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Fig. 1 | Parasites & Vectors

Fig. 1

From: Screening of the ‘Stasis Box’ identifies two kinase inhibitors under pharmaceutical development with activity against Haemonchus contortus

Fig. 1

Primary screen of 400 individual compounds from the ‘Stasis Box’ from the Medicines for Malaria Venture (MMV) at a concentration of 20 μM identified compound SNS-032 (MMV690767) to inhibit the motility of exsheathed third-stage larvae (xL3) of Haemonchus contortus (at 72 h) by ≥ 70% compared with negative (LB* + 0.5% dimethyl sulfoxide; DMSO) and positive controls (monepantel). Another compound, AG-1295 (MMV079840), was found to inhibit xL3 motility by ~50%, displaying a “coiled” phenotype based on visual inspection of video recordings (see Additional file 1). Other compounds with apparent inhibition of ≥ 50% did not exhibit a characteristic phenotype by visual inspection. Each data point represents the mean of a triplicate (± standard error of the mean, SEM). Chemical structures and physiochemical properties of ‘hit’ compounds SNS-032 and AG-1295 are indicated. Abbreviations: Mw, molecular weight; PSA, polar surface area; FRB, freely rotating bonds; HBD, hydrogen bond donor; HBA, hydrogen bond acceptor; ARC, aromatic ring count; cLogP, calculated partition coefficient

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