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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
(change energy unit to
kcal/mol
)
Found
44
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Target
Plasma kallikrein
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
Ki: 3nM
Assay Description:
Reversible inhibition of human plasma kallikrein assessed as inhibition constant
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Target
Plasma kallikrein
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: 3.30nM
Assay Description:
Plasma kallikrein inhibitory activity in vitro was determined using standard published methods (see e.g. Johansen et al., Int. J. Tiss. Reac. 1986, 8...
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Target
Plasma kallikrein
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: 3.30nM
Assay Description:
Plasma kallikrein inhibitory activity in vitro was determined using standard published methods. Human plasma kallikrein (Protogen) was incubated at 2...
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Target
Plasma kallikrein
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
Copy SMILES
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Affinity Data
IC50: 3.30nM
Assay Description:
Plasma kallikrein inhibitory activity in vitro was determined using standard published methods (see e.g. Johansen et al., Int. J. Tiss. Reac. 1986, 8...
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Target
Plasma kallikrein
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
Copy SMILES
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Affinity Data
IC50: 3.30nM
Assay Description:
Plasma kallikrein inhibitory activity in vitro was determined using standard published methods (see e.g. Johansen et al., Int. J. Tiss. Reac. 1986, 8...
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Target
Plasma kallikrein
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
Copy SMILES
Copy InChI
Affinity Data
IC50: 3.30nM
Assay Description:
Plasma kallikrein inhibitory activity in vitro was determined using standard published methods (see e.g. Johansen et al., Int. J. Tiss. Reac. 1986, 8...
More data for this Ligand-Target Pair
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Target
Plasma kallikrein
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: 3.30nM
Assay Description:
KLK1 inhibitory activity in vitro was determined using standard published methods. Human KLK1 (Callbiochem) was incubated at 25° C. with the fluoroge...
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Target
Plasma kallikrein
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: 6nM
Assay Description:
Inhibition of human plasma kallikrein using H-D-Pro-Phe-Arg-AFC as flurogenic substrate preincubated for 5 mins followed by substrate addition by flu...
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Target
Plasma kallikrein
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: 54nM
Assay Description:
Inhibition of DXS induced human whole plasma kallikrein using H-D-Pro-Phe-Arg-AFC as substrate preincubated for 5 mins followed by DXS stimulation by...
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Target
Beta-secretase 1
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >1.00E+4nM
Assay Description:
Inhibition of human beta-secretase 1 preincubated for 5 mins followed by substrate addition by fluorometer analysis
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Target
Cathepsin D
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >1.00E+4nM
Assay Description:
Inhibition of human Cathepsin D preincubated for 5 mins followed by substrate addition by fluorometer analysis
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Target
Cathepsin G
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >1.00E+4nM
Assay Description:
Inhibition of human Cathepsin G preincubated for 5 mins followed by substrate addition by fluorometer analysis
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Target
Renin
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >1.00E+4nM
Assay Description:
Inhibition of human renin preincubated for 5 mins followed by substrate addition by fluorometer analysis
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Target
Tryptase delta
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >1.00E+4nM
Assay Description:
Inhibition of human tryptase preincubated for 5 mins followed by substrate addition by fluorometer analysis
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Target
Tissue-type plasminogen activator
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >1.00E+4nM
Assay Description:
Inhibition of human tissue plasminogen activator preincubated for 5 mins followed by substrate addition by fluorometer analysis
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Target
Cytochrome P450 2C9
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >2.50E+4nM
Assay Description:
Inhibition of CYP2C9 in human liver microsomes assessed as reduction in 4 hydroxy-diclofenac metabolite formation incubated for 30 mins in presence o...
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Target
Cytochrome P450 1A2
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >2.50E+4nM
Assay Description:
Inhibition of CYP1A2 in human liver microsomes assessed as reduction in acetaminophen metabolite formation incubated for 30 mins in presence of NADPH...
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Cytochrome P450 2B6
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >2.50E+4nM
Assay Description:
Inhibition of CYP2B6 in human liver microsomes assessed as reduction in hydroxybupropion metabolite formation incubated for 30 mins in presence of NA...
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Cytochrome P450 2C8
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >2.50E+4nM
Assay Description:
Inhibition of CYP2C8 in human liver microsomes assessed as reduction in 6 alpha-hydroxypaclitaxel metabolite formation incubated for 30 mins in prese...
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Target
Cytochrome P450 3A4
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >2.50E+4nM
Assay Description:
Inhibition of CYP3A4 in human liver microsomes assessed as reduction in 6beta-hydroxytestosterone metabolite formation using testosterone as substrat...
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Cytochrome P450 2C19
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >2.50E+4nM
Assay Description:
Inhibition of CYP2C19 in human liver microsomes assessed as reduction in 4-hydroxymephenytoin metabolite formation incubated for 30 mins in presence ...
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Target
Cytochrome P450 2D6
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >2.50E+4nM
Assay Description:
Inhibition of CYP2D6 in human liver microsomes assessed as reduction in dextrorphan metabolite formation incubated for 30 mins in presence of NADPH b...
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Cytochrome P450 3A4
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >2.50E+4nM
Assay Description:
Inhibition of CYP3A4 in human liver microsomes assessed as reduction in 6beta-hydroxymidazolam metabolite formation using midazolam as substrate incu...
