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Compile Data Set for Download or QSAR
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
(change energy unit to
kcal/mol
)
Found
36
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Target
Histamine H1 receptor
(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research & Development
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
Ki: 37nM
Assay Description:
Binding affinity for H1 histamine receptor expressed in CHO cells
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Target
Histamine H1 receptor
(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research & Development
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
Ki: 311nM
Assay Description:
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
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Target
Histamine H1 receptor
(RAT)
Schering-Plough
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
Ki: 350nM
Assay Description:
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
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Target
Histamine H1 receptor
(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research & Development
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
Ki: 414nM
Assay Description:
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Vrije Universiteit Amsterdam
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
Ki: >1.00E+4nM ΔG°: >-29.7kJ/mole
pH: 7.4 T: 2°C
Assay Description:
Ligand displacement assays were performed on The SK-N-MC/hH4R cell homogenates. Retained radioactivity was determined by liquid scintillation countin...
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Target
Cytochrome P450 2D6
(Homo sapiens (Human))
Pfizer
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
IC50: <100nM
Assay Description:
Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate after 8 mins by LC-MS/MS analysis
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Target
Potassium voltage-gated channel subfamily H member 2
(Homo sapiens (Human))
Reverse Proteomics Research Institute
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
IC50: 170nM
Assay Description:
Inhibitory concentration against potassium channel HERG
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Potassium voltage-gated channel subfamily H member 2
(Homo sapiens (Human))
Reverse Proteomics Research Institute
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
IC50: 170nM
Assay Description:
Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique
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Target
Potassium voltage-gated channel subfamily H member 2
(Homo sapiens (Human))
Reverse Proteomics Research Institute
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
IC50: 170nM
Assay Description:
Inhibition of human Potassium channel HERG expressed in mammalian cells
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Target
Potassium voltage-gated channel subfamily H member 2
(Homo sapiens (Human))
Reverse Proteomics Research Institute
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
IC50: 173nM
Assay Description:
K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1
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Target
Potassium voltage-gated channel subfamily H member 2
(Homo sapiens (Human))
Reverse Proteomics Research Institute
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
IC50: 174nM
Assay Description:
Inhibition of human ERG in MCF7 cells
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Target
Potassium voltage-gated channel subfamily H member 2
(Homo sapiens (Human))
Reverse Proteomics Research Institute
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
IC50: 174nM
Assay Description:
Inhibition of human ERG
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Target
Histamine H1 receptor
(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research & Development
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
IC50: 290nM
Assay Description:
Inhibition constant against histamine H1 receptor
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Target
Cytochrome P450 2C19
(Homo sapiens (Human))
Pfizer
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
IC50: 2.80E+3nM
Assay Description:
Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate after 8 mins by LC-MS/MS analysis
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Cytochrome P450 2C8
(Homo sapiens (Human))
Pfizer
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
IC50: 2.95E+3nM
Assay Description:
Inhibition of CYP2C8 in human liver microsomes using paclitaxel as substrate after 8 mins by LC-MS/MS analysis
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Target
Bile acid receptor
(Homo sapiens (Human))
City Of Hope National Medical Center
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
IC50: 3.07E+3nM
Assay Description:
Antagonist activity at human GTS-tagged FXR after 20 mins by TR-FRET assay
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Target
Sodium-dependent neutral amino acid transporter B(0)AT2
(Homo sapiens (Human))
Max Planck Institute Of Psychiatry
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
IC50: 4.00E+3nM
Assay Description:
Inhibition of eGFP-tagged human B0AT2 expressed in HEK293 cells measured within 10 mins by [3H]proline uptake assay
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Target
ATP-dependent translocase ABCB1
(Homo sapiens (Human))
Schering-Plough Research Institute
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
IC50: 1.14E+4nM
Assay Description:
TP_TRANSPORTER: inhibition of Daunorubicin efflux (Daunorubicin: ? uM) in G185 cells
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Target
Voltage-dependent L-type calcium channel subunit alpha-1C/alpha-1D/alpha-1F/alpha-1S
(Homo sapiens (Human))
Chantest
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
IC50: 1.14E+4nM
Assay Description:
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
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Target
Bile salt export pump
(Homo sapiens (Human))
Amgen
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
IC50: 1.20E+4nM
Assay Description:
Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to ...
