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Sunitinib was the most selective inhibitor, followed by PKC421 and CEP701.
Compound 8 was found most selective MAO-A inhibitor while compound 20 was found most selective inhibitor for MAO-B isoform.
The α-conotoxin (α-CTx) LvIA has been identified as the most selective inhibitor of α3β2 nAChRs known to date, and it can distinguish the α3β2 nAChR subtype from the α6/α3β2β3 and α3β4 nAChR subtypes.
Compound 4f (3- biphen-3-yl -2- 4-fluorophenyl -6-phenylthioimidazo[1,2-a]pyridine) proved to be the most selective inhibitor of BVDV replication and showed no or only marginal cross-resistance with known inhibitors of pestivirus replication.
In addition, MD simulations of the NS2B/NS3 protease of WNV and DV complexed with Bz-Nle-Lys-Arg-Ala-H (most selective inhibitor, Ki = 193.00 μM for DV and IC50 = 4.6 μM for WNV) [2, 3] were also carried out.
A-385358 was rationally designed to be almost 100-fold more selective for Bcl-XL over Bcl-2, and is the most selective inhibitor for Bcl-XL to date.
Similar(54)
Consistent with in silico and in vitro analyses, they conclude that quinalizarin not only is one of the most selective inhibitors of CK2 but is also able to discriminate between the isolated CK2 catalytic subunit and CK2 holoenzyme.
In conclusion, the data presented provide the clear-cut demonstration that quinalizarin is one of most selective inhibitors of protein kinase CK2, with a high Gini coefficient and the lowest hit rate ever reported.
Here, by profiling quinalizarin on a larger panel of 140 kinases we reach the conclusion that quinalizarin is one of the most selective inhibitors of CK2, superior to the first-in-class CK2 inhibitor, CX-4945, now in clinical trials for the treatment of cancer.
1400W is considered today the most selective NOS2 inhibitor, as it inhibits NOS2 with 5000- and 200-folds greater potency than NOS3 and NOS1, respectively [20].
Among them, SNS-032 (BMS-387032) appears to be the most selective CDK9 inhibitor.
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