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Literature summary for 1.11.2.2 extracted from

  • Hu, C.H.; Neissel Valente, M.W.; Halpern, O.S.; Jusuf, S.; Khan, J.A.; Locke, G.A.; Duke, G.J.; Liu, X.; Duclos, F.J.; Wexler, R.R.; Kick, E.K.; Smallheer, J.M.
    Small molecule and macrocyclic pyrazole derived inhibitors of myeloperoxidase (MPO) (2021), Bioorg. Med. Chem. Lett., 42, 128010 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1-(2-[(propan-2-yl)oxy]ethyl)-2-sulfanylidene-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one i.e. AZD-3241, irreversible inhibitor Homo sapiens
2-[6-(5-chloro-2-methoxyphenyl)-4-oxo-2-sulfanylidene-3,4-dihydropyrimidin-1(2H)-yl]acetamide i.e. PF-06282999, irreversible inhibitor Homo sapiens
3-[(4-fluorophenyl)methyl]-2-sulfanylidene-1,2,3,7-tetrahydro-6H-purin-6-one i.e. TX2, irreversible inhibitor Homo sapiens
7-(5-amino-3H-[1,2,3]triazolo[4,5-b]pyridin-7-yl)-13-(2-phenylethyl)-3,4,10,13-tetraazatricyclo[13.3.1.13,6]icosa-1(19),4,6(20),15,17-pentaen-12-one
-
Homo sapiens
7-(benzyloxy)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine
-
Homo sapiens
7-([1-[(3-benzylphenyl)methyl]-1H-pyrazol-3-yl]methyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-([1-[(3-phenoxyphenyl)methyl]-1H-pyrazol-3-yl]methyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-([1-[(3-[[(3S)-pyrrolidin-3-yl]oxy]phenyl)methyl]-1H-pyrazol-3-yl]methyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-benzyl-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[(1-benzyl-1H-pyrazol-3-yl)methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[(1-phenyl-1H-pyrazol-3-yl)methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[(1-[[3-(piperidin-4-yl)phenyl]methyl]-1H-pyrazol-3-yl)methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[(17S)-18-phenyl-16-oxa-2,8,9-triazapentacyclo[16.2.2.11,17.16,9.111,15]pentacosa-6(25),7,11(24),12,14-pentaen-5-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[(1R)-1-phenyl-3-[(4-phenylbicyclo[2.2.2]octan-1-yl)amino]propyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[(1R)-3-[[(1R)-2,3-dihydro-1H-inden-1-yl]amino]-1-phenylpropyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[(2-fluorobenzyl)sulfanyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[(3R,4S,6S)-4-benzyl-2-oxa-7,13,14-triazatetracyclo[14.3.1.13,6.111,14]docosa-1(20),11(21),12,16,18-pentaen-10-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[14'-oxa-3',4',10'-triazaspiro[cyclopentane-1,12'-tricyclo[13.3.1.13,6]icosane]-1'(19'),4',6'(20'),15',17'-pentaen-7'-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[17-oxa-3,4,10-triazatetracyclo[16.3.1.13,6.112,16]tetracosa-1(22),4,6(24),12(23),13,15,18,20-octaen-7-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[17-oxa-3,4,10-triazatetracyclo[17.3.1.13,6.112,16]pentacosa-1(23),4,6(25),12(24),13,15,19,21-octaen-7-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[18-oxa-3,4,10-triazatetracyclo[17.3.1.13,6.112,16]pentacosa-1(23),4,6(25),12(24),13,15,19,21-octaen-7-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[18-oxa-3,4,10-triazatetracyclo[17.3.1.13,6.113,17]pentacosa-1(23),4,6(25),13(24),14,16,19,21-octaen-7-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[18-oxa-3,4,10-triazatetracyclo[18.3.1.13,6.113,17]hexacosa-1(24),4,6(26),13(25),14,16,20,22-octaen-7-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[3-oxa-10,11,17-triazatetracyclo[16.2.2.14,8.110,13]tetracosa-4(24),5,7,11,13(23)-pentaen-14-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[8,9,15-triazatetracyclo[16.3.1.12,6.18,11]tetracosa-1(22),2(24),3,5,9,11(23),18,20-octaen-12-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[[1-(1,2,3,4-tetrahydroisoquinolin-6-ylmethyl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[[1-(4-fluorophenyl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[[1-(biphenyl-3-yl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[[1-(biphenyl-3-ylmethyl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[[1-(isoquinolin-6-ylmethyl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[[1-(naphthalen-2-ylmethyl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[[1-(pyridin-2-yl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
-
Homo sapiens
7-[[1-([3-[(2,3-dihydro-1H-isoindol-4-yl)oxy]phenyl]methyl)-1H-pyrazol-3-yl]methyl]-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
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
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
0.000001
-
pH and temperature not specified in the publication Homo sapiens 7-[(1R)-1-phenyl-3-[(4-phenylbicyclo[2.2.2]octan-1-yl)amino]propyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000005
-
pH and temperature not specified in the publication Homo sapiens 7-[(3R,4S,6S)-4-benzyl-2-oxa-7,13,14-triazatetracyclo[14.3.1.13,6.111,14]docosa-1(20),11(21),12,16,18-pentaen-10-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000007
-
pH and temperature not specified in the publication Homo sapiens 7-[(17S)-18-phenyl-16-oxa-2,8,9-triazapentacyclo[16.2.2.11,17.16,9.111,15]pentacosa-6(25),7,11(24),12,14-pentaen-5-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000008
