Probe Selectivity in Vitro:
The AlphaScreen assays were employed to screen NVS-MLLT-1 against a panel of bromodomains. NVS-MLLT-1 shows potent activity on MLLT1/3 whilst being selective for YEATS2/4. NVS-MLLT-1 shows selectivity across all bromodomains (CERC2 IC50 > 40 μM).
Outside target family: NVS-MLLT-1 shows no activity on kinases tested, NVS-MLLT-1 has some activity on ACES and E3 binding. NVS-MLLT-C (control Compound) shows no activity in a panel of kinases, and no activities on other targets tested.