AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: droperidol
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.263
Assay: DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug: droperidol
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.602
Action type: ANTAGONIST
Drug: droperidol
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.954
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: droperidol
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.49
Assay: Inhibition of human Potassium channel HERG expressed in mammalian cells
Drug: droperidol
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.86
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
Drug: droperidol
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.132
Action type: ANTAGONIST
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: droperidol
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.069
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: droperidol
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.623
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: droperidol
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.996
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: droperidol
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.027
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: droperidol
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.28
Assay: DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug: droperidol
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.27
Assay: DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: droperidol
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.782
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: droperidol
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.592
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: droperidol
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.076
Drug: droperidol
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.175
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: droperidol
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.01
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: droperidol
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.695
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: droperidol
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.78
Drug: droperidol
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.62
Drug: droperidol
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 = 6.13
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: drospirenone
Target: Mineralocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C2
UniProt: P08235 (MCR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 10.5
Action type: ANTAGONIST
Drug: drospirenone
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.5
Drug: drospirenone
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 10.5
Action type: AGONIST
Drug: drotaverine
Target: cAMP-specific 3',5'-cyclic phosphodiesterase 4B (Enzyme)
Gene: PDE4B
UniProt: Q07343 (PDE4B_HUMAN)
Organism: Homo sapiens
Drug: drotaverine
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: CACNA1C
UniProt: Q13936 (CAC1C_HUMAN)
Organism: Homo sapiens
Drug: droxidopa
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.1
Action type: ANTAGONIST
Drug: droxidopa
Target: Adrenergic receptor (GPCR)
Gene: ADRB2|ADRB1|ADRA2A|ADRB3|ADRA2B|ADRA2C|ADRA1D|ADRA1A|ADRA1B
UniProt: P07550|P08588|P08913|P13945|P18089|P18825|P25100|P35348|P35368 (ADRB2_HUMAN|ADRB1_HUMAN|ADA2A_HUMAN|ADRB3_HUMAN|ADA2B_HUMAN|ADA2C_HUMAN|ADA1D_HUMAN|ADA1A_HUMAN|ADA1B_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action; CHEMBL2331074; PROTEIN FAMILY
Drug: duloxetine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.62
Action type: INHIBITOR
Assay: Displacement of [3H]citalopram from human SERT transfected in HEK293 cells after 3 hrs by Wallac counting analysis
Drug: duloxetine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.22
Action type: INHIBITOR
Assay: Inhibition of human NET
Drug: duloxetine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.301
Drug: duloxetine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.3
Action type: ANTAGONIST
Drug: duloxetine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.678
Drug: duloxetine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6
Action type: ANTAGONIST
Drug: duloxetine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.4
Action type: ANTAGONIST
Drug: duloxetine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.646
Drug: duloxetine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.638
Drug: duloxetine
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.402
Drug: duloxetine
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.523
Drug: duloxetine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.62
Assay: Ability to inhibit the reuptake of dopamine at human dopamine transporter
Drug: duloxetine
Target: 5-hydroxytryptamine receptor 1F (GPCR)
Gene: HTR1F
UniProt: P30939 (5HT1F_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.352
Drug: duloxetine
Target: 5-hydroxytryptamine receptor 1E (GPCR)
Gene: HTR1E
UniProt: P28566 (5HT1E_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.428
Drug: duloxetine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: Slc6a4
UniProt: P31652 (SC6A4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 10.09
Assay: Displacement of [3H]-citalopram from Sprague-Dawley rat brain SERT after 1 hr
Drug: duloxetine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: Slc6a3
UniProt: P23977 (SC6A3_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.43
Assay: Displacement of [125I]RTI55 from DAT in Sprague-dawley rat striatum by liquid scintillation spectrophotometry
Drug: duloxetine
Target: Transporter (Transporter)
Gene: NET
UniProt: Q63380 (Q63380_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.52
Assay: Displacement of [3H]nisoxetine from rat NET in rat cerebral cortex
Drug: duloxetine
Target: Serine hydroxymethyltransferase, mitochondrial (Enzyme)
Gene: SHMT2
UniProt: P34897 (GLYM_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.16
Assay: Inhibition of His-tagged human recombinant SHMT2 expressed in Escherichia coli BLR(DE3) assessed as reduction in NADPH level using L-serine, THF and NADP+ incubated for 5 mins by SHMT2-MTHFD coupled reaction based fluorescence assay
Drug: dutasteride
Target: Glycine receptor subunit alpha-1 (Ion channel)
Gene: GLRA1
UniProt: P23415 (GLRA1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.48
Drug: dutasteride
Target: 3-oxo-5-alpha-steroid 4-dehydrogenase 2 (Enzyme)
Gene: SRD5A2
UniProt: P31213 (S5A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.2
Action type: INHIBITOR
Drug: dutasteride
Target: 3-oxo-5-alpha-steroid 4-dehydrogenase 1 (Enzyme)
Gene: SRD5A1
UniProt: P18405 (S5A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.49
Action type: INHIBITOR
Drug: dyclonine
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P22303 (ACES_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.74
Assay: Inhibition of AChE (unknown origin)
Drug: dyclonine
Target: Sodium channel protein type 10 subunit alpha (Ion channel)
Gene: SCN10A
UniProt: Q9Y5Y9 (SCNAA_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: dydrogesterone
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.9
Action type: AGONIST
Drug: dydrogesterone
Target: Nuclear receptor subfamily 2 group E member 1 (Nuclear hormone receptor)
Gene: NR2E1
UniProt: Q9Y466 (NR2E1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.561
Assay: orthogonal direct binding assay
Drug: diprophylline
Target: cGMP-inhibited 3',5'-cyclic phosphodiesterase A (Enzyme)
Gene: PDE3A
UniProt: Q14432 (PDE3A_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL241; SINGLE PROTEIN
Drug: diprophylline
Target: cAMP-specific 3',5'-cyclic phosphodiesterase 4B (Enzyme)
