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Literature summary extracted from

  • Wang, X.; Moon, J.; Dodge, M.E.; Pan, X.; Zhang, L.; Hanson, J.M.; Tuladhar, R.; Ma, Z.; Shi, H.; Williams, N.S.; Amatruda, J.F.; Carroll, T.J.; Lum, L.; Chen, C.
    The development of highly potent inhibitors for porcupine (2013), J. Med. Chem., 56, 2700-2704.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.250 2-((3,6-dimethyl-4-oxo-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio)-N-(6-methylbenzo[d]thiazol-2-yl)acetamide
-
 Danio rerio
2.3.1.250 2-((3-(3-methoxyphenyl)-4-oxo-3,4,4a,6,7,7a-hexahydrothieno[3,2-d]pyrimidin-2-yl)thio)-N-(6-methylbenzo[d]thiazol-2-yl)acetamide
-
 Danio rerio
2.3.1.250 2-((3-(4-fluorophenyl)-4-oxo-3,4,4a,6,7,7a-hexahydrothieno[3,2-d]pyrimidin-2-yl)thio)-N-(6-methylbenzo[d]thiazol-2-yl)acetamide
-
 Danio rerio
2.3.1.250 2-((3-cyclopentyl-4-oxo-3,4-dihydroquinazolin-2-yl)thio)-N-(4-(dimethylamino)phenyl)acetamide
-
 Danio rerio
2.3.1.250 2-((4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio)-N-(4-(piperidin-1-yl)phenyl)acetamide
-
 Danio rerio
2.3.1.250 2-((4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio)-N-(4-phenylthiazol-2-yl)acetamide
-
 Danio rerio
2.3.1.250 2-((4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio)-N-(5-(prop-1-en-2-yl)pyridin-2-yl)acetamide
-
 Danio rerio
2.3.1.250 2-((4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio)-N-(5-phenylthiazol-2-yl)acetamide
-
 Danio rerio
2.3.1.250 2-[(4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(5-phenylpyridin-2-yl)acetamide
-
 Danio rerio
2.3.1.250 2-[(4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(5-phenylpyrimidin-2-yl)acetamide
-
 Danio rerio
2.3.1.250 2-[(4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(6-phenylpyridin-3-yl)acetamide
-
 Danio rerio
2.3.1.250 2-[(4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-[4-(pyridin-2-yl)phenyl]acetamide
-
 Danio rerio
2.3.1.250 2-[(4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-[4-(pyridin-3-yl)phenyl]acetamide
-
 Danio rerio
2.3.1.250 2-[(4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-[4-(pyridin-4-yl)phenyl]acetamide
-
 Danio rerio
2.3.1.250 2-[(4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-[5-(pyrimidin-5-yl)pyridin-2-yl]acetamide
-
 Danio rerio
2.3.1.250 2-[(4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-[5-(thiophen-2-yl)pyridin-2-yl]acetamide
-
 Danio rerio
2.3.1.250 2-[(4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-[5-(thiophen-3-yl)pyridin-2-yl]acetamide
-
 Danio rerio
2.3.1.250 5-((3aR,4R,6aS)-6-(4-(2-((2-((6-methylbenzo[d]thiazol-2-yl)amino)-2-oxoethyl)thio)-4-oxo-4a,6,7,7a-tetrahydrothieno[3,2-d]pyrimidin-3(4H)-yl)phenethyl)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanoic acid
-
 Danio rerio
2.3.1.250 6-oxo-N-(2-oxo-2-(thiazol-2-ylamino)ethyl)-1-phenyl-1,6-dihydropyridazine-3-carboxamide
-
 Danio rerio
2.3.1.250 ethyl 4-(2-((4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio)acetamido)benzoate
-
 Danio rerio
2.3.1.250 LGK974
-
 Danio rerio
2.3.1.250 additional information identification, synthesis, and analysis of small molecule enzyme IWP inhibitors, i.e. inhibitors of Wnt production, structure-activity relationship, overview Danio rerio
2.3.1.250 N-(2-((6-methoxybenzo[d]thiazol-2-yl)amino)-2-oxoethyl)-3-(4-methoxyphenyl)-4-oxo-3,4-dihydrophthalazine-1-carboxamide
-
 Danio rerio
2.3.1.250 N-(2-((6-methoxybenzo[d]thiazol-2-yl)amino)-2-oxoethyl)-6-oxo-1-phenyl-1,6-dihydropyridine-3-carboxamide
-
 Danio rerio
2.3.1.250 N-(3,3'-bipyridin-6-yl)-2-[(4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]acetamide
-
 Danio rerio
2.3.1.250 N-(4-(dimethylamino)phenyl)-2-((4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio)acetamide
-
 Danio rerio
2.3.1.250 N-(4-butylphenyl)-2-((4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio)acetamide
-
 Danio rerio
2.3.1.250 N-(5-ethoxypyridin-2-yl)-2-((4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio)acetamide
-
 Danio rerio
2.3.1.250 N-(6-methoxyquinolin-2-yl)-2-((4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio)acetamide
-
 Danio rerio
2.3.1.250 N-(6-methylbenzo[d]thiazol-2-yl)-2-((4-oxo-3-phenyl-3,4,4a,6,7,7a-hexahydrothieno[3,2-d]pyrimidin-2-yl)thio)acetamide
-
 Danio rerio
2.3.1.250 N-(benzo[d]thiazol-2-yl)-2-((3-ethyl-6-methyl-4-oxo-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio)acetamide
-
 Danio rerio
2.3.1.250 N-(biphenyl-2-yl)-2-[(4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]acetamide
-
 Danio rerio
2.3.1.250 N-(biphenyl-3-yl)-2-[(4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]acetamide
-
 Danio rerio
2.3.1.250 N-([1,1'-biphenyl]-4-yl)-2-((4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio)acetamide
-
 Danio rerio
2.3.1.250 N-[5-(furan-2-yl)pyridin-2-yl]-2-[(4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]acetamide
-
 Danio rerio
2.3.1.250 N-[5-(furan-2-yl)pyrimidin-2-yl]-2-[(4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]acetamide
-
 Danio rerio
2.3.1.250 N-[5-(furan-3-yl)pyridin-2-yl]-2-[(4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]acetamide
-
 Danio rerio
2.3.1.250 N-[5-(furan-3-yl)pyrimidin-2-yl]-2-[(4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]acetamide
-
 Danio rerio

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.250 Danio rerio
-
-
-

Synonyms

EC Number Synonyms Comment Organism
2.3.1.250 PORCN
-
 Danio rerio

General Information

EC Number General Information Comment Organism
2.3.1.250 evolution the enzyme is a member of the membrane-bound O-acyltransferase family proteins Danio rerio
2.3.1.250 malfunction compromised Porcn activity commonly results in developmental disorders including focal dermal hypoplasia (Goltz syndrome) whereas hyperactivity of Porcn is associated with cancerous cell growth. Enzyme inhibition by small molecule IWP inhibitors affect Wnt-dependent developmental processes including zebrafish posterior axis formation and kidney tubule formation Danio rerio
2.3.1.250 additional information structure-activity relationship, overview Danio rerio
2.3.1.250 physiological function the enzyme catalyzes the palmitoylation of Wnt proteins to enable its exit from the secretory pathway and subsequent activation of cellular responses Danio rerio