AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: benserazide
Target: SUMO-activating enzyme (Enzyme)
Gene: SAE1|UBA2
UniProt: Q9UBE0|Q9UBT2 (SAE1_HUMAN|SAE2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.63
Assay: PUBCHEM_BIOASSAY: uHTS HTRF assay for identification of inhibitors of SUMOylation. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID2011, AID2018, AID2069, AID2614, AID2658]
Drug: benserazide
Target: Cytoplasmic zinc-finger protein (Unclassified)
Gene: pos-1
UniProt: G5EF15 (G5EF15_CAEEL)
Organism: Caenorhabditis elegans
Activity: EC50 = 4.43
Assay: Active
Drug: benserazide
Target: Genome polyprotein [Cleaved into: P1; Capsid protein VP0 (Unclassified)
UniProt: P03313 (POLG_CXB3N)
Organism: Coxsackievirus B3
Activity: IC50 = 5.62
Assay: Inhibition of recombinant Coxsackievirus B3 3C protease expressed in Escherichia coli BL21 (DE3) preincubated for 5 mins followed by addition of NMA-EALFQGPPVK-DNP-rrr-NH2 as substrate measured every 10 mins for 2 hrs by FRET-based enzyme assay
Drug: benserazide
Target: Hexokinase-2 (Kinase)
Gene: HK2
UniProt: P52789 (HXK2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.26
Assay: Inhibition of HK2 (unknown origin) using glucose-6-phosphate dehydrogenase as substrate preincubated for 10 mins followed by substrate addition
Drug: benzarone
Target: Solute carrier family 22 member 12 (Transporter)
Gene: SLC22A12
UniProt: Q96S37 (S22AC_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.55
Assay: Inhibition of human URAT1 expressed in xenopus oocyte assessed as inhibition of [14C]-labelled urate uptake after 60 mins by liquid scintillation counting
Drug: benzarone
Target: Eyes absent homolog 3 (Enzyme)
Gene: EYA3
UniProt: Q99504 (EYA3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.77
Assay: Inhibition of poly-histidine and GST-tagged full length human Eya3 isoform 2 (127 to 573 residues) using para-nitrophenol phosphate substrate incubated for 30 mins
Drug: benzbromarone
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.94
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: benzbromarone
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.53
Assay: DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
Drug: benzbromarone
Target: Multidrug resistance-associated protein 1 (Transporter)
Gene: ABCC1
UniProt: P33527 (MRP1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.72
Assay: Inhibition of human MRP1 expressed in Spodoptera frugiperda Sf9 cells assessed as inhibition of NEM-GS-induced vanadate-sensitive ATPase activity measured by generation of inorganic phosphate by spectrophotometry in presence of glutathione
Drug: benzbromarone
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.796
Assay: DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: benzbromarone
Target: Aldo-keto reductase family 1 member C1 (Enzyme)
Gene: AKR1C1
UniProt: Q04828 (AK1C1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.32
Assay: Inhibition of 20-alpha HSD
Drug: benzbromarone
Target: Tyrosine-protein phosphatase non-receptor type 1 (Enzyme)
Gene: PTPN1
UniProt: P18031 (PTN1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.27
Assay: Inhibition of PTP1B (unknown origin) by p-nitrophenylphosphate assay
Drug: benzbromarone
Target: cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Enzyme)
Gene: PDE4A
UniProt: P27815 (PDE4A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.976
Assay: DRUGMATRIX: Phosphodiesterase PDE4 enzyme inhibition (substrate: [3H]cAMP + cAMP)
Drug: benzbromarone
Target: Mitogen-activated protein kinase 14 (Kinase)
Gene: MAPK14
UniProt: Q16539 (MK14_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.908
Assay: DRUGMATRIX: Protein Serine/Threonine Kinase, p38alpha enzyme inhibition (substrate: Myelin Basic Protein)
Drug: benzbromarone
Target: Mitogen-activated protein kinase 1 (Kinase)
Gene: MAPK1
UniProt: P28482 (MK01_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.711
Assay: DRUGMATRIX: Protein Serine/Threonine Kinase, ERK2 enzyme inhibition (substrate: Myelin Basic Protein)
Drug: benzbromarone
Target: M1-family alanyl aminopeptidase (Enzyme)
UniProt: Q8IEK1 (Q8IEK1_PLAF7)
Organism: Plasmodium falciparum (isolate 3D7)
Activity: IC50 = 4.2
Assay: Active
Drug: benzbromarone
Target: Envelope glycoprotein gp160 (Viral envelope protein)
Gene: env
UniProt: Q75760 (Q75760_9HIV1)
Organism: Human immunodeficiency virus 1
Activity: IC50 = 4.89
Assay: Active
Drug: benzbromarone
Target: Polymerase acidic protein (Enzyme)
Gene: PA
UniProt: P03433 (PA_I34A1)
Organism: Influenza A virus (strain A/Puerto Rico/8/1934 H1N1)
Activity: Kd = 4.32
Assay: Binding affinity to PA cavity of recombinant Influenza A virus A/PR/8/34(H1N1) PA (239 to 716 residues) measured after 2 mins by SPR analysis
Drug: benzbromarone
Target: Eyes absent homolog 2 (Enzyme)
Gene: EYA2
UniProt: O00167 (EYA2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.99
Assay: Inhibition of human Eya2 catalytic domain by p-nitrophenylphosphate assay
Drug: benzbromarone
Target: Eyes absent homolog 3 (Enzyme)
Gene: EYA3
UniProt: Q99504 (EYA3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.08
Assay: Inhibition of poly-histidine and GST-tagged full length human Eya3 isoform 2 (127 to 573 residues) using para-nitrophenol phosphate substrate incubated for 30 mins