-
pH and temperature not specified in the publication Homo sapiens 7-[17-oxa-3,4,10-triazatetracyclo[17.3.1.13,6.112,16]pentacosa-1(23),4,6(25),12(24),13,15,19,21-octaen-7-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000014
-
pH and temperature not specified in the publication Homo sapiens 7-[18-oxa-3,4,10-triazatetracyclo[17.3.1.13,6.113,17]pentacosa-1(23),4,6(25),13(24),14,16,19,21-octaen-7-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000017
-
pH and temperature not specified in the publication Homo sapiens 7-[18-oxa-3,4,10-triazatetracyclo[18.3.1.13,6.113,17]hexacosa-1(24),4,6(26),13(25),14,16,20,22-octaen-7-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000021
-
pH and temperature not specified in the publication Homo sapiens 7-[8,9,15-triazatetracyclo[16.3.1.12,6.18,11]tetracosa-1(22),2(24),3,5,9,11(23),18,20-octaen-12-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000025
-
pH and temperature not specified in the publication Homo sapiens 7-[18-oxa-3,4,10-triazatetracyclo[17.3.1.13,6.112,16]pentacosa-1(23),4,6(25),12(24),13,15,19,21-octaen-7-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000026
-
pH and temperature not specified in the publication Homo sapiens 7-[14'-oxa-3',4',10'-triazaspiro[cyclopentane-1,12'-tricyclo[13.3.1.13,6]icosane]-1'(19'),4',6'(20'),15',17'-pentaen-7'-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000026
-
pH and temperature not specified in the publication Homo sapiens 7-[[1-([3-[(2,3-dihydro-1H-isoindol-4-yl)oxy]phenyl]methyl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000029
-
pH and temperature not specified in the publication Homo sapiens 7-(5-amino-3H-[1,2,3]triazolo[4,5-b]pyridin-7-yl)-13-(2-phenylethyl)-3,4,10,13-tetraazatricyclo[13.3.1.13,6]icosa-1(19),4,6(20),15,17-pentaen-12-one
0.000031
-
pH and temperature not specified in the publication Homo sapiens 7-[3-oxa-10,11,17-triazatetracyclo[16.2.2.14,8.110,13]tetracosa-4(24),5,7,11,13(23)-pentaen-14-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000036
-
pH and temperature not specified in the publication Homo sapiens 7-[17-oxa-3,4,10-triazatetracyclo[16.3.1.13,6.112,16]tetracosa-1(22),4,6(24),12(23),13,15,18,20-octaen-7-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000039
-
pH and temperature not specified in the publication Homo sapiens 7-([1-[(3-benzylphenyl)methyl]-1H-pyrazol-3-yl]methyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.00004
-
pH and temperature not specified in the publication Homo sapiens 7-[(2-fluorobenzyl)sulfanyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000044
-
pH and temperature not specified in the publication Homo sapiens 7-([1-[(3-phenoxyphenyl)methyl]-1H-pyrazol-3-yl]methyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000046
-
pH and temperature not specified in the publication Homo sapiens 7-([1-[(3-[[(3S)-pyrrolidin-3-yl]oxy]phenyl)methyl]-1H-pyrazol-3-yl]methyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000052
-
pH and temperature not specified in the publication Homo sapiens 7-[[1-(naphthalen-2-ylmethyl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000053
-
pH and temperature not specified in the publication Homo sapiens 7-[[1-(4-fluorophenyl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000054
-
pH and temperature not specified in the publication Homo sapiens 7-[[1-(pyridin-2-yl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000055
-
pH and temperature not specified in the publication Homo sapiens 7-[(1-phenyl-1H-pyrazol-3-yl)methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000055
-
pH and temperature not specified in the publication Homo sapiens 7-[[1-(biphenyl-3-ylmethyl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000058
-
pH and temperature not specified in the publication Homo sapiens 7-[(1R)-3-[[(1R)-2,3-dihydro-1H-inden-1-yl]amino]-1-phenylpropyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000058
-
pH and temperature not specified in the publication Homo sapiens 7-[[1-(1,2,3,4-tetrahydroisoquinolin-6-ylmethyl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.00008
-
pH and temperature not specified in the publication Homo sapiens 7-benzyl-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.000085
-
pH and temperature not specified in the publication Homo sapiens 7-[[1-(biphenyl-3-yl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.0001
-
pH and temperature not specified in the publication Homo sapiens 7-[(1-[[3-(piperidin-4-yl)phenyl]methyl]-1H-pyrazol-3-yl)methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.00012
-
pH and temperature not specified in the publication Homo sapiens 7-[(1-benzyl-1H-pyrazol-3-yl)methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.00014
-
pH and temperature not specified in the publication Homo sapiens 7-[[1-(isoquinolin-6-ylmethyl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
0.00019
-
pH and temperature not specified in the publication Homo sapiens 7-(benzyloxy)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine