CERALASERTIB

CERALASERTIB : Inhibitor of ATR

Structure

SERP Rating

In Cells

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In Model Organisms

(1 ratings)

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Probe CERALASERTIB is in the process of SERP review.

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Information

Inhibitor

up to 1 uM

Probe Availability:

In Vitro Validations

Uniprot ID: Q13535

Target Class: Kinase

Target SubClass: PI3/PI4

Potency: IC50

Potency Value: 1 nM

Potency Assay: Biochemical assay using 32P radioactive assays

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

Target aliases:

Serine/threonine-protein kinase ATR, FRP1, ATR, AT ...

DOI Reference: 10.18632/oncotarget.6247

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): AZD6738 was screened against a 71 kinase panel including related PI3K and protein PI3K-like kinases (ATM, DNA-PK and mTOR) in in vitro isolated enzyme assays using 32P radioactive assays. Kinase selectivity was also determined using active-site dependent competition binding assays against 442 targets at 1 μM AZD6738 with only PI3KC2G showing any significant inhibition (20%) AZD-6738 showed excellent selectivity, with inhibition of ∼60% for PIK3C2G and CLK4 (at 1 μM) and <50% inhibition for the remaining 407 kinases tested.

Potency assay, off target (cells): Selectivity was assessed in cells against mTOR, PI3Kalpha, ATM, DNA-PK with IC50s >2 uM.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

This late phase clinical asset is an excellent probe for investigating pharmacology for ATR inhibition. It's use alongside other probe compounds with differing chemotypes, such as camonsertib, can help confirm on-target vs off-target pharmacology, though the molecule appears highly selective, reducing the risk of observed off-target pharmacology.

(last updated: 5 Mar 2024 )