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Message: Re: Thoughts?
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Apr 06, 2021 12:51AM

Sorry for awful formatting above.

Key reason i posted was in this paragraph....

At the time this work was carried out, there were no highly potent BD2-selective inhibitors known. The best-studied molecule reported to show bias in favor of BD2 was RVX-208 (Figure 1), which has a Kd of 8.9 μM against BD1 and 300 nM against BD2 by ITC, a selectivity of approximately 30-fold.(33) Independent ITC measurements showed greater potency but lower selectivity (Kd of 1.1 μM for BRD4 BD1 and 135 nM for BRD4 BD2).(27) We have subsequently reported a series of quinoxaline-based inhibitors such as GSK340, which show greater potency and selectivity (Kd in the Discoverx BROMOscan assays of 1.5 μM against BRD4 BD1 and 7 nM against BRD4 BD2).(29) Very recently, ABBV-744 was reported as a nanomolar BD2 inhibitor and clinical candidate with >290-fold selectivity over the BD1 domains of BRD2/3/4.(34,35)

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