HDM2004

HDM2004 : Inhibitor of MAP4K1

Structure

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Information

MAP4K1

Inhibitor

up to 1 uM

In Vitro Validations

Uniprot ID: Q92918

Target Class: Kinase

Target SubClass: STE

Potency: IC50

Potency Value: 1.89 nM

Potency Assay: ADP-Glo kinase assay

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

Target aliases:

Mitogen-activated protein kinase kinase kinase kin ...

DOI Reference: 10.1016/j.ejmech.2026.118708

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Kinase profiling screening against a panel of 60 wild-type kinases was conducted under a concentration of 1 μM.

Probe Selectivity in Vitro:

HDM2004 displayed moderate kinome selectivity. Potent “off target” kinase hits mainly include ROCK1, JAK3, JNK1, CLK1 and LCK, AXL and PKD2.

Potency assay (off target): Screening HDM2004 against a Safety Panel of 47 targets, including receptors, enzymes, kinases, and transporters relevant to human safety pharmacology.

Probe Selectivity in Vitro:

At a screening concentration of 1 μM, HDM2004 inhibited ROCK1 (94.04% inhibition), VEGFR2 (91.39%), and LCK (78.25%), with no significant inhibition detected against the other profiled proteins. The IC50 values of HDM2004 against ROCK1, VEGFR2, and LCK were determined to be 230.0 nM, 116.7 nM, and 300.1 nM, respectively.

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