GDC-0879

ATP-competitive inhibitor of BRAF (Mutant:V600E)

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(2 ratings)

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Information

BRAF (Mutant:V600E)

ATP-competitive inhibitor

1-300 nM

Probe Availability:

In Vitro Validations

Uniprot ID: P15056

Target Class: Kinase

Target SubClass: TKL

Potency: IC50

Potency Value: 63 nM

Potency Assay: In vitro substrate phosphorylation assay

PDB ID for probe-target interaction (3D structure): 4MNF

Target aliases:

Serine/threonine-protein kinase B-raf, RAFB1, BRAF ...

DOI Reference: 10.1158/0008-5472.CAN-08-3563

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): 1 uM GDC-0879 was tested against 140 kinases and exhibited >90% inhibitory activity against RAF kinases and >50% inhibitory activity against CSNK1D.

Probe Selectivity in Vitro:

1 uM GDC-0879 was tested against 140 kinases and exhibited >90% inhibitory activity against RAF kinases and >50% inhibitory activity against CSNK1D.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

The chemotype for this probe is very selective for RAF but is expected to inhibit both mutant and wild-type forms as well as c-RAF. The fact that it is orally bioavailable makes it a very useful probe to interrogate RAF biology.

(last updated: 3 Jun 2016 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 21 Nov 2016 )

SERP Ratings

In Cell Rating

(last updated: 12 Dec 2016 )