Drug: benzbromarone
Target: Solute carrier family 22 member 12 (Transporter)
Gene: SLC22A12
UniProt: Q96S37 (S22AC_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.59
Action type: INHIBITOR
Assay: Inhibition of human URAT1 expressed in xenopus oocyte assessed as inhibition of [14C]-labelled urate uptake after 60 mins by liquid scintillation counting
Drug: benziodarone
Target: Baculoviral IAP repeat-containing protein 5 (Unclassified)
Gene: BIRC5
UniProt: O15392 (BIRC5_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.1
Assay: Binding affinity to human survivin expressed in Escherichia coli BL21 cells after 30 mins
Drug: benziodarone
Target: Eyes absent homolog 3 (Enzyme)
Gene: EYA3
UniProt: Q99504 (EYA3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.47
Assay: Inhibition of poly-histidine and GST-tagged full length human Eya3 isoform 2 (127 to 573 residues) using para-nitrophenol phosphate substrate incubated for 30 mins
Drug: benzocaine
Target: Sodium channel protein type 1 subunit alpha (Ion channel)
Gene: SCN1A
UniProt: P35498 (SCN1A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Assay: Mechanism of Action
Drug: benzocaine
Target: Sodium channel protein type 2 subunit alpha (Ion channel)
Gene: SCN2A
UniProt: Q99250 (SCN2A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Assay: Mechanism of Action
Drug: benzocaine
Target: Sodium channel protein type 3 subunit alpha (Ion channel)
Gene: SCN3A
UniProt: Q9NY46 (SCN3A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Assay: Mechanism of Action
Drug: benzocaine
Target: Sodium channel protein type 4 subunit alpha (Ion channel)
Gene: SCN4A
UniProt: P35499 (SCN4A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Assay: Mechanism of Action
Drug: benzocaine
Target: Sodium channel protein type 8 subunit alpha (Ion channel)
Gene: SCN8A
UniProt: Q9UQD0 (SCN8A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Assay: Mechanism of Action
Drug: benzocaine
Target: Sodium channel protein type 9 subunit alpha (Ion channel)
Gene: SCN9A
UniProt: Q15858 (SCN9A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Assay: Mechanism of Action
Drug: benzocaine
Target: Sodium channel protein type 11 subunit alpha (Ion channel)
Gene: SCN11A
UniProt: Q9UI33 (SCNBA_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Assay: Mechanism of Action
Drug: benzocaine
Target: Sodium channel protein type 10 subunit alpha (Ion channel)
Gene: SCN10A
UniProt: Q9Y5Y9 (SCNAA_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Assay: Mechanism of Action
Drug: benzocaine
Target: Sodium channel protein type 7 subunit alpha (Ion channel)
Gene: SCN7A
UniProt: Q01118 (SCN7A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Assay: Mechanism of Action
Drug: benzocaine
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Activity: ED50 = 3.495
Action type: BLOCKER
Drug: benzonatate
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Drug: benzphetamine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Drug: benzphetamine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Action type: RELEASING AGENT
Assay: Mechanism of Action; CHEMBL222; SINGLE PROTEIN
Drug: benzphetamine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Drug: benzphetamine
Target: Synaptic vesicular amine transporter (Transporter)
Gene: SLC18A2
UniProt: Q05940 (VMAT2_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL1893; SINGLE PROTEIN
Drug: benzquinamide
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.32
Action type: INHIBITOR
Drug: benzquinamide
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.4
Action type: AGONIST
Drug: benzquinamide
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.445
Drug: benzquinamide
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.241
Drug: benzquinamide
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.865
Drug: benzquinamide
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.161
Drug: benzquinamide
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.264
Drug: benzthiazide
Target: Carbonic anhydrase 2 (Enzyme)
Gene: CA2
UniProt: P00918 (CAH2_HUMAN)
Organism: Homo sapiens
Drug: benzthiazide
Target: Solute carrier family 12 member 3 (Transporter)
Gene: SLC12A3
UniProt: P55017 (S12A3_HUMAN)
Organism: Homo sapiens
Activity: A2 = 8.17
Action type: INHIBITOR
Drug: benzthiazide
Target: Carbonic anhydrase 1 (Enzyme)
Gene: CA1
UniProt: P00915 (CAH1_HUMAN)
Organism: Homo sapiens
Drug: benzthiazide
Target: Carbonic anhydrase 4 (Enzyme)
Gene: CA4
UniProt: P22748 (CAH4_HUMAN)
Organism: Homo sapiens
Drug: benzthiazide
Target: Calcium-activated potassium channel subunit alpha-1 (Ion channel)
Gene: KCNMA1
UniProt: Q12791 (KCMA1_HUMAN)
Organism: Homo sapiens
Drug: benzatropine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.69
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: benzatropine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.229
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: benzatropine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.62
Assay: Binding affinity of [3H]citalopram for serotonin transporter in monkey
Drug: benzatropine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.86
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: benzatropine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.157
