AZ3246

AZ3246 : Inhibitor of MAP4K1

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe AZ3246 is in the process of SERP review.

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Information

MAP4K1

Inhibitor

up to 100 nM
Reviewer recommended concentration: 200-500 nM

In Vitro Validations

Uniprot ID: Q92918

Target Class: Kinase

Target SubClass: STE

Potency: IC50

Potency Value: <3 nM

Potency Assay: ADP-Glo assay

PDB ID for probe-target interaction (3D structure): 9H8F

Target aliases:

Mitogen-activated protein kinase kinase kinase kin ...

DOI Reference: 10.1021/acs.jmedchem.4c02631

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): AZ3246 exhibits exquisite kinome selectivity: in a Thermo-Fisher kinase panel of 357 kinases, 100 nM of 24 hits only HPK1 and MYLK at >80% inhibition.

Potency assay, off target (cells): Chemoproteomics data from physiologically relevant cell lysates also demonstrated that AZ3246 is highly selective for HPK1 over other kinases to which it binds: STK3, STK4, and TNIK.

Potency assay (off target): The compound is neither a Cyp inhibitor nor an inducer and is also clean in hERG and other cardiac ion channel assays.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 18 Mar 2025 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 1 Apr 2025 )