MRTX1133

MRTX1133 : Inhibitor of KRAS G12D

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe MRTX1133 is in the process of SERP review.

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Information

KRAS (Mutant:G12D)

Inhibitor

up to 100 nM

Probe Availability:

In Vitro Validations

Uniprot ID: P01116

Target Class: Enzyme

Target SubClass: GTPase

Potency: Kd

Potency Value: ~0.0002 nM

Potency Assay: SPR

PDB ID for probe-target interaction (3D structure): 7RPZ

Target aliases:

GTPase KRas, RASK2, KRAS2, KRAS, RASK_HUMAN, c-Ki- ...

DOI Reference: 10.1021/acs.jmedchem.1c01688

Uniprot ID: P01116

Target Class: Enzyme

Target SubClass: GTPase

Potency: IC50

Potency Value: 5 nM

Potency Assay: AlphaLISA

PDB ID for probe-target interaction (3D structure): 7RPZ

Target aliases:

GTPase KRas, RASK2, KRAS2, KRAS, RASK_HUMAN, c-Ki- ...

DOI Reference: 10.1021/acs.jmedchem.1c01688

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay, off target (cells): pERK Activity of MRTX1133 was tested against a panel of KRASG12D Cell lines showing similar potencies up to 10 nM

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 8 Apr 2024 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

The MRTX1133 compound has been refined to have very high affinity for the G12D-specific mutant of KRAS (not other mutations of the protein). The compound is effective in preventing KRAS-dependent phosphorylation of ERK in cell culture and in mice. I note that off-target effects of the compound were not evaluated.

(last updated: 3 May 2024 )