AZD-7648

AZD-7648 : Inhibitor of PRKDC

Structure

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In Cells

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In Model Organisms

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Probe AZD-7648 is in the process of SERP review.

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Information

PRKDC

Inhibitor

up to 500 nM

Probe Availability:

In Vitro Validations

Uniprot ID: P78527

Target Class: Kinase

Target SubClass: PI3/PI4

Potency: IC50

Potency Value: 0.63 nM

Potency Assay: Measured by time-resolved fluorescence (TR-FRET) in a biochemical assay.

PDB ID for probe-target interaction (3D structure): 6T3C

Target aliases:

DNA-dependent protein kinase catalytic subunit, HY ...

DOI Reference: 10.1021/acs.jmedchem.9b01684

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Panel of 397 Kinases at Thermofisher

Probe Selectivity in Vitro:

Within target family - Only PI3 kinases had >50% inhibition at 1 μM. TR-FRET IC50 results: PI3Kγ 52 nM, PI3Kα 100 nM, PI3Kδ 760 nM, PI3Kβ 1200 nM. Outside target family - Screened in a diverse panel of 195 distinct molecular targets (receptors, ion channels, transporters, and enzymes), and no targets had activity within 100-fold of the primary target potency

Probe Selectivity in Cell:

Cell Selectivity versus Structurally Related PIKKs and PI3 Kinases: PI3Kγ (RAW-264, pAKT Thr308) IC50 1370 nM (15x)

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In Cell Rating

In Model Organisms

(last updated: 12 Apr 2022 )