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Literature summary for 1.11.2.2 extracted from

  • Wurtz, N.; Viet, A.; Shaw, S.; Dilger, A.; Valente, M.; Khan, J.; Jusuf, S.; Narayanan, R.; Fernando, G.; Lo, F.; Liu, X.; Locke, G.; Kopcho, L.; Abell, L.; Sleph, P.; Basso, M.; Zhao, L.; Wexler, R.; Duclos, F.; Kick, E.
    Potent triazolopyridine myeloperoxidase inhibitors (2018), ACS Med. Chem. Lett., 9, 1175-1180 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
(5-(((5-amino-3H-[1,2,3]triazolo[4,5-b]pyridin-7-yl)oxy)methyl)-2-phenyl-2H-1,2,3-triazol-4-yl)methanol
-
Homo sapiens
7-(((5-(difluoromethyl)-2-phenyl-2H-1,2,3-triazol-4-yl)methyl)thio)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-((1-phenyl-1H-1,2,3-triazol-4-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-((2'-fluorobiphenyl-3-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-((2,6-dichlorobenzyl)oxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-((2,6-dichlorobenzyl)thio)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-((2-(1H-pyrazol-1-yl)benzyl)oxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-((2-(methylsulfonyl)benzyl)oxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-((2-fluorobenzyl)thio)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-((3'-fluoro-2-methylbiphenyl-3-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-((3'-fluorobiphenyl-3-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-((3-phenylisoxazol-5-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-((4-chloro-3'-fluorobiphenyl-3-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-((5-(difluoromethyl)-2-phenyl-2H-1,2,3-triazol-4-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-((5-methyl-2-phenyl-2H-1,2,3-triazol-4-yl)methoxy)-3H-[1,2,3]triazolo [4,5-b]pyridin-5-amine
-
Homo sapiens
7-((5-phenyloxazol-2-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-(2-chlorobenzyloxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-(2-fluorobenzyloxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-(2-methyl-3-(1-methyl-1H-pyrazol-3-yl)benzyloxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-(3-(1-methyl-1H-pyrazol-3-yl)benzyloxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-(3-(1-methyl-1H-pyrazol-4-yl)benzyloxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-(3-chlorobenzyloxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-(4-chlorobenzyloxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-(benzyloxy)-3a,7a-dihydro-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine
-
Homo sapiens
7-(benzyloxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
Cl- + H2O2 + H+ Homo sapiens
-
HClO + H2O
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P05164
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Amplex Red + H2O2 i.e. 10-acetyl-2,7-dihydroxyphenoxazine Homo sapiens resorufin + H2O
-
?
Cl- + H2O2 + H+
-
Homo sapiens HClO + H2O
-
?

Synonyms

Synonyms Comment Organism
MPO
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
heme
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000046
-
at pH 7.4 and 25°C Homo sapiens 7-((2,6-dichlorobenzyl)thio)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.0000067
-
at pH 7.4 and 25°C Homo sapiens 7-((2,6-dichlorobenzyl)oxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.0000085
-
at pH 7.4 and 25°C Homo sapiens 7-(((5-(difluoromethyl)-2-phenyl-2H-1,2,3-triazol-4-yl)methyl)thio)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.0000087
-
at pH 7.4 and 25°C Homo sapiens 7-((2-fluorobenzyl)thio)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000012
-
at pH 7.4 and 25°C Homo sapiens 7-((5-(difluoromethyl)-2-phenyl-2H-1,2,3-triazol-4-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000021
-
at pH 7.4 and 25°C Homo sapiens 7-((3'-fluorobiphenyl-3-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000021
-
at pH 7.4 and 25°C Homo sapiens 7-(3-(1-methyl-1H-pyrazol-3-yl)benzyloxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000021
-
at pH 7.4 and 25°C Homo sapiens 7-(3-chlorobenzyloxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000023
-
at pH 7.4 and 25°C Homo sapiens 7-((3'-fluoro-2-methylbiphenyl-3-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000024
-
at pH 7.4 and 25°C Homo sapiens 7-((4-chloro-3'-fluorobiphenyl-3-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000026
-
at pH 7.4 and 25°C Homo sapiens 7-((2-(1H-pyrazol-1-yl)benzyl)oxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000026
-
at pH 7.4 and 25°C Homo sapiens 7-(2-chlorobenzyloxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000026
-
at pH 7.4 and 25°C Homo sapiens 7-(2-methyl-3-(1-methyl-1H-pyrazol-3-yl)benzyloxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000026
-
at pH 7.4 and 25°C Homo sapiens 7-(4-chlorobenzyloxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000027
-
at pH 7.4 and 25°C Homo sapiens 7-((5-methyl-2-phenyl-2H-1,2,3-triazol-4-yl)methoxy)-3H-[1,2,3]triazolo [4,5-b]pyridin-5-amine
0.00003
-
at pH 7.4 and 25°C Homo sapiens 7-(2-fluorobenzyloxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000036
-
at pH 7.4 and 25°C Homo sapiens 7-(benzyloxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000078
-
at pH 7.4 and 25°C Homo sapiens 7-(3-(1-methyl-1H-pyrazol-4-yl)benzyloxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.00011
-
at pH 7.4 and 25°C Homo sapiens 7-(benzyloxy)-3a,7a-dihydro-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine
0.00012
-
at pH 7.4 and 25°C Homo sapiens 7-((3-phenylisoxazol-5-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.00016
-
at pH 7.4 and 25°C Homo sapiens 7-((2'-fluorobiphenyl-3-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.00025
-
at pH 7.4 and 25°C Homo sapiens (5-(((5-amino-3H-[1,2,3]triazolo[4,5-b]pyridin-7-yl)oxy)methyl)-2-phenyl-2H-1,2,3-triazol-4-yl)methanol
0.00029
-
at pH 7.4 and 25°C Homo sapiens 7-((5-phenyloxazol-2-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.0004
-
at pH 7.4 and 25°C Homo sapiens 7-((1-phenyl-1H-1,2,3-triazol-4-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.00072
-
at pH 7.4 and 25°C Homo sapiens 7-((2-(methylsulfonyl)benzyl)oxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine