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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
26
hits in this display
Target
Tyrosine-protein kinase BTK
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
IC50: <0.5nM
Assay Description:
Inhibition of human BTK using fluorescein-labeled polyGAT peptide as substrate incubated for 30 mins by FRET assay
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Target
Tyrosine-protein kinase BTK
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
IC50: <1nM
Assay Description:
The purpose of the BTK in vitro assay is to determine compound potency against BTK through the measurement of IC50. Compound inhibition is measured a...
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Target
Tyrosine-protein kinase BTK [14-552]
(Homo sapiens (Human))
Biogen Ma
US Patent
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
IC50: <1nM
Assay Description:
The purpose of the BTK in vitro assay is to determine compound potency against BTK through the measurement of IC50. Compound inhibition is measured a...
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Target
Tyrosine-protein kinase BTK
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
IC50: <1nM
Assay Description:
The purpose of the BTK in vitro assay is to determine compound potency against BTK through the measurement of IC50. Compound inhibition is measured a...
More data for this Ligand-Target Pair
Target Info
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Target
Tyrosine-protein kinase BTK
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
IC50: 5.40nM
Assay Description:
Inhibition of BTK in anti-IgM stimulated human PBMC cells assessed as reduction in PLCgamma2 phosphorylation
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Target
Tyrosine-protein kinase BTK
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
IC50: 22nM
Assay Description:
Inhibition of human BTK assessed as reduction in OVA323-329 specific T cells proliferation
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Target
Tyrosine-protein kinase BTK
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
IC50: 24nM
Assay Description:
Inhibition of BTK phosphorylation in human whole blood assessed as reduction in BTK phosphorylation incubated for 30 mins
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Target
Early activation antigen CD69
(Homo sapiens)
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
IC50: 70nM
Assay Description:
Inhibition of CD69 in human whole blood preincubated for 30 mins followed by anti-human IgD stimulation and measured after 18 to 22 hrs by flow cytom...
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Target
Early activation antigen CD69
(Homo sapiens)
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
IC50: 71nM
Assay Description:
Inhibition of CD69 (unknown origin) assessed as reduction in BCR mediated B cell activation
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Target
CD63 antigen
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
IC50: 82nM
Assay Description:
Inhibition of CD63 (unknown origin) assessed as FcepsilonR induced basophil activation
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Target
Tyrosine-protein kinase BTK
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
IC50: 505nM
Assay Description:
The purpose of the BTK in vitro assay is to determine compound potency against BTK through the measurement of IC50. Compound inhibition is measured a...
More data for this Ligand-Target Pair
Target Info
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Target
Tyrosine-protein kinase BTK
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
IC50: 6.90E+3nM
Assay Description:
Inhibition of BTK in human Ramos cells assessed as reduction in PLCgamma2 phosphorylation
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Target
Sodium channel protein type 5 subunit alpha
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
IC50: >2.50E+4nM
Assay Description:
Inhibition of phasic human Nav1.5
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Target
Sodium channel protein type 5 subunit alpha
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
IC50: >2.50E+4nM
Assay Description:
Inhibition of tonic human Nav1.5
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Target
Voltage-dependent L-type calcium channel subunit alpha-1C
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
IC50: >2.50E+4nM
Assay Description:
Inhibition of human Cav1.2
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Target
Potassium voltage-gated channel subfamily H member 2
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
IC50: >2.50E+4nM
Assay Description:
Inhibition of human ERG by patch clamp method
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Target
Cyclin-dependent kinase-like 2
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
Kd: 240nM
Assay Description:
Binding affinity to wild-type human partial length CDKL2 (M1 to D327 residues) expressed in bacterial expression system by Kinomescan method
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Target
Cytoplasmic tyrosine-protein kinase BMX
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
Kd: 88nM
Assay Description:
Binding affinity to wild-type human full length BMX (M1 to H675 residues) expressed in bacterial expression system by Kinomescan method
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Target
Aurora kinase A
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
Kd: 660nM
Assay Description:
Binding affinity to wild-type human partial length AURKA (E122 to K401 residues) expressed in mammalian expression system by Kinomescan method
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Target
Tyrosine-protein kinase BTK
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
Kd: 0.0700nM
Assay Description:
Binding affinity to wild-type human full length BTK (M1 to S659 residues) expressed in mammalian expression system by Kinomescan method
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Target
Tyrosine-protein kinase receptor Tie-1
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
Kd: 40nM
Assay Description:
Binding affinity to wild-type human partial length TIE1 (T819 to A1138 residues) expressed in bacterial expression system by Kinomescan method
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Target
Tyrosine-protein kinase Tec
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
Kd: 240nM
Assay Description:
Binding affinity to wild-type human partial length TEC (L341 to D620 residues) expressed in bacterial expression system by Kinomescan method
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Target
Proto-oncogene tyrosine-protein kinase Src
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
Kd: 320nM
Assay Description:
Binding affinity to wild-type human partial length SRC (L240 to L536 residues) expressed in bacterial expression system by Kinomescan method
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Target
Mitogen-activated protein kinase kinase kinase 13
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
Kd: >3.00E+3nM
Assay Description:
Binding affinity to wild-type human full length LZK (M1 to W966 residues) expressed in mammalian expression system by Kinomescan method
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Target
Dual specificity mitogen-activated protein kinase kinase 2
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
Kd: 200nM
Assay Description:
Binding affinity to wild-type human full length MEK2 (M1 to V400 residues) expressed in mammalian expression system by Kinomescan method
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Target
Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma
(Homo sapiens (Human))
Biogen
Curated by
ChEMBL
Ligand
BDBM324284
((R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4...)
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Affinity Data
Kd: 420nM
Assay Description:
Binding affinity to wild-type human partial length PIP5K1C (M1 to T668 residues) expressed in mammalian expression system by Kinomescan method
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