BDBM408794 N-[(3-ethyl-2-fluorophenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1- yl)methyl]phenyl}methyl)pyrazole-4-carboxamide ::US10364238, Example 132::US11001578, Example 132::US11084809, Example 132::US11198691, Example 132

SMILES CCc1cccc(CNC(=O)c2cn(Cc3ccc(Cn4ccccc4=O)cc3)nc2COC)c1F

InChI Key InChIKey=TVACIVBKATZGQV-UHFFFAOYSA-N

Data  9 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 9 hits for monomerid = 408794   

TargetPlasma kallikrein(Human)
Kalvista Pharmaceuticals

US Patent
LigandPNGBDBM408794(US10364238, Example 132 | N-[(3-ethyl-2-fluorophe...)
Affinity DataIC50: 135nMAssay 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
In Depth
Date in BDB:
6/29/2020
Entry Details
Go to US Patent

TargetKallikrein-1(Human)
Kalvista Pharmaceuticals

US Patent
LigandPNGBDBM408794(US10364238, Example 132 | N-[(3-ethyl-2-fluorophe...)
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 fluoroge...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/29/2020
Entry Details
Go to US Patent

TargetPlasma kallikrein(Human)
Kalvista Pharmaceuticals

US Patent
LigandPNGBDBM408794(US10364238, Example 132 | N-[(3-ethyl-2-fluorophe...)
Affinity DataIC50: 135nMAssay 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
In Depth
Date in BDB:
1/24/2022
Entry Details
Go to US Patent

TargetKallikrein-1(Human)
Kalvista Pharmaceuticals

US Patent
LigandPNGBDBM408794(US10364238, Example 132 | N-[(3-ethyl-2-fluorophe...)
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
In Depth
Date in BDB:
1/24/2022
Entry Details
Go to US Patent

TargetPlasma kallikrein(Human)
Kalvista Pharmaceuticals

US Patent
LigandPNGBDBM408794(US10364238, Example 132 | N-[(3-ethyl-2-fluorophe...)
Affinity DataIC50: 135nMAssay 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
In Depth
Date in BDB:
11/8/2021
Entry Details
Go to US Patent

TargetKallikrein-1(Human)
Kalvista Pharmaceuticals

US Patent
LigandPNGBDBM408794(US10364238, Example 132 | N-[(3-ethyl-2-fluorophe...)
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
In Depth
Date in BDB:
11/8/2021
Entry Details
Go to US Patent

TargetPlasma kallikrein(Human)
Kalvista Pharmaceuticals

US Patent
LigandPNGBDBM408794(US10364238, Example 132 | N-[(3-ethyl-2-fluorophe...)
Affinity DataIC50: 135nMAssay 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
In Depth
Date in BDB:
4/24/2022
Entry Details
Go to US Patent

TargetKallikrein-1(Human)
Kalvista Pharmaceuticals

US Patent
LigandPNGBDBM408794(US10364238, Example 132 | N-[(3-ethyl-2-fluorophe...)
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
In Depth
Date in BDB:
4/24/2022
Entry Details
Go to US Patent

TargetPlasma kallikrein(Human)
Kalvista Pharmaceuticals

US Patent
LigandPNGBDBM408794(US10364238, Example 132 | N-[(3-ethyl-2-fluorophe...)
Affinity DataIC50: 140nMAssay 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
In Depth
Date in BDB:
6/20/2023
Entry Details
PubMed