GFH018

GFH018 : Inhibitor of TGFB1

Structure

SERP Rating

Probe GFH018 is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

TGFB1

Inhibitor

up to 1 uM

In Vitro Validations

Uniprot ID: P01137

Target Class: Catalytic receptor

Target SubClass: Transforming Growth Factor

Potency: IC50

Potency Value: 40 nM

Potency Assay: Biochemical assay

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

Target aliases:

Transforming growth factor beta-1 proprotein, TGFB ...

DOI Reference: 10.1021/acs.jmedchem.5c00121

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity assessment of GFH018 on the ALK family and selected kinases was performed at a concentration of 1 μM, the residual activity of 4 kinases (ALK4, LCK, RIPK2, and TNIK) was less than 50%.The highest inhibition was observed for ALK4, which shares a high degree of homology with TGF-βR1 in the kinase domain. GFH018 was also examined in a human GPCR selectivity panel of 22 targets and was found to be inactive against these GPCR receptors.

I have extra information to add

SERP ratings and comments

No SERP comments found for GFH018