (Ion channel)
Gene: CHRNA1|CHRNB1|CHRND
UniProt: P02708|P11230|Q07001 (ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.824
Action type: ANTAGONIST
Drug: vecuronium
Target: Neuronal acetylcholine receptor; alpha4/beta2 (Ion channel)
Gene: CHRNB2|CHRNA4
UniProt: P17787|P43681 (ACHB2_HUMAN|ACHA4_HUMAN)
Organism: Homo sapiens
Drug: vecuronium
Target: Neuronal acetylcholine receptor; alpha4/beta4 (Ion channel)
Gene: CHRNB4|CHRNA4
UniProt: P30926|P43681 (ACHB4_HUMAN|ACHA4_HUMAN)
Organism: Homo sapiens
Drug: vecuronium
Target: Acetylcholine receptor; alpha1/beta1/delta/gamma (Ion channel)
Gene: CHRNA1|CHRNG|CHRNB1|CHRND
UniProt: P02708|P07510|P11230|Q07001 (ACHA_HUMAN|ACHG_HUMAN|ACHB_HUMAN|ACHD_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.09
Assay: GRAC: human AChR-alpha1 commonly used antagonist
Drug: venlafaxine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.051
Action type: INHIBITOR
Drug: venlafaxine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.975
Action type: INHIBITOR
Drug: venlafaxine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.652
Drug: venlafaxine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.698
Drug: venlafaxine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.554
Drug: venlafaxine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.44
Assay: Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay
Drug: venlafaxine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.05
Assay: Inhibition of binding of [3H]imipramine to imipramine receptor in rat brain
Drug: venlafaxine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: Slc6a4
UniProt: P31652 (SC6A4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.6
Assay: Displacement of [3H]-citalopram from Sprague-Dawley rat brain SERT after 1 hr
Drug: venlafaxine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: Slc6a3
UniProt: P23977 (SC6A3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.44
Assay: Inhibition of [3H]- DA reuptake into rat striatal synaptosomes
Drug: venlafaxine
Target: Transporter (Transporter)
Gene: Slc6a2
UniProt: Q9WTR4 (Q9WTR4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.86
Assay: Inhibition of [3H]- NE reuptake into rat hippocampal synaptosomes
Drug: venlafaxine
Target: Transporter (Transporter)
Gene: NET
UniProt: Q63380 (Q63380_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.19
Assay: Inhibition of norepinephrine uptake at rat brain norepinephrine transporter
Drug: verapamil
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Drug: verapamil
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.664
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: verapamil
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8
Assay: Inhibition of human ERG
Drug: verapamil
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.22
Action type: INHIBITOR
Assay: Inhibition of testosterone 6&beta;-hydroxylation.
Drug: verapamil
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.52
Assay: High affinity constant at binding site of human P-Glycoprotein (P-gp) in two-affinity model
Drug: verapamil
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.896
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: verapamil
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.763
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
Drug: verapamil
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.854
Drug: verapamil
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.979
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: verapamil
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.81
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: verapamil
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.201
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: verapamil
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.594
Assay: DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug: verapamil
Target: Aldehyde oxidase (Enzyme)
Gene: AOX1
UniProt: Q06278 (AOXA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.456
Drug: verapamil
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.072
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: verapamil
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: CACNA1C
UniProt: Q13936 (CAC1C_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Action type: BLOCKER
Drug: verapamil
Target: Multidrug resistance-associated protein 1 (Transporter)
