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 |
n.d.=not determined.