Literature summary for 2.3.1.250 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.

Search for more literature for 2.3.1.250

Inhibitors

Inhibitors	Comment	Organism
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-(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-(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-cyclopentyl-4-oxo-3,4-dihydroquinazolin-2-yl)thio)-N-(4-(dimethylamino)phenyl)acetamide	-	Danio rerio
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-((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-((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-((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-[(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-[(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-[(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-[(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-[(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-[(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-[(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-[(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-[(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
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
6-oxo-N-(2-oxo-2-(thiazol-2-ylamino)ethyl)-1-phenyl-1,6-dihydropyridazine-3-carboxamide	-	Danio rerio
ethyl 4-(2-((4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio)acetamido)benzoate	-	Danio rerio
LGK974	-	Danio rerio
additional information	identification, synthesis, and analysis of small molecule enzyme IWP inhibitors, i.e. inhibitors of Wnt production, structure-activity relationship, overview	Danio rerio
N-(2-((6-methoxybenzo[d]thiazol-2-yl)amino)-2-oxoethyl)-3-(4-methoxyphenyl)-4-oxo-3,4-dihydrophthalazine-1-carboxamide	-	Danio rerio
N-(2-((6-methoxybenzo[d]thiazol-2-yl)amino)-2-oxoethyl)-6-oxo-1-phenyl-1,6-dihydropyridine-3-carboxamide	-	Danio rerio
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
N-(4-(dimethylamino)phenyl)-2-((4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio)acetamide	-	Danio rerio
N-(4-butylphenyl)-2-((4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio)acetamide	-	Danio rerio
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
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
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
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
N-(biphenyl-2-yl)-2-[(4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]acetamide	-	Danio rerio
N-(biphenyl-3-yl)-2-[(4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]acetamide	-	Danio rerio
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
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
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
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
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

Organism	UniProt	Comment	Textmining
Danio rerio	-	-	-

Synonyms

Synonyms	Comment	Organism
PORCN	-	Danio rerio

General Information

General Information	Comment	Organism
evolution	the enzyme is a member of the membrane-bound O-acyltransferase family proteins	Danio rerio
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
additional information	structure-activity relationship, overview	Danio rerio
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