Both neurons with high response selectivity (left panel, n=62 DLPFC units) and neurons with low chosen value selectivity (right panel, n= 62 DLPFC units) show the effect found in Figure 5A.
Neurons with high chosen value selectivity (top panel, n=62 DLPFC units) show the effect found in Figure 5A, whereas neurons with low chosen value selectivity (bottom panel, n= 62 DLPFC units) do not.
Duplexes CMOD12 (three mismatches) and CMOD13 (four mismatches) were chosen for closer examination and achieved 11- and 23-fold selectivities, respectively (panels C and D of Figure 3, respectively).
A series of substituted benzofuropyrimidinones with pan-PIM activities and excellent selectivity against a panel of diverse kinases is described.
Three representative compounds (21, 33, and 34) were demonstrated to have good selectivity against a panel of 80 kinase assays.
The clinical candidate from this series, R1663, exhibits excellent selectivity against a panel of serine proteases and good pharmacokinetic properties in rats and monkeys.
Liu et al. discovered sixteen compounds with IC50 < 20 μM, three of which showed low micromolar inhibitory activities against p90 ribosomal S6 protein kinase 2 (RSK2) and exhibited <span class="lh">selectivity across a panel of related kinases using SHAFTS [23].
Further optimization using structure-based design led to inhibitors with pM affinity for FXIa, excellent selectivity against a panel of relevant serine proteases, and good potency in the activated partial thromboplastin time (aPTT) clotting assay.
The impact of the substituent at the 3-position of 2-oxindole core on the potency and selectivity against a panel of seven different cancer cell lines was examined.
PCM combines information from compounds and related targets, e.g. orthologs, in a single machine learning model [3,11], which enables the simultaneous modelling of chemical and biological information, and thus the prediction of compound affinity and selectivity across a panel of targets.
