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Literature summary extracted from

  • Jacobs, C.; Frotscher, M.; Dannhardt, G.; Hartmann, R.W.
    1-Imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase (2000), J. Med. Chem., 43, 1841-1851.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.3.99.5 1-[2-(4,5,6,7-tetrahydrobenzo[b]furan-4-yl)ethyl]-1H-imidazole 0.001 mM, 50% inhibition Homo sapiens
5.3.99.5 1-[2-(4,5,6,7-tetrahydrobenzo[b]furan-4-ylidene)ethyl]-1H-imidazole E isomer, 0.00355 mM, 50% inhibition; Z isomer, 0.0041 mM, 50% inhibition Homo sapiens
5.3.99.5 1-[2-(4,5,6,7-tetrahydrobenzo[b]thiophen-4-yl)ethyl]-1H-imidazole 0.0012 mM, 50% inhibition Homo sapiens
5.3.99.5 1-[2-(4,5,6,7-tetrahydrobenzo[b]thiophen-4-ylidene)ethyl]-1H-imidazole E isomer, 0.0017 mM, 50% inhibition; Z isomer, 0.0013 mM, 50% inhibition Homo sapiens
5.3.99.5 1-[2-(benzo[b]thiophen-4-yl)ethyl]-1H-imidazole 0.0053 mM, 50% inhibition Homo sapiens
5.3.99.5 5-[2-(imidazol-1-yl)-ethyl]-5,6,7,8-tetrahydroquinoline 0.00063 mM, 50% inhibition Homo sapiens
5.3.99.5 5-[2-(imidazol-1-yl)ethyl]-1,2,3,4-tetrahydronaphthalene 0.0034 mM, 50% inhibition Homo sapiens
5.3.99.5 5-[2-(imidazol-1-yl)ethyl]-7,8-dihydroquinoline 0.00029 mM, 50% inhibition Homo sapiens
5.3.99.5 5-[2-(imidazol-1-yl)ethyl]quinoline 0.0012 mM, 50% inhibition Homo sapiens
5.3.99.5 5-[3-(imidazol-1-yl)-propyl]-5,6,7,8-tetrahydroquinoline 0.0023 mM, 50% inhibition Homo sapiens
5.3.99.5 5-[3-(imidazol-1-yl)-propyl]-7,8-dihydroquinoline 0.00068 mM, 50% inhibition Homo sapiens
5.3.99.5 5-[imidazol-1-yl-methyl]-5,6,7,8-tetrahydroquinoline 0.002 mM, 50% inhibition Homo sapiens
5.3.99.5 5-[imidazol-1-yl-methyl]-7,8-dihydroquinoline 0.0015 mM, 50% inhibition Homo sapiens
5.3.99.5 7-[(imidazol-1-yl)methyl]isoquinoline 0.0054 mM, 50% inhibition Homo sapiens
5.3.99.5 indomethacin 0.000017 mM, 50% inhibition of PGE2 formation, 0.000013 mM, 50% inhibition of 12-HHT formation Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
5.3.99.5 (5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate Homo sapiens
-
 (5Z,13E)-(15S)-9alpha,11alpha-epoxy-15-hydroxythromboxa-5,13-dienoate i.e. TXA2 ?
5.3.99.5 (5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate Homo sapiens
-
 12-L-hydroxy-5,8,10-heptadecaotrienoic acid + malondialdehyde ratio of TXA2/heptadecatrienoic acid/malondialdehyde, 1/1/1 ?

Organism

EC Number Organism UniProt Comment Textmining
5.3.99.5 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5.3.99.5 (5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
-
 Homo sapiens (5Z,13E)-(15S)-9alpha,11alpha-epoxy-15-hydroxythromboxa-5,13-dienoate i.e. TXA2 ?
5.3.99.5 (5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
-
 Homo sapiens 12-L-hydroxy-5,8,10-heptadecaotrienoic acid + malondialdehyde ratio of TXA2/heptadecatrienoic acid/malondialdehyde, 1/1/1 ?