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The cationic inhibitors 15, 16, 19, 20, and 30 were also much more selective (900 - 344,000) over human cells than the non-targeted neutral derivatives (selectivity >8-fold).
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For several derivatives, significant selectivity both over 5-HT1AR anD2R2R was found.
A large pool of derivatives, moderate selectivity, and cell membrane permeability are regarded as their advantages as tools in intact cell studies.
We are currently creating and testing the effects of JQ1 derivatives possessing selectivity for BRDT to extend the favorable therapeutic window of BRDT inhibition for male contraception.
Among synthesized, only the benzylsulfonyl derivative showed selectivity toward dGMIIb.
Most importantly, a chain length of eight carbons as in derivative 5 creates selectivity towards the KDM4 subfamily.
Synthetic derivatives showed excellent selectivity, such as compound 6m demonstrated a strong inhibition of EGFR (IC50 = 0.0032 μM), with selectivity of over 2000-fold otherother kinases.
Synthetic derivatives showed excellent selectivity, as they were toxic against only HCT116 cell line.
Optimized derivatives display high selectivity over IP, FP, and other EP receptor panels.
All these derivatives had high selectivity for c-myc G-quadruplex DNA over duplex DNA.
The initially identified tetralone derivatives showed complete selectivity for E. coli MetAP versus human MetAP-1 and MetAP-2.
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