Table 5. Biochemical Characterization of 5.
| Compound 5 | |
|---|---|
| IC50 BRPF2 (TR-FRET/Alpha Screen) [nM] | 67/97 |
| IC50 TAF1 BD2 (TR-FRET) [nM] | 8 |
| IC50 TAF1L BD2 (TR-FRET) [nM] | 106 |
| IC50 BRPF1 (TR-FRET/Alpha Screen) [nM] | 3150/2280 |
| IC50 BRPF3 (TR-FRET/Alpha Screen) [nM] | 5550/2450 |
| IC50 BRD4 BD1/BD2 (TR-FRET) [nM] | >15650/>20000 |
| IC50 CREBBP (Alpha Screen) [nM] | 1710 |
| Kd BRPF2 (ITC) [nM] | 45 |
| Kd TAF1 BD2 (ITC) [nM] | 17 |
| IC50 BRPF2 BD/H4 cellular [nM]a | 575 |
| IC50 TAF1 BD2/H4 cellular [nM]a | 970 |
| Selectivity Kinases (300 entries) | >10000 |
| Selectivity LeadProfilingScreen (68 entries) | >10000 |
a
Determined using NanoBRET.