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Target
Potassium voltage-gated channel subfamily H member 2
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >3.30E+4nM
Assay Description:
Inhibition of hERG expressed in CHO cells by whole cell patch clamp assay
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Target
Trypsin
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >4.00E+4nM
Assay Description:
Inhibition of human trypsin preincubated for 5 mins followed by substrate addition by fluorometer analysis
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Target
Prothrombin
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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IC50: >4.00E+4nM
Assay Description:
Inhibition of human thrombin preincubated for 5 mins followed by substrate addition by fluorometer analysis
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Target
Plasminogen
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >4.00E+4nM
Assay Description:
Inhibition of human plasmin preincubated for 5 mins followed by substrate addition by fluorometer analysis
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Target
Coagulation factor VII
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >4.00E+4nM
Assay Description:
Inhibition of human factor 7a preincubated for 5 mins followed by substrate addition by fluorometer analysis
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Coagulation factor X
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >4.00E+4nM
Assay Description:
Inhibition of human factor 10a preincubated for 5 mins followed by substrate addition by fluorometer analysis
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Coagulation factor XI
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >4.00E+4nM
Assay Description:
Inhibition of human factor 11a preincubated for 5 mins followed by substrate addition by fluorometer analysis
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Target
Coagulation factor XII
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >4.00E+4nM
Assay Description:
Inhibition of human factor 12a preincubated for 5 mins followed by substrate addition by fluorometer analysis
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Target
Kallikrein-1
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >4.00E+4nM
Assay Description:
Inhibition of human KLK1 preincubated for 5 mins followed by substrate addition by fluorometer analysis
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Target
Kallikrein-1
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >4.00E+4nM
Assay Description:
Plasma kallikrein inhibitory activity in vitro was determined using standard published methods. Human plasma kallikrein (Protogen) was incubated at 2...
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Target
Coagulation factor XII
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >4.00E+4nM
Assay Description:
Factor XIIa inhibitory activity in vitro was determined using standard published methods (see e.g. Shori et al., Biochem. Pharmacol., 1992, 43, 1209;...
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Coagulation factor XI
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >4.00E+4nM
Assay Description:
FXIa inhibitory activity in vitro was determined using standard published methods (see e.g. Johansen et al., Int. J. Tiss. Reac. 1986, 8, 185; Shori ...
More data for this Ligand-Target Pair
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Target
Kallikrein-1
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
Copy SMILES
Copy InChI
Affinity Data
IC50: >4.00E+4nM
Assay Description:
KLK1 inhibitory activity in vitro was determined using standard published methods (see e.g. Johansen et al., Int. J. Tiss. Reac. 1986, 8, 185; Shori ...
More data for this Ligand-Target Pair
Target Info
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Target
Kallikrein-1
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
Copy SMILES
Copy InChI
Affinity Data
IC50: >4.00E+4nM
Assay Description:
KLK1 inhibitory activity in vitro was determined using standard published methods (see e.g. Johansen et al., Int. J. Tiss. Reac. 1986, 8, 185; Shori ...
More data for this Ligand-Target Pair
Target Info
PDB
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antibodypedia
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PC cid
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In Depth
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US Patent
Copy BDB DOI
Target
Kallikrein-1
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
Copy SMILES
Copy InChI
Affinity Data
IC50: >4.00E+4nM
Assay Description:
KLK1 inhibitory activity in vitro was determined using standard published methods (see e.g. Johansen et al., Int. J. Tiss. Reac. 1986, 8, 185; Shori ...
More data for this Ligand-Target Pair
Target Info
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Target
Coagulation factor XII
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
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Affinity Data
IC50: >4.00E+4nM
Assay Description:
Factor XIIa inhibitory activity in vitro was determined using standard published methods (see e.g. Shori et al., Biochem. Pharmacol., 1992, 43, 1209;...
More data for this Ligand-Target Pair
Target Info
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US Patent
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Target
Kallikrein-1
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
Copy SMILES
Copy InChI
Affinity Data
IC50: >4.00E+4nM
Assay Description:
KLK1 inhibitory activity in vitro was determined using standard published methods. Human KLK1 (Callbiochem) was incubated at 25° C. with the fluorog...
More data for this Ligand-Target Pair
Target Info
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Target
Coagulation factor XI
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
Copy SMILES
Copy InChI
Affinity Data
IC50: >4.00E+4nM
Assay Description:
FXIa inhibitory activity in vitro was determined using standard published methods (see e.g. Johansen et al., Int. J. Tiss. Reac. 1986, 8, 185; Shori ...
More data for this Ligand-Target Pair
Target Info
PDB
MMDB
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KEGG
UniProtKB/SwissProt
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DrugBank
antibodypedia
GoogleScholar
Ligand Info
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PC cid
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In Depth
Details
US Patent
Copy BDB DOI
Target
Kallikrein-1
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
Copy SMILES
Copy InChI
Affinity Data
IC50: >4.00E+4nM
Assay Description:
KLK1 inhibitory activity in vitro was determined using standard published methods (see e.g. Johansen et al., Int. J. Tiss. Reac. 1986, 8, 185; Shori ...
More data for this Ligand-Target Pair
Target Info
PDB
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US Patent
Copy BDB DOI
Target
Plasma kallikrein
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
Copy SMILES
Copy InChI
Affinity Data
EC50: 55nM
Assay Description:
Example compounds were evaluated for inhibition of the human activated kallikrein enzyme in two formats of an assay employing a fluorogenic peptide s...
More data for this Ligand-Target Pair
Target Info
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US Patent
Copy BDB DOI
Target
Plasma kallikrein
(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by
ChEMBL
Ligand
BDBM408717
( N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(met...)
Copy SMILES
Copy InChI
Affinity Data
EC50: 55nM
Assay Description:
Example compounds were evaluated for inhibition of the human activated kallikrein enzyme in two formats of an assay employing a fluorogenic peptide s...
More data for this Ligand-Target Pair
Target Info
PDB
Reactome pathway
UniProtKB/SwissProt
antibodypedia
GoogleScholar
Ligand Info
Purchase
PC cid
PC sid
In Depth
Details
US Patent
Copy BDB DOI