Gene: ABCC1
UniProt: P33527 (MRP1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.88
Assay: Inhibition of MRP1 in human 2008/MRP1 cells by Lineweaver-Burke plot analysis
Drug: verapamil
Target: ATP-binding cassette sub-family G member 2 (Transporter)
Gene: ABCG2
UniProt: Q9UNQ0 (ABCG2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.43
Drug: verapamil
Target: Carbonic anhydrase 1 (Enzyme)
Gene: CA1
UniProt: P00915 (CAH1_HUMAN)
Organism: Homo sapiens
Drug: verapamil
Target: G protein-activated inward rectifier potassium channel 2 (Ion channel)
Gene: KCNJ6
UniProt: P48051 (KCNJ6_HUMAN)
Organism: Homo sapiens
Drug: verapamil
Target: Voltage-dependent T-type calcium channel subunit alpha-1H (Ion channel)
Gene: CACNA1H
UniProt: O95180 (CAC1H_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.485
Action type: BLOCKER
Drug: verapamil
Target: Voltage-dependent L-type calcium channel subunit alpha-1S (Ion channel)
Gene: CACNA1S
UniProt: Q13698 (CAC1S_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: verapamil
Target: Potassium voltage-gated channel subfamily A member 10 (Ion channel)
Gene: KCNA10
UniProt: Q16322 (KCA10_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.3
Action type: BLOCKER
Drug: verapamil
Target: Potassium voltage-gated channel subfamily A member 3 (Ion channel)
Gene: KCNA3
UniProt: P22001 (KCNA3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.1
Assay: Inhibition of Kv1.3 expressed in mouse L929 cells exposed to depolarizing step pulses from -80 mV to +40 mV by whole cell patch clamp method
Drug: verapamil
Target: Potassium voltage-gated channel subfamily C member 2 (Ion channel)
Gene: KCNC2
UniProt: Q96PR1 (KCNC2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.9
Drug: verapamil
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.17
Assay: Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Drug: verapamil
Target: Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (Ion channel)
Gene: HCN4
UniProt: Q9Y3Q4 (HCN4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.348
Drug: verapamil
Target: Potassium voltage-gated channel subfamily A member 7 (Ion channel)
Gene: KCNA7
UniProt: Q96RP8 (KCNA7_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.8
Drug: verapamil
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.027
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: verapamil
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.76
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: verapamil
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.68
Drug: verapamil
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.52
Drug: verapamil
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: CACNA1C
UniProt: P15381 (CAC1C_RABIT)
Organism: Oryctolagus cuniculus
Activity: IC50 = 6
Assay: Inhibition of [3H]nitrendipine binding to calcium channels in Rabbit cardiac muscle.
Drug: verapamil
Target: Translocator protein (Membrane receptor)
Gene: Tspo
UniProt: P16257 (TSPO_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.85
Assay: Ability to inhibit [3H]-PK 11195 binding to peripheral-type benzodiazepine receptor(PBR) in rat cerebral cortex homogenate.
Drug: verapamil
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: Cacna1c
UniProt: P22002 (CAC1C_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.41
Assay: Ability to inhibit [3H]nitrendipine binding to the L-type calcium channel receptor(CCR) in rat heart homogenate.
Drug: verapamil
Target: Voltage-dependent L-type calcium channel subunit alpha-1S (Ion channel)
Gene: Cacna1s
UniProt: Q02485 (CAC1S_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.24
Assay: Inhibition of [3H]D-888 binding to L-type [Ca2+] channel of membranes from rat skeletal muscle
Drug: verapamil
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P06199 (ACM2_PIG)
Organism: Sus scrofa
Activity: EC50 = 4.51
Drug: verapamil
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.071
Drug: verapamil
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 = 5.48
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: verapamil
Target: Voltage-gated L-type calcium channel (Ion channel)
Gene: Cacna1c|Cacna1d|Cacna1s
UniProt: P22002|P27732|Q02485 (CAC1C_RAT|CAC1D_RAT|CAC1S_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.43
Assay: Ability to inhibit [3H]nitrendipine binding to the calcium channel receptor(CCR) in rat cerebral cortex homogenate.
