Inhibitor of CREBBP, EP300



Protein target names: CREBBP, EP300

Mechanism of action: Inhibitor

Recommended in-cell concentration:
100 nM

In Vitro Validations

Uniprot ID: Q92793
Target Class: Epigenetic
Target SubClass: Bromodomain
Potency: IC 50
Potency Value: 1.1 nM
Potency Assay: Time-Resolved Fluorescence Resonance Energy Transfer Assays
PDB ID for probe-target interaction (3D structure): 5W0L
Structure-activity relationship: yes
Target aliases:
CREB-binding protein, CBP, CREBBP, CBP_HUMAN, Prot ...

DOI Reference: 10.1021/acs.jmedchem.7b00796

In Cell Validations

In Vivo Data

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SERP ratings and comments

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

GNE-049 has been studied in various cellular assays and is a potent, selective, cell-penetrant probe. It has also been evaluated in preliminary PK studies in 4 species (mouse, rat, dog, cyno) and studied in preliminary high dose rat TK up to 250 mg/kg, at which dose adverse CNS-related signs were observed. Kpuu 3h post dose was 0.43. A second probe, GNE-781 (cpd 19 in the same paper) has a similar profile to GNE-049, but with higher polar surface area and no CNS penetration. Both probes are high quality, the 2nd probe GNE-781 has more published in vivo data, and unless there is a need for CNS penetration, then should be used in preference to this probe GNE-049. However, both are high quality probes.

(last updated: 24 Mar 2021 )