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Literature summary for 3.4.22.38 extracted from

  • Altmann, E.; Renaud, J.; Green, J.; Farley, D.; Cutting, B.; Jahnke, W.
    Arylaminoethyl amides as novel non-covalent cathepsin K inhibitors (2002), J. Med. Chem., 45, 2352-2354.
    View publication on PubMed
Search for more literature for 3.4.22.38

Inhibitors

Inhibitors Comment Organism Structure
N-(2,3-dichlorophenyl)triazolyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide IC50: 9 nM Homo sapiens
N-(2-chlorophenyl)triazolyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide IC50: 6 nM Homo sapiens
N-(5-isopropyl)pyridine-2-carboxyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide IC50: less than 3 nM Homo sapiens
N-4-benzyloxybenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide IC50: 6 nM Homo sapiens
N-4-isopropylbenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide IC50: less than 3 nM Homo sapiens
N-4-methoxybenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
 Homo sapiens
N-4-propylbenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide IC50: less than 3 nM Homo sapiens
Nalpha-3-chlorobenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide less efficient than Nalpha-benzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide Oryctolagus cuniculus
Nalpha-3-methoxybenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide less efficient than Nalpha-benzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide Oryctolagus cuniculus
Nalpha-3-methylbenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
 Oryctolagus cuniculus
Nalpha-4-chlorobenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
 Oryctolagus cuniculus
Nalpha-4-methoxybenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide IC50: 64 nM Oryctolagus cuniculus
Nalpha-4-methylbenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
 Oryctolagus cuniculus
Nalpha-benzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide IC50: 470 nM Oryctolagus cuniculus

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Oryctolagus cuniculus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
osteoclast
-
 Homo sapiens
-
osteoclast
-
 Oryctolagus cuniculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Z-Phe-Arg-4-methylcoumarin 7-amide + H2O
-
 Homo sapiens Z-Phe-Arg + 7-amino-4-methylcoumarin
-
 ?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000011
-
 N-(2,3-dichlorophenyl)triazolyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide standard assay conditions Homo sapiens
0.000015
-
 N-4-benzyloxybenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide standard assay conditions Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000003
-
 IC50: less than 3 nM Homo sapiens N-4-propylbenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
0.000003
-
 IC50: less than 3 nM Homo sapiens N-4-isopropylbenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
0.000003
-
 IC50: less than 3 nM Homo sapiens N-(5-isopropyl)pyridine-2-carboxyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
0.000006
-
 IC50: 6 nM Homo sapiens N-4-benzyloxybenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
0.000006
-
 IC50: 6 nM Homo sapiens N-(2-chlorophenyl)triazolyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
0.000009
-
 IC50: 9 nM Homo sapiens N-(2,3-dichlorophenyl)triazolyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
0.000064
-
 IC50: 64 nM Oryctolagus cuniculus Nalpha-4-methoxybenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
0.00047
-
 IC50: 470 nM Oryctolagus cuniculus Nalpha-benzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide