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. Author manuscript; available in PMC: 2020 Jun 24.
Published in final edited form as: Angew Chem Int Ed Engl. 2016 Aug 17;55(38):11382–11386. doi: 10.1002/anie.201603928

Table 3. Profile of 16 (GSK8814) and its enantiomer 17 (GSK8815). For statistics see Table S1b, Supporting Information.

16 17
ATAD2 pKd ITC 8.1 5.5
ATAD2 BROMOScan pKi 8.9 n.d.[a]
ATAD2 TR-FRET pIC50 7.3 5.5
ATAD2B TR-FRET pIC50 7.7 5.5
BRD4 tandem pKd ITC <5.3 <5.3
BRD2 BD1/ BD2 TR-FRET pIC50 ≤4.4/<4.3 ≤4.9/≤4.6
BRD3 BD1/ BD2 TR-FRET pIC50 <4.3/<4.3 ≤4.6/≤4.7
BRD4 BD1/ BD2 TR-FRET pIC50 ≤4.5/<3.3 ≤4.4/≤4.7
BRDT BD1/ BD2 TR-FRET pIC50 ≤4.3/<4.3 ≤4.5/≤4.4
CLND solubility [μM] >439 326
[a]

n.d.=not determined.