GNE-064 (compound 5) is a selective, orally active and highly soluble inhibitor of SMARCA4 , SMARCA2 and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC 50 of 0.035 μM and inhibits SMARCA2 with an EC 50 of 0.10 μM. GNE-064 possess K d s with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of agent synthesis.
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