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Initial schistosomula screens of the 14 compounds and their intermediate analogues.

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posted on 19.10.2020, 17:33 by Helen Whiteland, Alessandra Crusco, Lisa W. Bloemberg, Jamie Tibble-Howlings, Josephine Forde-Thomas, Avril Coghlan, Patrick J. Murphy, Karl F. Hoffmann

A total of 120 mechanically transformed schistosomula were co-cultured with each compound, titrated at doses between 10 and 0.625 μM. Test plates were incubated at 37°C for 72 hrs in an atmosphere containing 5% CO2. At 72hrs, schistosomula were scored using the Roboworm platform for both motility and phenotype as previously described [17, 25]. A) Of the 14 compounds evaluated, two fell within the hit region. Z’ scores for motility and phenotype were 0.40079 and 0.56846 respectively. B) Further titration of the two hit compounds resulted in good compound effect being observed for compound 1 down to a concentration of 1.25 μM. Z´ scores for motility and phenotype were 0.37864 and 0.47882 respectively. *Average EC50 value across motility and phenotype is presented for each compound.

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