BDBM408717 N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin- 1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide ::US10364238, Example 41::US10730874, Example 00397::US11001578, Example 41::US11084809, Example 41::US11198691, Example 41::US11352356, Table II.3::US11584735, Example 41 of WO2016/083820
SMILES COCc1nn(Cc2ccc(Cn3ccccc3=O)cc2)cc1C(=O)NCc1nccc(OC)c1F
InChI Key InChIKey=KGMPDQIYDKKXRD-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 44 hits for monomerid = 408717
Affinity DataKi: 3nMAssay Description:Reversible inhibition of human plasma kallikrein assessed as inhibition constantMore data for this Ligand-Target Pair
Affinity DataIC50: >4.00E+4nMAssay 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
Affinity DataEC50: 55nMAssay 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
Affinity DataIC50: 3.30nMAssay 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
Affinity DataIC50: >4.00E+4nMAssay 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
Affinity DataIC50: 3.30nMAssay 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
Affinity DataIC50: >4.00E+4nMAssay 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
Affinity DataIC50: 3.30nMAssay 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
Affinity DataIC50: >4.00E+4nMAssay 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
Affinity DataIC50: >4.00E+4nMAssay 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
Affinity DataIC50: >4.00E+4nMAssay 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
Affinity DataIC50: 3.30nMAssay Description:KLK1 inhibitory activity in vitro was determined using standard published methods. Human KLK1 (Callbiochem) was incubated at 25° C. with the fluoroge...More data for this Ligand-Target Pair
Affinity DataIC50: >4.00E+4nMAssay Description:Plasma kallikrein inhibitory activity in vitro was determined using standard published methods. Human plasma kallikrein (Protogen) was incubated at 2...More data for this Ligand-Target Pair
Affinity DataEC50: 55nMAssay 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
Affinity DataIC50: 6nMAssay 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...More data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by ChEMBL
Kalvista Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: >3.30E+4nMAssay Description:Inhibition of hERG expressed in CHO cells by whole cell patch clamp assayMore data for this Ligand-Target Pair
Affinity DataIC50: >2.50E+4nMAssay Description:Inhibition of CYP1A2 in human liver microsomes assessed as reduction in acetaminophen metabolite formation incubated for 30 mins in presence of NADPH...More data for this Ligand-Target Pair
Affinity DataIC50: >2.50E+4nMAssay Description:Inhibition of CYP2B6 in human liver microsomes assessed as reduction in hydroxybupropion metabolite formation incubated for 30 mins in presence of NA...More data for this Ligand-Target Pair
Affinity DataIC50: >2.50E+4nMAssay Description:Inhibition of CYP2C8 in human liver microsomes assessed as reduction in 6 alpha-hydroxypaclitaxel metabolite formation incubated for 30 mins in prese...More data for this Ligand-Target Pair
Affinity DataIC50: >2.50E+4nMAssay Description:Inhibition of CYP2C9 in human liver microsomes assessed as reduction in 4 hydroxy-diclofenac metabolite formation incubated for 30 mins in presence o...More data for this Ligand-Target Pair
Affinity DataIC50: >2.50E+4nMAssay Description:Inhibition of CYP2C19 in human liver microsomes assessed as reduction in 4-hydroxymephenytoin metabolite formation incubated for 30 mins in presence ...More data for this Ligand-Target Pair
Affinity DataIC50: >2.50E+4nMAssay Description:Inhibition of CYP2D6 in human liver microsomes assessed as reduction in dextrorphan metabolite formation incubated for 30 mins in presence of NADPH b...More data for this Ligand-Target Pair
Affinity DataIC50: >2.50E+4nMAssay Description:Inhibition of CYP3A4 in human liver microsomes assessed as reduction in 6beta-hydroxymidazolam metabolite formation using midazolam as substrate incu...More data for this Ligand-Target Pair
Affinity DataIC50: >2.50E+4nMAssay Description:Inhibition of CYP3A4 in human liver microsomes assessed as reduction in 6beta-hydroxytestosterone metabolite formation using testosterone as substrat...More data for this Ligand-Target Pair
Affinity DataIC50: 54nMAssay 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...More data for this Ligand-Target Pair
Affinity DataIC50: >4.00E+4nMAssay Description:Inhibition of human KLK1 preincubated for 5 mins followed by substrate addition by fluorometer analysisMore data for this Ligand-Target Pair
Affinity DataIC50: >4.00E+4nMAssay Description:Inhibition of human factor 12a preincubated for 5 mins followed by substrate addition by fluorometer analysisMore data for this Ligand-Target Pair
Affinity DataIC50: >4.00E+4nMAssay Description:Inhibition of human factor 11a preincubated for 5 mins followed by substrate addition by fluorometer analysisMore data for this Ligand-Target Pair
Affinity DataIC50: >4.00E+4nMAssay Description:Inhibition of human factor 10a preincubated for 5 mins followed by substrate addition by fluorometer analysisMore data for this Ligand-Target Pair
Affinity DataIC50: >4.00E+4nMAssay Description:Inhibition of human factor 7a preincubated for 5 mins followed by substrate addition by fluorometer analysisMore data for this Ligand-Target Pair
Affinity DataIC50: >4.00E+4nMAssay Description:Inhibition of human plasmin preincubated for 5 mins followed by substrate addition by fluorometer analysisMore data for this Ligand-Target Pair
Affinity DataIC50: >4.00E+4nMAssay Description:Inhibition of human thrombin preincubated for 5 mins followed by substrate addition by fluorometer analysisMore data for this Ligand-Target Pair
Affinity DataIC50: >4.00E+4nMAssay Description:Inhibition of human trypsin preincubated for 5 mins followed by substrate addition by fluorometer analysisMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of human beta-secretase 1 preincubated for 5 mins followed by substrate addition by fluorometer analysisMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of human Cathepsin D preincubated for 5 mins followed by substrate addition by fluorometer analysisMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of human Cathepsin G preincubated for 5 mins followed by substrate addition by fluorometer analysisMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of human renin preincubated for 5 mins followed by substrate addition by fluorometer analysisMore data for this Ligand-Target Pair
TargetTissue-type plasminogen activator(Homo sapiens (Human))
Kalvista Pharmaceuticals
Curated by ChEMBL
Kalvista Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of human tissue plasminogen activator preincubated for 5 mins followed by substrate addition by fluorometer analysisMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of human tryptase preincubated for 5 mins followed by substrate addition by fluorometer analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 3.30nMAssay 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
Affinity DataIC50: >4.00E+4nMAssay 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
Affinity DataIC50: >4.00E+4nMAssay 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
Affinity DataIC50: 3.30nMAssay Description:Plasma kallikrein inhibitory activity in vitro was determined using standard published methods. Human plasma kallikrein (Protogen) was incubated at 2...More data for this Ligand-Target Pair
Affinity DataIC50: >4.00E+4nMAssay 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