Idelalisib

Idelalisib : Inhibitor of PIK3CD

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(0 ratings)

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Information

PIK3CD

Inhibitor

up to 1 uM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: O00329

Target Class: Kinase

Target SubClass: PI3/PI4 family

Potency: IC50

Potency Value: 2.5 nM

Potency Assay: Enzymatic assay using recombinant protein at Km ATP

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

Target aliases:

Phosphatidylinositol 4,5-bisphosphate 3-kinase cat ...

DOI Reference: 10.1182/blood-2010-03-275305

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay, off target (cells): In cell-based assays, CAL-101 had 240- to 2500-fold selectivity for p110δ over the other class I PI3K isoforms.

Potency assay (off target): 40- to 300-fold more selective for p110δ relative to other PI3K class I enzymes (IC50 p110δ = 2.5nM; p110α, p110β, and p110γ IC50 were 820, 565, and 89nM, respectively, measured at Km ATP for respective kinase in an enzymatic assay); greater selectivity (400- to 4000-fold) was seen against related kinases C2β, hVPS34, DNA-PK, and mTOR, whereas no activity was observed against a panel of 402 diverse kinases at 10μM (Ambit KinomeScan, data not shown).

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

This compound is likely to be a pan-p110 inhibitor unless used at <100 nM in cells

(last updated: 3 Jul 2023 )

SERP Ratings

In Cell Rating

(last updated: 18 Jul 2023 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

This is a highly selective inhibitor.

(last updated: 17 Jun 2024 )