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Literature summary for 1.13.11.33 extracted from

  • Pelcman, B.; Sanin, A.; Nilsson, P.; No, K.; Schaal, W.; Oehrman, S.; Krog-Jensen, C.; Forsell, P.; Hallberg, A.; Larhed, M.; Boesen, T.; Kromann, H.; Vogensen, S.B.; Groth, T.; Claesson, H.E.
    3-Substituted pyrazoles and 4-substituted triazoles as inhibitors of human 15-lipoxygenase-1 (2015), Bioorg. Med. Chem. Lett., 25, 3024-3029 .
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
recombinant expression of 15-LOX-1 in Spodoptera frugiperda SF9 cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-(1H-pyrazol-3-yl)-1,3-benzoxazole
-
Homo sapiens
4,5-dichloro-N-(2-chloro-4-fluorophenyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
4-amino-N-(2-chloro-4-fluorophenyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
4-bromo-5-chloro-N-(2-chloro-4-fluorophenyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
4-bromo-N-(2-chloro-4-fluorophenyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
4-butyl-N-(2-chloro-4-fluorophenyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
4-chloro-N-(2-chloro-4-fluorophenyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
4-chloro-N-(2-chloro-4-fluorophenyl)-5-(difluoromethyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
4-chloro-N-(2-chloro-4-fluorophenyl)-5-(trifluoromethyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
5-amino-N-(2-chloro-4-fluorophenyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
5-chloro-2-(1H-pyrazol-3-yl)-1,3-benzoxazole
-
Homo sapiens
5-chloro-N-(2-chloro-4-fluorophenyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
5-fluoro-2-(1H-pyrazol-3-yl)-1,3-benzoxazole
-
Homo sapiens
5-tert-butyl-N-(2-chloro-4-fluorophenyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
6-chloro-2-(1H-pyrazol-3-yl)-1,3-benzoxazole
-
Homo sapiens
6-chloro-2-(4,5-dichloro-1H-pyrazol-3-yl)-1,3-benzoxazole
-
Homo sapiens
6-chloro-2-(5-chloro-1H-pyrazol-3-yl)-1,3-benzoxazole
-
Homo sapiens
6-fluoro-2-(1H-pyrazol-3-yl)-1,3-benzoxazole
-
Homo sapiens
additional information 3-substituted pyrazoles and 4-substituted triazoles as inhibitors of human 15-lipoxygenase-1, overview. The 1N-substituent is not essential for activity or selectivity. Additional halogen substituents on the pyrazole ring increase activity. Further development leads to triazole-4-carboxanilides and 2-(3-pyrazolyl) benzoxazoles, which are potent and selective 15-LOX-1 inhibitors Homo sapiens
N-(2,4-dichlorophenyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(2,5-dichlorophenyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(2-chloro-4-fluorophenyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(2-chloro-4-fluorophenyl)-4,5-bis(trifluoromethyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(2-chloro-4-fluorophenyl)-4-(trifluoromethyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(2-chloro-4-fluorophenyl)-4-fluoro-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(2-chloro-4-fluorophenyl)-4-iodo-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(2-chloro-4-fluorophenyl)-4-methyl-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(2-chloro-4-fluorophenyl)-4-methyl-5-(trimethylsilyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(2-chloro-4-fluorophenyl)-4-nitro-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(2-chloro-4-fluorophenyl)-4-phenyl-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(2-chloro-4-fluorophenyl)-4-[(methanesulfonyl)amino]-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(2-chloro-4-fluorophenyl)-5-(difluoromethyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(2-chloro-4-fluorophenyl)-5-(trifluoromethyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(2-chloro-4-fluorophenyl)-5-iodo-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(2-chloro-4-fluorophenyl)-5-methyl-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(2-chloro-4-fluorophenyl)-5-nitro-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(2-chloro-4-fluorophenyl)-5-[(methanesulfonyl)amino]-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(2-chlorophenyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(2-chlorophenyl)-N-methyl-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(3,4-dichlorophenyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(4-fluorophenyl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(5-chloro-1,3-thiazol-2-yl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(5-chloropyridin-2-yl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(5-fluoropyridin-2-yl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(7-fluoroquinolin-3-yl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(isoquinolin-3-yl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(pyridin-2-yl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(pyridin-3-yl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(pyridin-4-yl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(quinolin-2-yl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(quinolin-3-yl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-(quinolin-6-yl)-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-benzyl-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-phenyl-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-[4-(trifluoromethyl)phenyl]-1H-pyrazole-3-carboxamide
-
Homo sapiens
N-[4-fluoro-2-(trifluoromethyl)phenyl]-1H-pyrazole-3-carboxamide
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
arachidonate + O2 Homo sapiens best substrate (5Z,8Z,11Z,13E)-(15S)-15-hydroperoxyicosa-5,8,11,13-tetraenoate
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P16050
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
arachidonate + O2 best substrate Homo sapiens (5Z,8Z,11Z,13E)-(15S)-15-hydroperoxyicosa-5,8,11,13-tetraenoate
-
?

Synonyms

Synonyms Comment Organism
15-lipoxygenase
-
Homo sapiens
15-lipoxygenase-1
-
Homo sapiens
15-LOX-1
-
Homo sapiens