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: benzatropine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.896
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: benzatropine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.495
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: benzatropine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.888
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: benzatropine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.523
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: benzatropine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.654
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: benzatropine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.959
Drug: benzatropine
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.926
Assay: DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug: benzatropine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.636
Action type: ANTAGONIST
Drug: benzatropine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.854
Action type: ANTAGONIST
Drug: benzatropine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.959
Action type: ANTAGONIST
Drug: benzatropine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.959
Action type: ANTAGONIST
Drug: benzatropine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.553
Action type: ANTAGONIST
Drug: benzatropine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.244
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: benzatropine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.253
Drug: benzatropine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.585
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: benzatropine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.387
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: benzatropine
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.951
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: benzatropine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.85
Drug: benzatropine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: Chrm2
UniProt: P10980 (ACM2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.59
Assay: Affinity for rat M1 acetylcholine receptor using [3H]-AF DX 384 displacement.
Drug: benzatropine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: Chrm1
UniProt: P08482 (ACM1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.23
Assay: Displacement of [3H]pirenzepine binding at Muscarinic acetylcholine receptor M1 in rat brain P2 membranes.
Drug: benzatropine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: Slc6a4
UniProt: P31652 (SC6A4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.29
Assay: Binding affinity against serotonin transporter using [125]RTI-55
Drug: benzatropine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: Slc6a3
UniProt: P23977 (SC6A3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.93
Assay: Displacement of [3H]WIN-35428 binding to the dopamine transporter in rat caudate putamen tissue.
Drug: benzatropine
Target: Sodium-dependent neutral amino acid transporter B(0)AT1 (Transporter)
Gene: SLC6A19
UniProt: Q695T7 (S6A19_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.36
Action type: INHIBITOR
Drug: benzyl benzoate
Target: Beta-lactamase (Enzyme)
Gene: ampC
UniProt: P00811 (AMPC_ECOLI)
Organism: Escherichia coli (strain K12)
Activity: IC50 = 4.05
Assay: Compound was tested for the inhibition of beta-lactamase
Drug: benzyl benzoate
Target: Hormone-sensitive lipase (Enzyme)
Gene: Lipe
UniProt: P15304 (LIPS_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.96
Assay: Inhibition of HSL in Wistar rat isolated fat cells by spectrophotometric assay
Drug: bepotastine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Drug: bepridil
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Drug: bepridil
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.26
Drug: bepridil
Target: Voltage-dependent P/Q-type calcium channel subunit alpha-1A (Ion channel)
Gene: CACNA1A
UniProt: O00555 (CAC1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.6
Action type: BLOCKER
Drug: bepridil
Target: Voltage-dependent T-type calcium channel subunit alpha-1H (Ion channel)
Gene: CACNA1H
UniProt: O95180 (CAC1H_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.149
Action type: BLOCKER
Drug: bepridil
Target: Lethal factor (Enzyme)
Gene: lef
UniProt: P15917 (LEF_BACAN)
Organism: Bacillus anthracis
Activity: IC50 = 5.32
Assay: Protection against Bacillus anthracis lethal toxin-mediated cytotoxicity in mouse RAW264.7 cells assessed as change in viability after 24 hrs by WST1 dye reduction assay
Drug: bepridil
Target: Potassium voltage-gated channel subfamily KQT member 4 (Ion channel)
Gene: KCNQ4
UniProt: P56696 (KCNQ4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5
Action type: BLOCKER
Drug: bepridil
Target: Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (Ion channel)
Gene: HCN4
UniProt: Q9Y3Q4 (HCN4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.31
Drug: bepridil
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: CACNA1C
UniProt: P15381 (CAC1C_RABIT)
Organism: Oryctolagus cuniculus
Activity: IC50 = 4.66
Assay: Inhibition of [3H]nitrendipine binding to calcium channels in Rabbit cardiac muscle.