Drug: verapamil
Target: Equilibrative nucleoside transporter 4 (Transporter)
Gene: SLC29A4
UniProt: Q7RTT9 (S29A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.73
Action type: INHIBITOR
Drug: verapamil
Target: Chloroquine resistance transporter (Transporter)
Gene: CRT
UniProt: Q9N623 (CRT_PLAFA)
Organism: Plasmodium falciparum
Activity: IC50 = 4.52
Assay: Inhibition of chloroquine-resistant Plasmodium falciparum Dd2 CRT expressed in Xenopus laevis oocyte assessed as inhibition of [3H]chloroquine uptake measured from 1 to 2 hrs
Drug: verapamil
Target: Potassium voltage-gated channel subfamily C member 2 (Ion channel)
Gene: Kcnc2
UniProt: P22462 (KCNC2_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 4.9
Action type: BLOCKER
Drug: verapamil
Target: Two pore calcium channel protein 1 (Ion channel)
Gene: TPCN1
UniProt: Q9ULQ1 (TPC1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.64
Action type: BLOCKER
Drug: verapamil
Target: Two pore calcium channel protein 2 (Ion channel)
Gene: TPCN2
UniProt: Q8NHX9 (TPC2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5
Action type: BLOCKER
Drug: vesnarinone
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.96
Assay: Inhibition of human Potassium channel HERG expressed in mammalian cells
Drug: vesnarinone
Target: cGMP-inhibited 3',5'-cyclic phosphodiesterase A (Enzyme)
Gene: PDE3A
UniProt: Q14432 (PDE3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.97
Assay: Inhibition of human PDE3A by fluorescence microplate reader
Drug: vesnarinone
Target: cGMP-inhibited 3',5'-cyclic phosphodiesterase B (Enzyme)
Gene: PDE3B
UniProt: Q13370 (PDE3B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.88
Assay: Inhibition of human PDE3B by fluorescence microplate reader
Drug: vesnarinone
Target: Phosphodiesterase 3 (Enzyme)
Gene: PDE3B|PDE3A
UniProt: Q13370|Q14432 (PDE3B_HUMAN|PDE3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.21
Assay: In vivo inhibition of cyclic AMP phosphodiesterase from human platelets
Drug: vesnarinone
Target: Transitional endoplasmic reticulum ATPase (Enzyme)
Gene: VCP
UniProt: P55072 (TERA_HUMAN)
Organism: Homo sapiens
Assay: Vesnarinone binds to the D1 domain of VCP
Drug: vidarabine
Target: DNA polymerase catalytic subunit (Enzyme)
UniProt: P04293 (DPOL_HHV11)
Organism: Human herpesvirus 1 (strain 17)
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL1872; SINGLE PROTEIN
Drug: vidarabine
Target: Deoxycytidine kinase (Kinase)
Gene: DCK
UniProt: P27707 (DCK_HUMAN)
Organism: Homo sapiens
Drug: vidarabine
Target: DNA polymerase alpha catalytic subunit (Enzyme)
Gene: POLA1
UniProt: P09884 (DPOLA_HUMAN)
Organism: Homo sapiens
Drug: vidarabine
Target: Ribonucleoside-diphosphate reductase large subunit (Enzyme)
Gene: RRM1
UniProt: P23921 (RIR1_HUMAN)
Organism: Homo sapiens
Drug: vidarabine
Target: Ribonucleoside-diphosphate reductase subunit M2 (Enzyme)
Gene: RRM2
UniProt: P31350 (RIR2_HUMAN)
Organism: Homo sapiens
Drug: vidarabine
Target: Deoxyguanosine kinase, mitochondrial (Kinase)
Gene: DGUOK
UniProt: Q16854 (DGUOK_HUMAN)
Organism: Homo sapiens
Drug: vidarabine
Target: Ribose-phosphate pyrophosphokinase 1 (Kinase)
Gene: PRPS1
UniProt: P60891 (PRPS1_HUMAN)
Organism: Homo sapiens
Drug: vidarabine
Target: Dipeptidyl peptidase 4 (Enzyme)
Gene: DPP4
UniProt: P27487 (DPP4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.21
Assay: Inhibition of human DPP4 from human Caco-2 cells
Drug: vidarabine
Target: Adenylate cyclase type V (Enzyme)
Gene: Adcy5
UniProt: Q04400 (ADCY5_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.09
Assay: Compound was evaluated for inhibition of adenylate cyclase from rat brain
Drug: vidarabine
Target: Adenosylhomocysteinase  (Enzyme)
Gene: Ahcy
UniProt: P50247 (SAHH_MOUSE)
Organism: Mus musculus
Activity: Ki = 4.52
Assay: Activity determined in mouse liver S-adenosyl-L-homocysteine hydrolase and expressed as KI values.
