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This azepinoindole has excellent affinity for 5-HT2C (Ki 4.8 nM) and modest selectivity over 5-HT2A (∼4-fold).
Compounds were designed and synthesized to test our hypothesis and were found to be potent T-type calcium channel inhibitors with modest selectivity over L-type calcium channels.
Furthermore, profiling other members of this series identified compounds with >20-fold selectivity over PARP5a/TNKS1, and modest selectivity over PARP10, a closely related mono- ADP-ribosyl transferase.
(R)- 2 has modest selectivity over BRD4(1) [ KD=1.4 μ m (ITC)] and good selectivity over seven other phylogentically diverse BCPs.
One related compound, DBS (51), was identified as a 2.9 μM enzyme inhibitor, with modest selectivity over the human PyK [IC50 of 8 and 16.3 μM for human tissue HsRPyK (from erythrocyte) and HsM2PyK (from embryonic or tumor cells), respectively].
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NBI-59159 is a non-substrate inhibitor with modest selectivity for EAAT3 over EAAT1 (>10-fold) and EAAT2 (5-fold) 43, 44.
A binding protein for secretory phospholipase A2 has been identified which shows modest selectivity for sPLA2-1B over sPLA2-2A, alsoalso binds snake toxin phospholipase A2 216.
The chelator 1 shows modest selectivity for calcium ion (K11=6720 M−1) over magnesium ion (K11=564 M−1) by 1H NMR titration.
Additionally, analysis of toxic ROS-enhancing screening hits in isogenic, engineered "models" of tumorigenesis revealed several electrophilic compounds with modest selectivity for fully transformed cells over isogenic immortalized cells.
wortmannin is irreversible and shows modest selectivity between Class I and Class II PI3K, while LY294002 is reversible and selective for Class I compared to Class II PI3K.
The sensor 1 shows modest selectivity for 1,4-phenylenediacetate.
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