BRENDA - Enzyme Database show

Guanidine derivatives as combined thromboxane A2 receptor antagonists and synthase inhibitors

Soyka, R.; Guth, B.D.; Weisenberger, H.M.; Luger, P.; Muller, T.H.; J. Med. Chem. 42, 1235-1249 (1999)

Data extracted from this reference:

Inhibitors
EC Number
Inhibitors
Commentary
Organism
Structure
5.3.99.5
(5E)-6-(3-(2-cyano-3,3-dimethyl)guanidinophenyl)-6-(3-pyridyl)hex-5-enoic acid
0.000026 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-(1-adamantyl)-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.000003 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-(2-dimethylaminoethyl)-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.0029 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-(2-methylpropyl)guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.000025 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-(3-methylbutyl)guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.000003 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-(3-pyridylmethyl)-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.000032 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-benzylguanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.000011 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-cyclohexyl-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.000003 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-cyclopentyl-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.000003 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-cyclopropyl-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.00038 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-isopropyl)guanidinophenyl)-6-(3-pyridyl)hex-5-enoic acid
0.000024 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-methyl)guanidinophenyl)-6-(3-pyridyl)hex-5-enoic acid
0.00025 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-tert-butyl-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.000004 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(4-(2-cyano-3-cyclopentyl-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.00018 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(4-(2-cyano-3-cyclopropyl-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.0039 mM, 50% inhibition
Homo sapiens
5.3.99.5
5E-6-(3-cyanoguanidino)phenyl-6-(3-pyridyl)hex-5-enoic acid
0.00043 mM, 50% inhibition
Homo sapiens
5.3.99.5
ridogrel
0.000004 mM, 50% inhibition
Homo sapiens
5.3.99.5
samixogrel
0.000004 mM, 50% inhibition
Homo sapiens
Natural Substrates/ Products (Substrates)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
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
Homo sapiens
?
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
5.3.99.5
Homo sapiens
-
-
-
Substrates and Products (Substrate)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
5.3.99.5
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
-
652716
Homo sapiens
(5Z,13E)-(15S)-9alpha,11alpha-epoxy-15-hydroxythromboxa-5,13-dienoate
i.e. TXA2
652716
Homo sapiens
?
Inhibitors (protein specific)
EC Number
Inhibitors
Commentary
Organism
Structure
5.3.99.5
(5E)-6-(3-(2-cyano-3,3-dimethyl)guanidinophenyl)-6-(3-pyridyl)hex-5-enoic acid
0.000026 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-(1-adamantyl)-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.000003 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-(2-dimethylaminoethyl)-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.0029 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-(2-methylpropyl)guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.000025 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-(3-methylbutyl)guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.000003 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-(3-pyridylmethyl)-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.000032 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-benzylguanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.000011 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-cyclohexyl-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.000003 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-cyclopentyl-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.000003 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-cyclopropyl-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.00038 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-isopropyl)guanidinophenyl)-6-(3-pyridyl)hex-5-enoic acid
0.000024 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-methyl)guanidinophenyl)-6-(3-pyridyl)hex-5-enoic acid
0.00025 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(3-(2-cyano-3-tert-butyl-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.000004 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(4-(2-cyano-3-cyclopentyl-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.00018 mM, 50% inhibition
Homo sapiens
5.3.99.5
(5E)-6-(4-(2-cyano-3-cyclopropyl-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
0.0039 mM, 50% inhibition
Homo sapiens
5.3.99.5
5E-6-(3-cyanoguanidino)phenyl-6-(3-pyridyl)hex-5-enoic acid
0.00043 mM, 50% inhibition
Homo sapiens
5.3.99.5
ridogrel
0.000004 mM, 50% inhibition
Homo sapiens
5.3.99.5
samixogrel
0.000004 mM, 50% inhibition
Homo sapiens
Natural Substrates/ Products (Substrates) (protein specific)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
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
Homo sapiens
?
Substrates and Products (Substrate) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
5.3.99.5
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
-
652716
Homo sapiens
(5Z,13E)-(15S)-9alpha,11alpha-epoxy-15-hydroxythromboxa-5,13-dienoate
i.e. TXA2
652716
Homo sapiens
?