Literature summary for 2.7.11.21 extracted from

Long, T.; Neitz, R.J.; Beasley, R.; Kalyanaraman, C.; Suzuki, B.M.; Jacobson, M.P.; Dissous, C.; McKerrow, J.H.; Drewry, D.H.; Zuercher, W.J.; Singh, R.; Caffrey, C.R.
Structure-bioactivity relationship for benzimidazole thiophene inhibitors of polo-like kinase 1 (PLK1), a potential drug target in Schistosoma mansoni (2016), PLoS Negl. Trop. Dis., 10, e0004356 .

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Inhibitors

Inhibitors	Comment	Organism	Structure
(4E)-5-methyl-4-[[(2-methylbenzoyl)oxy]imino]-2-(propan-2-yl)cyclohexa-2,5-dien-1-one	poloxin	Schistosoma mansoni
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[5-(1-methyl-1H-pyrrol-3-yl)-1H-benzo[3,4]cyclobuta[1,2-d]imidazol-1-yl]thiophene-2-carboxamide	GSK580432A, little inhibitory activity	Schistosoma mansoni
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[5-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1H-benzo[3,4]cyclobuta[1,2-d]imidazol-1-yl]thiophene-2-carboxamide	GSK641502A	Schistosoma mansoni
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-(pyridin-4-yl)-1H-benzo[3,4]cyclobuta[1,2-d]imidazol-1-yl]thiophene-2-carboxamide	GSK483724A	Schistosoma mansoni
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzo[3,4]cyclobuta[1,2-d]imidazol-1-yl]thiophene-2-carboxamide	GSK571989A	Schistosoma mansoni
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzo[3,4]cyclobuta[1,2-d]imidazol-1-yl]thiophene-2-carboxamide	GSK579289A	Schistosoma mansoni
5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzo[3,4]cyclobuta[1,2-d]imidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide	GSK326090A	Schistosoma mansoni
BI2536	-	Schistosoma mansoni
BI6727	-	Schistosoma mansoni
GSK461364	-	Schistosoma mansoni
GW843682X	little inhibitory activity	Schistosoma mansoni
HMN-214	little inhibitory activity	Schistosoma mansoni
methyl 5-(5,6-dimethoxy-1H-benzo[3,4]cyclobuta[1,2-d]imidazol-1-yl)-3-[[2-(trifluoromethyl)phenyl]methoxy]thiophene-2-carboxylate	GSK1030058A	Schistosoma mansoni
additional information	GSK479719A, albendazole, albendazole sulfoxide, MLN0905, HMN-214 and SBE13 display no inhibitory activity	Schistosoma mansoni
ON01910	little inhibitory activity	Schistosoma mansoni
TAK960	little inhibitory activity	Schistosoma mansoni
thymoquinone	-	Schistosoma mansoni

Organism

Organism	UniProt	Comment	Textmining
Schistosoma mansoni	Q5UES2	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
adult	-	Schistosoma mansoni	-
sporocyst	-	Schistosoma mansoni	-

Synonyms

Synonyms	Comment	Organism
Plk1	-	Schistosoma mansoni
Polo-like kinase 1	-	Schistosoma mansoni

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Release 2023.1 (January 2023)