Assay Detail

CHEMBL3855735

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding

Inhibition of PI3Kdelta in IgM-stimulated human Raji cells assessed as reduction in AKT phosphorylation at S473 incubated for 30 mins followed by stimulation with IgM for 30 mins by ELISA

ChEMBL ↗

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Target

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (CHEMBL3130) ↗

Open DB target context

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Loading context

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (CHEMBL3130) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform

CHEMBL3130

Anchored from Assay target.

Protein identity Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Cell Type	Raji
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (CHEMBL3130) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate.

Evans CA, Liu T, Lescarbeau A, Nair SJ, Grenier L, Pradeilles JA, Glenadel Q, Tibbitts T, Rowley AM, DiNitto JP, Brophy EE, O'Hearn EL, Ali JA, Winkler DG, Goldstein SI, O'Hearn P, Martin CM, Hoyt JG, Soglia JR, Cheung C, Pink MM, Proctor JL, Palombella VJ, Tremblay MR, Castro AC.
ACS Med Chem Lett (2016) 7 : 862 -867
PubMed 27660692 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	6.75	6.75

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3984425	EGANELISIB	2.0	1	6.75

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3984425	EGANELISIB	IC50	=	180.0	nM	6.75