Drug: vigabatrin
Target: 4-aminobutyrate aminotransferase, mitochondrial (Enzyme)
Gene: ABAT
UniProt: P80404 (GABT_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2044; SINGLE PROTEIN
Drug: vigabatrin
Target: Gamma-amino-N-butyrate transaminase (Enzyme)
Gene: Abat
UniProt: P50554 (GABT_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.38
Assay: Inhibition of Rattus norvegicus (rat) brain gamma-amino butyrate aminotransferase using gamma-amino butyrate as substrate assessed as decrease in NADPH generation after 30 min by spectrophotometric analysis
Drug: viloxazine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.76
Assay: Equilibrium dissociation constant (KD) for Competitive binding between [3H]- imipramine and the compound at human transporter-hSERT
Drug: viloxazine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.81
Assay: Equilibrium dissociation constant (KD) for Competitive binding between [3H]WIN-35428 and the compound at human transporter-hDAT
Drug: viloxazine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: Slc6a4
UniProt: P31652 (SC6A4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.78
Assay: Inhibition of [3H]5-HT reuptake into rat frontal cortex synaptosomes
Drug: viloxazine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: Slc6a3
UniProt: P23977 (SC6A3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.32
Assay: Inhibition of [3H]- DA reuptake into rat striatal synaptosomes
Drug: viloxazine
Target: Transporter (Transporter)
Gene: Slc6a2
UniProt: Q9WTR4 (Q9WTR4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.77
Assay: Inhibition of [3H]- NE reuptake into rat hippocampal synaptosomes
Drug: viloxazine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.7
Action type: ANTAGONIST
Assay: Possible mechanism of action in ADHD
Drug: vinblastine
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7
Assay: High affinity constant at binding site of human P-Glycoprotein (P-gp) in two-affinity model
Drug: vinblastine
Target: Canalicular multispecific organic anion transporter 1 (Transporter)
Gene: ABCC2
UniProt: Q92887 (MRP2_HUMAN)
Organism: Homo sapiens
Drug: vinblastine
Target: Multidrug resistance-associated protein 1 (Transporter)
Gene: ABCC1
UniProt: P33527 (MRP1_HUMAN)
Organism: Homo sapiens
Drug: vinblastine
Target: Multidrug resistance-associated protein 7 (Transporter)
Gene: ABCC10
UniProt: Q5T3U5 (MRP7_HUMAN)
Organism: Homo sapiens
Drug: vinblastine
Target: Thromboxane-A synthase (Enzyme)
Gene: TBXAS1
UniProt: P24557 (THAS_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.728
Assay: DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2)
Drug: vinblastine
Target: Arachidonate 15-lipoxygenase (Enzyme)
Gene: ALOX15
UniProt: P12530 (LOX15_RABIT)
Organism: Oryctolagus cuniculus
Activity: IC50 = 5.298
Assay: DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid)
Drug: vinblastine
Target: Amine oxidase [flavin-containing] B (Enzyme)
Gene: MAOB
UniProt: P56560 (AOFB_BOVIN)
Organism: Bos taurus
Activity: Ki = 4.11
Assay: Inhibitory activity against Monoamine oxidase B isolated from beef liver mitochondria was determined