GNE-781

Inhibitor of CREBBP, EP300

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe GNE-781 is in the process of SERP review.

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Information

CREBBP
EP300

Inhibitor

100 nM

Probe Availability:

In Vitro Validations

Uniprot ID: Q92793

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: IC 50

Potency Value: 0.94 nM

Potency Assay: Time-Resolved Fluorescence Resonance Energy Transfer Assays

PDB ID for probe-target interaction (3D structure): --

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

Off-Target Selectivity Assesments

Potency end-point : IC50 5.2 uM BRD4

Potency assay (off target): BromoScan, CEREP, KinomeScan

Probe Selectivity in Vitro:

BromoScan KD results >10 uM for all except BRD4 (5.3 nM), BRDT (4.9 uM); 5.1 uM BRD4(1) BRET Outside Target Family: CEREP @ 10 uM does not highlight any target inhibition, KinomeScan @ 1 uM reports no kinase inhibition.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 14 Apr 2021 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 19 Apr 2021 )