Assay Detail

CHEMBL4016623

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

Functional

Ex vivo inhibition of PI3Kdelta in po dosed Balb/c mouse assessed as reduction in anti-mIgE-mediated increase in CD63 positive cells in whole blood pretreated for 1 hr followed by anti-mIgE activation for 30 mins by FACS analysis

ChEMBL ↗

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Target

Mus musculus (CHEMBL375) ↗

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Primary target Mus musculus

CHEMBL375

Anchored from Assay target.

Protein identity Mus musculus

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	Functional
Organism	Mus musculus
Confidence	1 — Organism
Curated By	Autocuration

Target

Mus musculus (CHEMBL375) ↗

Type	ORGANISM
Organism	Mus musculus

Publication

Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.

Liu Q, Shi Q, Marcoux D, Batt DG, Cornelius L, Qin LY, Ruan Z, Neels J, Beaudoin-Bertrand M, Srivastava AS, Li L, Cherney RJ, Gong H, Watterson SH, Weigelt C, Gillooly KM, McIntyre KW, Xie JH, Obermeier MT, Fura A, Sleczka B, Stefanski K, Fancher RM, Padmanabhan S, Rp T, Kundu I, Rajareddy K, Smith R, Hennan JK, Xing D, Fan J, Levesque PC, Ruan Q, Pitt S, Zhang R, Pedicord D, Pan J, Yarde M, Lu H, Lippy J, Goldstine C, Skala S, Rampulla RA, Mathur A, Gupta A, Arunachalam PN, Sack JS, Muckelbauer JK, Cvijic ME, Salter-Cid LM, Bhide RS, Poss MA, Hynes J, Carter PH, Macor JE, Ruepp S, Schieven GL, Tino JA.
J Med Chem (2017) 60 : 5193 -5208
PubMed 28541707 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	1	8.70	8.70
EC90	1	-	-
Inhibition	1	-	-

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4064666	—	—	3	8.70

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4064666	—	EC50	=	2.0	nM	8.70
CHEMBL4064666	—	EC90	=	9.0	nM	-
CHEMBL4064666	—	Inhibition		-	%	-