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In coagulation assays (prothrombin time, activated partial thromboplastin time and thrombin time) in vitro, most compounds demonstrated excellent activities to promote blood coagulation.
Antibacterial bioassay results indicated that most compounds demonstrated good inhibitory effect antibacterial bioactivities against rice bacterial leaf blight and leaf streak.
Most compounds demonstrated statistically maximal proliferative effects by day 3 in these extensively hormone-stripped serum conditions.
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Most compound demonstrated good oral exposure, with compound 32 exhibited the highest AUC(0 5h) as well as a high Cmax (∼13-fold above the 3D7 potency).
The most potent compounds demonstrated selectivity towards isoform I and affinities of 0.5 nM.
Notably, two of the most potent compounds demonstrated nanomolar-level cell-based potency and limited toxicity.
It was found that the most active compounds demonstrated the best binding scores in the active site of EGFR, which may clarify their high inhibition profile.
Most of the compounds demonstrated surface anaesthetic activity higher than that of lidocaine, ropivacaine and bupivacaine.
The preliminary screening results indicated that most of the compounds demonstrated moderate to very good antibacterial and antifungal activities, comparable to the first-line drugs.
Results obtained from this screening showed that most of the compounds demonstrated antiviral activity, which ranged from weak through moderate to high effects, based on EC50 and SI values relative to their parent and reference drugs (Table 2).
Most of the new compounds demonstrated high in vitro antibacterial activity.
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CEO of Professional Science Editing for Scientists @ prosciediting.com