Assay Detail

CHEMBL5153874

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Binding

Inhibition of PI3Kgamma (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assay

ChEMBL ↗

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Target

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (CHEMBL3267) ↗

Open DB target context

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Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (CHEMBL3267) 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 gamma isoform

CHEMBL3267

Anchored from Assay target.

Protein identity Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma 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 gamma isoform (CHEMBL3267) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.

Hanan EJ, Braun MG, Heald RA, MacLeod C, Chan C, Clausen S, Edgar KA, Eigenbrot C, Elliott R, Endres N, Friedman LS, Gogol E, Gu XH, Thibodeau RH, Jackson PS, Kiefer JR, Knight JD, Nannini M, Narukulla R, Pace A, Pang J, Purkey HE, Salphati L, Sampath D, Schmidt S, Sideris S, Song K, Sujatha-Bhaskar S, Ultsch M, Wallweber H, Xin J, Yeap S, Young A, Zhong Y, Staben ST.
J Med Chem (2022) 65 : 16589 -16621
PubMed 36455032 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	1	7.74	7.74

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4650215	INAVOLISIB	4.0	1	7.74

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4650215	INAVOLISIB	Ki	=	18.2	nM	7.74