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更新時(shí)間：2019-06-26

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產(chǎn)品活性：GNE-049 是一種高效的選擇性 CBP 抑制劑，在 TR-FRET 實(shí)驗(yàn)中 IC50 為 1.1 nM。GNE-049 還抑制 BRET 和 BRD4 (1)，IC50 分別為 12 nM 和 4200 nM。

研究領(lǐng)域：Epigenetics

作用靶點(diǎn)：Epigenetic Reader Domain | Histone Acetyltransferase

In Vitro: GNE-049 is selected for further profiling as it has the best balance of liver microsomes (LM) stability, selectivity, and cellular potency GNE-049 has excellent potency in the BRET cellular assay and, in an orthogonal measure of the target engagement, GNE-049 is shown to inhibit the expression of MYC (MV4-11 cell line) with an EC50 of 14 nM.

In Vivo: GNE-049 demonstrates acceptable PK in mouse, rat, dog, and monkey. Determination of potency versus a selection of bromodomains revealed that GNE-049 is selective for CBP/P300 and, importantly, quite selective (3820-fold) over BRD4(1). GNE-049 is further evaluated in a rat single dose (30-250 mg/kg QD) toxicokinetic study. Adverse central nervous system (CNS)-related signs (e.g., marked hyperactivity and vocalization) are observed in several of the rats at the 250 mg/kg dose level. Furthermore, at the 250 mg/kg dose level, the ratio of the unbound drug concentration in brain to unbound drug concentration in plasma (Kp,uu) 3 h post dose is determined to be 0.43, indicating that GNE-049 is penetrating into the CNS and potentially resulting in the observed toxicity.

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