PF-07265028

PF-07265028 : Inhibitor of MAP4K1

Structure

SERP Rating

Probe PF-07265028 is in the process of SERP review.

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Information

MAP4K1

Inhibitor

up to 100 nM

In Vitro Validations

Uniprot ID: Q92918

Target Class: Kinase

Target SubClass: STE

Potency: Ki

Potency Value: <0.05 nM

Potency Assay: Biochemical assay (chelation-enhanced fluorescence (CHEF) PhosphoSens® method)

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

Target aliases:

Mitogen-activated protein kinase kinase kinase kin ...

DOI Reference: 10.1021/acs.jmedchem.4c01930

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): kinome selectivity was assessed using an Invitrogen 21-kinase mini-panel showed very high selectivity, with most off-targets showing windows over 100-fold. Only three kinases, TAOK1, MAP4K3 and MAP4K5, showed windows less than 50-fold.

Potency assay (off target): PF-07265028 was further profiled in the full Invitrogen panel (395 kinases, 402 assays, with follow up IC50 values measured for top inhibited kinases.

Probe Selectivity in Vitro:

2 out of 395 kinases (MAP4K5 and TAOK1) have the potential to be inhibited at a less than 30-fold window relative to HPK1

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SERP ratings and comments

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