CAMONSERTIB

CAMONSERTIB : Inhibitor of ATR

Structure

SERP Rating

Probe CAMONSERTIB is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

Inhibitor

up to 100 nM

In Vitro Validations

Uniprot ID: Q13535

Target Class: Kinase

Target SubClass: PI3/PI4

Potency: IC50

Potency Value: 1.0 nM

Potency Assay: ATR kinase assay at 3 µM ATP

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

Target aliases:

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

DOI Reference: 10.1158/1535-7163.MCT-21-0615

Uniprot ID: Q13535

Target Class: Kinase

Target SubClass: PI3/PI4

Potency: Ki

Potency Value: 0.022 nM

Potency Assay: ATR/ATRIP Biochemical assay

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

Target aliases:

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

DOI Reference: 10.1158/1535-7163.MCT-21-0615

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): RP-3500 is highly selective for ATR with 30-fold selectivity over mammalian target of rapamycin (mTOR) and more than 2,000-fold selectivity over ataxia telangiectasia mutated (ATM), DNA-dependent protein kinase (DNA-PK), and phosphatidylinositol 3-kinase alpha (PI3Kα) kinases. At 300 nmol/L, RP-3500 showed no binding activity to more than 300 kinases outside of the PIKK family. Weak binding was detected to five PIKK or PI3K family members.

Potency assay, off target (cells): Specific cell-based kinase assays were developed to determine the intracellular inhibitory activity within the PIKK family. In each assay, RP-3500 showed weak inhibition of PIKK family cellular kinase activity resulting in 30-fold selectivity over mTOR and more than 2,000-fold selectivity over ATM, DNA-PK, and PI3Kα kinases

I have extra information to add

SERP ratings and comments

No SERP comments found for CAMONSERTIB