NUAK1-In-10i

NUAK1-In-10i : Inhibitor of NUAK1

Structure

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Information

NUAK1

Inhibitor

up to 10 µM

In Vitro Validations

Uniprot ID: O60285

Target Class: Kinase

Target SubClass: CAMK

Potency: IC50

Potency Value: 0.49 nM

Potency Assay: Biochemical Kinase Assay (TR-FRET)

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

Target aliases:

NUAK family SNF1-like kinase 1, OMPHK1, KIAA0537, ...

DOI Reference: 10.1021/acs.jmedchem.5c03079

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Cpd 10i activity was profiled against a panel of 416 human kinases via the ADP-Glo or HTRF assay @ 1 uM.

Probe Selectivity in Vitro:

Only nine wild-type kinases were inhibited >90% by cpd 10i, namely PDGFRβ, TNK1, RET, NUAK1, KDR, QIK, FLT3, NUAK2, and JAK3. Selective against NUAK2 541x and JAK3 459x.

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