Assay Detail

CHEMBL5389576

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

Binding

Inhibition of PI3Kalpha H1047R mutant (unknown origin) using PI(4,5)P2:PS as substrate incubated in presence of ATP by ADP-Glo assay

ChEMBL ↗

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Target

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL4005) ↗

Open DB target context

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Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL4005) 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 alpha isoform

CHEMBL4005

Anchored from Assay target.

Protein identity Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha 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
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL4005) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein.

Ketcham JM, Harwood SJ, Aranda R, Aloiau AN, Bobek BM, Briere DM, Burns AC, Caddell Haatveit K, Calinisan A, Clarine J, Elliott A, Engstrom LD, Gunn RJ, Ivetac A, Jones B, Kuehler J, Lawson JD, Nguyen N, Parker C, Pearson KE, Rahbaek L, Saechao B, Wang X, Waters A, Waters L, Watkins AH, Olson P, Smith CR, Christensen JG, Marx MA.
J Med Chem (2024) 67 : 4936 -4949
PubMed 38477582 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	3	7.35	8.52

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2396661	ALPELISIB	4.0	1	8.52
CHEMBL5402470	—	—	1	7.14
CHEMBL5436038	—	—	1	6.39

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2396661	ALPELISIB	IC50	=	3.0	nM	8.52
CHEMBL5402470	—	IC50	=	73.0	nM	7.14
CHEMBL5436038	—	IC50	=	411.0	nM	6.39