Assay Detail

CHEMBL4724092

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Binding

Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate in presence of ATP measured after 45 mins by HTRF assay relative to control

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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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
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 Potent and Selective PI3Kδ Inhibitor (S)-2,4-Diamino-6-((1-(7-fluoro-1-(4-fluorophenyl)-4-oxo-3-phenyl-4H-quinolizin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile with Improved Pharmacokinetic Profile and Superior Efficacy in Hematological Cancer Models.

Shukla MR,Patra S,Verma M,Sadasivam G,Jana N,Mahangare SJ,Vidhate P,Lagad D,Tarage A,Cheemala M,Kulkarni C,Bhagwat S,Chaudhari VD,Sayyed M,Pachpute V,Phadtare R,Gole G,Phukan S,Sunkara B,Samant C,Shingare M,Naik A,Trivedi S,Marisetti AK,Reddy M,Gholve M,Mahajan N,Sabde S,Patil V,Modi D,Mehta M,Nigade P,Tamane K,Tota S,Goyal H,Volam H,Pawar S,Ahirrao P,Dinchhana L,Mallurwar S,Akarte A,Bokare A,Kanhere R,Reddy N,Koul S,Dandekar M,Singh M,Bernstein PR,Narasimham L,Bhonde M,Gundu J,Goel R,Kulkarni S,Sharma S,Kamboj RK,Palle VP
J Med Chem (2020) 63 : 14700 -14723
PubMed 33297683 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	8.77	9.05
IC90	1	-	-

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3805348	—	—	1	9.05
CHEMBL4756563	—	—	2	8.48

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3805348	—	IC50	=	0.9	nM	9.05
CHEMBL4756563	—	IC50	=	3.3	nM	8.48
CHEMBL4756563	—	IC90	=	28.1	nM	-