Gene: PDE4B
UniProt: Q07343 (PDE4B_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Drug: ebastine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.224
Assay: DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug: ebastine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.21
Assay: Compound is evaluated for in vitro receptor binding affinity against Dopamine receptor D2
Drug: ebastine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.506
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: ebastine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.55
Drug: ebastine
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.82
Assay: Inhibition of human ABCB1-mediated rhodamine 123 efflux in mouse L5178 cells expressing human MDR1 after 20 mins by FACS analysis
Drug: ebastine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.185
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: ebastine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.341
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: ebastine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.33
Assay: Compound is evaluated for in vitro receptor binding affinity against 5-hydroxytryptamine 1A receptor
Drug: ebastine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.588
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: ebastine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.701
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: ebastine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.905
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: ebastine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.991
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: ebastine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.472
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: ebastine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.384
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: ebastine
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.543
Assay: DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug: ebastine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.96
Assay: Compound is evaluated for in vitro receptor binding affinity against Muscarinic acetylcholine receptor M1
Drug: ebastine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.554
Assay: DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: ebastine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.863
Assay: DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: ebastine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.937
Assay: DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: ebastine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.615
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: ebastine
Target: Beta-3 adrenergic receptor (GPCR)
Gene: ADRB3
UniProt: P13945 (ADRB3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.719
Assay: DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug: ebastine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.397
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: ebastine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.106
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: ebastine
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.743
Assay: DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
Drug: ebastine
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.341
Assay: DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug: ebastine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.06
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: ebastine
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P22303 (ACES_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.126
Assay: DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine)
Drug: ebastine
Target: Epidermal growth factor receptor (Kinase)
Gene: EGFR
UniProt: P00533 (EGFR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.253
Assay: DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: ebastine
Target: Tyrosine-protein kinase Fyn (Kinase)
Gene: FYN
UniProt: P06241 (FYN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.091
Assay: DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: ebastine
Target: Receptor tyrosine-protein kinase erbB-2 (Kinase)
Gene: ERBB2
UniProt: P04626 (ERBB2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.976
Assay: DRUGMATRIX: Protein Tyrosine Kinase, ERBB2 (HER2) enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: ebastine
Target: Substance-K receptor (GPCR)
Gene: TACR2
UniProt: P21452 (NK2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.191
Assay: DRUGMATRIX: Tachykinin NK2  radioligand binding (ligand: [3H] SR-48968)
Drug: ebastine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.633
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: ebastine
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.849
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug: ebastine
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.871
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: ebastine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.58
Drug: ebastine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P31389 (HRH1_CAVPO)
Organism: Cavia porcellus
Activity: IC50 = 7.35
Assay: Compound is evaluated for in vitro receptor binding affinity against H1 receptor
Drug: ebastine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8
Action type: ANTAGONIST
Drug: ebrotidine
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Assay: Mechanism of Action
Drug: echothiophate
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P22303 (ACES_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL220; SINGLE PROTEIN
Drug: econazole
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.131
Assay: DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug: econazole
Target: Cannabinoid receptor 1 (GPCR)
Gene: CNR1
UniProt: P21554 (CNR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.543
Assay: DRUGMATRIX: Cannabinoid CB1 radioligand binding (ligand: [3H] SR141716A)
Drug: econazole
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.636
Assay: DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine)
Drug: econazole
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.336
Assay: DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug: econazole
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.37
Assay: DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
Drug: econazole
Target: Adenosine receptor A2a (GPCR)
Gene: ADORA2A
UniProt: P29274 (AA2AR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.086
Assay: DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA)
Drug: econazole
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.79
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: econazole
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.052
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: econazole
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.301
Assay: DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin)
Drug: econazole
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.648
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: econazole
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.617
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: econazole
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.034
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
Drug: econazole
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.939
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: econazole
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.362
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: econazole
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.202
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)