Drug: bepridil
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 = 6.08
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: bepridil
Target: Potassium channel subfamily T member 1 (Ion channel)
Gene: Kcnt1
UniProt: Q9Z258 (KCNT1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6
Action type: GATING INHIBITOR
Drug: bepridil
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: CACNA1C
UniProt: Q13936 (CAC1C_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Assay: Mechanism of Action
Drug: bepridil
Target: Voltage-dependent L-type calcium channel subunit alpha-1D (Ion channel)
Gene: CACNA1D
UniProt: Q01668 (CAC1D_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Assay: Mechanism of Action
Drug: beraprost
Target: Prostaglandin E2 receptor EP3 subtype (GPCR)
Gene: PTGER3
UniProt: P43115 (PE2R3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.17
Action type: AGONIST
Drug: beraprost
Target: Prostaglandin E2 receptor EP4 subtype (GPCR)
Gene: PTGER4
UniProt: P35408 (PE2R4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.14
Action type: AGONIST
Drug: beraprost
Target: Prostacyclin receptor (GPCR)
Gene: Ptgir
UniProt: P43252 (PI2R_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.8
Action type: AGONIST
Drug: beraprost
Target: Prostacyclin receptor (GPCR)
Gene: Ptgir
UniProt: P43253 (PI2R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.72
Action type: AGONIST
Drug: beraprost
Target: Prostacyclin receptor (GPCR)
Gene: PTGIR
UniProt: P43119 (PI2R_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.37
Action type: AGONIST
Drug: betacarotene
Target: Core protein (Unclassified)
UniProt: Q2Q167 (Q2Q167_9HEPC)
Organism: Hepatitis C virus
Activity: IC50 = 4.53
Assay: Not Active
Drug: betahistine
Target: Histamine H3 receptor (GPCR)
Gene: Hrh3
UniProt: Q9QYN8 (HRH3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.69
Assay: Binding affinity to rat histamine H3 receptor
Drug: betahistine
Target: Histamine H3 receptor (GPCR)
Gene: HRH3
UniProt: Q9Y5N1 (HRH3_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 9.523
Action type: INVERSE AGONIST
Assay: [125I]Iodoproxyfan binding to H3 receptors in CHO cells
Drug: betamethasone
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.07
Action type: AGONIST
Drug: betamethasone
Target: Annexin A1 (Cytosolic other)
Gene: ANXA1
UniProt: P04083 (ANXA1_HUMAN)
Organism: Homo sapiens
Drug: betamethasone acetate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action; CHEMBL2034; SINGLE PROTEIN
Drug: betamethasone benzoate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action; CHEMBL2034; SINGLE PROTEIN
Drug: betamethasone dipropionate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action; CHEMBL2034; SINGLE PROTEIN
Drug: betamethasone dipropionate
Target: Glucocorticoid receptor (Transcription factor)
Gene: Nr3c1
UniProt: P06536 (GCR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.28
Assay: Competitive displacement of [3H]dexamethasone from glucocorticoid receptor of rat liver cytosol
Drug: betamethasone valerate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action; CHEMBL2034; SINGLE PROTEIN
Drug: betamipron
Target: Solute carrier family 22 member 6 (Transporter)
Gene: SLC22A6
UniProt: Q4U2R8 (S22A6_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.62
Drug: betamipron
Target: Solute carrier family 22 member 8 (Transporter)
Gene: SLC22A8
UniProt: Q8TCC7 (S22A8_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.32
Drug: betaxolol
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.8
Action type: ANTAGONIST
Drug: betaxolol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.2