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Literature summary extracted from

  • Takeuchi, K.; Kohn, T.J.; True, T.A.; Mais, D.E.; Wikel, J.H.; Utterback, B.G.; Wyss, V.L.; Jakubowski, J.A.
    Development of dual-acting agents for thromboxane receptor antagonism and thromboxane synthase inhibition. 3. Synthesis and biological activities of oxazolecarboxamide-substituted omega-phenyl-omega-(3-pyridyl)alkenoic acid derivatives and related compounds (1998), J. Med. Chem., 41, 5362-5374.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.3.99.5 (+)-(E)-7-[4-[4-[[[2-(trans)-phenylcyclopropyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid 0.0000085 mM, 50% inhibition Homo sapiens
5.3.99.5 (-)-(E)-7-[4-[4-[[[2-(trans)-phenylcyclopropyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid 0.0000059 mM, 50% inhibition Homo sapiens
5.3.99.5 (E)-7-[4-[4-[(benzylamino)carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid 0.000025 mM, 50% inhibition Homo sapiens
5.3.99.5 (E)-7-[4-[4-[(pentylamino)carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridiyl)hept-6-enoic acid 0.000031 mM, 50% inhibition Homo sapiens
5.3.99.5 (E)-7-[4-[4-[(phenylethylamino)carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid 0.0000094 mM, 50% inhibition Homo sapiens
5.3.99.5 (E)-7-[4-[4-[[(2-phenoxybutyl)amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid 0.000049 mM, 50% inhibition Homo sapiens
5.3.99.5 (E)-7-[4-[4-[[(2-phenoxyethyl)amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid 0.0000026 mM, 50% inhibition Homo sapiens
5.3.99.5 (E)-7-[4-[4-[[(2-phenoxypentyl)amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid 0.000049 mM, 50% inhibition Homo sapiens
5.3.99.5 (E)-7-[4-[4-[[(4-cyclohexylbutyl)amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid 0.000055 mM, 50% inhibition Homo sapiens
5.3.99.5 (E)-7-[4-[4-[[(4-cyclopropylmethyl)amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid 0.000025 mM, 50% inhibition Homo sapiens
5.3.99.5 (E)-7-[4-[4-[[3-(morpholinopropyl)amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid 0.0000051 mM, 50% inhibition Homo sapiens
5.3.99.5 (E)-7-[4-[4-[[[2-(benzyloxy)ethyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid 0.000048 mM, 50% inhibition Homo sapiens
5.3.99.5 (E)-7-[4-[4-[[[2-(cyclohexylmethoxy)ethyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid 0.0000037 mM, 50% inhibition Homo sapiens
5.3.99.5 (E)-7-[4-[4-[[[2-(cyclohexyloxy)ethyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid 0.0000033 mM, 50% inhibition Homo sapiens
5.3.99.5 (E)-7-[4-[4-[[[2-(tetrahydropyran-2-ylmethoxy)ethyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid 0.0000063 mM, 50% inhibition Homo sapiens
5.3.99.5 (E)-7-[4-[4-[[[3-(1-cyclohexylethoxy)propyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid 0.0000012 mM, 50% inhibition Homo sapiens
5.3.99.5 (E)-7-[4-[4-[[[3-(4-methoxyphenyl)propyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid 0.0000027 mM, 50% inhibition Homo sapiens
5.3.99.5 (E)-7-[4-[4-[[[3-(cyclohexyloxy)propyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid 0.0000042 mM, 50% inhibition Homo sapiens
5.3.99.5 (E)-7-[4-[4-[[[3-[(cis)-4-methoxycyclohexyl]propyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid 0.0000029 mM, 50% inhibition Homo sapiens
5.3.99.5 (E)-7-[4-[4-[[[4-(cyclohexyloxy)butyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid 0.0000049 mM, 50% inhibition Homo sapiens
5.3.99.5 CV4151 0.0000049 mM, 50% inhibition Homo sapiens
5.3.99.5 R68070 0.0000015 mM, 50% inhibition 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 ?

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 ?