BDBM408733 3-cyclopropyl-N-[(2-fluoro-3-methoxyphenyl)methyl]-1-({4-[(2-oxopyridin-1- yl)methyl]phenyl}methyl)pyrazole-4-carboxamide ::US10364238, Example 52::US11001578, Example 52::US11084809, Example 52::US11198691, Example 52

SMILES COc1cccc(CNC(=O)c2cn(Cc3ccc(Cn4ccccc4=O)cc3)nc2C2CC2)c1F

InChI Key InChIKey=NFLOZDGNLCLQAJ-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:
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 9 hits for monomerid = 408733   

TargetPlasma kallikrein(Human)
Kalvista Pharmaceuticals

US Patent
LigandPNGBDBM408733(US10364238, Example 52 | 3-cyclopropyl-N-[(2-fluo...)
Affinity DataIC50: 23.3nMAssay 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
LigandPNGBDBM408733(US10364238, Example 52 | 3-cyclopropyl-N-[(2-fluo...)
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
LigandPNGBDBM408733(US10364238, Example 52 | 3-cyclopropyl-N-[(2-fluo...)
Affinity DataIC50: 23.3nMAssay 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
LigandPNGBDBM408733(US10364238, Example 52 | 3-cyclopropyl-N-[(2-fluo...)
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
LigandPNGBDBM408733(US10364238, Example 52 | 3-cyclopropyl-N-[(2-fluo...)
Affinity DataIC50: 23.3nMAssay 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
LigandPNGBDBM408733(US10364238, Example 52 | 3-cyclopropyl-N-[(2-fluo...)
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
LigandPNGBDBM408733(US10364238, Example 52 | 3-cyclopropyl-N-[(2-fluo...)
Affinity DataIC50: 23.3nMAssay 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
LigandPNGBDBM408733(US10364238, Example 52 | 3-cyclopropyl-N-[(2-fluo...)
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
LigandPNGBDBM408733(US10364238, Example 52 | 3-cyclopropyl-N-[(2-fluo...)
Affinity DataIC50: 23nMAssay 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