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Target
Cytochrome P450 2C9
(Homo sapiens (Human))
Pfizer
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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IC50: >3.00E+4nM
Assay Description:
Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate after 8 mins by LC-MS/MS analysis
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Cytochrome P450 3A4
(Homo sapiens (Human))
Pfizer
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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IC50: >3.00E+4nM
Assay Description:
Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate after 8 mins by LC-MS/MS analysis
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Cytochrome P450 1A2
(Homo sapiens (Human))
Pfizer
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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IC50: >3.00E+4nM
Assay Description:
Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate after 8 mins by LC-MS/MS analysis
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Target
Platelet-activating factor receptor
(Homo sapiens (Human))
Schering-Plough
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
IC50: >5.00E+4nM
Assay Description:
Concentration required to cause 50% inhibition of platelet activating factor (PAF)-induced platelet aggregation of human platelet rich plasma when ch...
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Potassium channel subfamily K member 9
(Homo sapiens (Human))
Universidad De Talca
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
IC50: 6.34E+4nM
Assay Description:
Inhibition of human TASK3 expressed in HEK293 cells by Ti+ flux assay
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ATP-binding cassette sub-family C member 2
(Homo sapiens (Human))
Amgen
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
IC50: >1.33E+5nM
Assay Description:
Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...
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ATP-binding cassette sub-family C member 3
(Homo sapiens (Human))
Amgen
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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IC50: >1.33E+5nM
Assay Description:
Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ...
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ATP-binding cassette sub-family C member 4
(Homo sapiens (Human))
Amgen
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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IC50: >1.33E+5nM
Assay Description:
Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...
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Platelet-activating factor receptor
(Homo sapiens (Human))
Schering-Plough
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
IC50: 1.35E+5nM
Assay Description:
Inhibitory concentration against platelet activating factor receptor
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Target
Histamine H1 receptor
(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research & Development
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
IC50: 1.50E+6nM
Assay Description:
The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determine...
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Histamine H1 receptor
(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research & Development
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
IC50: 1.50E+6nM
Assay Description:
Affinities of the test compounds for peripheral human histamine H-4-receptors were assessed using receptor-binding assays. The specific binding of th...
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Target
Nuclear receptor subfamily 1 group I member 2
(Homo sapiens (Human))
National Institutes Of Health Chemical Genomics Center
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
EC50: 1.00E+4nM
Assay Description:
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
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Target
Histamine H1 receptor
(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research & Development
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
Kd: 190nM
Assay Description:
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
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Reactome pathway
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Target
Nuclear receptor subfamily 1 group I member 2
(Homo sapiens (Human))
National Institutes Of Health Chemical Genomics Center
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
EC50: 3.00E+3nM
Assay Description:
Agonist activity at PXR (unknown origin) expressed in human HepG2 cells assessed as induction of CYP3A4 transactivation after 16 hrs by luciferase re...
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Target
Nuclear receptor subfamily 1 group I member 2
(Homo sapiens (Human))
National Institutes Of Health Chemical Genomics Center
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
EC50: 1.00E+4nM
Assay Description:
Competitive binding affinity to human PXR LBD (111 to 434) by TR-FRET assay
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Target
Nuclear receptor subfamily 1 group I member 2
(Homo sapiens (Human))
National Institutes Of Health Chemical Genomics Center
Curated by
ChEMBL
Ligand
BDBM22876
(CHEMBL998 | Claritin | Loratadine | Sch 29851 | US...)
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Affinity Data
EC50: 1.26E+4nM
Assay Description:
Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
More data for this Ligand-Target Pair
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