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Assay Detail

CHEMBL4134269

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

Functional
Ex-vivo inhibition of PI3Kdelta in po dosed Lewis rat assessed as reduction in anti-IgM/IL4-induced AKT phosphorylation at ser473 residue in whole blood pretreated up to 24 hrs followed by anti-IgM/IL4 stimulation after 10 mins by flow cytometric analysis
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors.
Hoegenauer K, Soldermann N, Zécri F, Strang RS, Graveleau N, Wolf RM, Cooke NG, Smith AB, Hollingworth GJ, Blanz J, Gutmann S, Rummel G, Littlewood-Evans A, Burkhart C.
ACS Med Chem Lett (2017) 8 : 975 -980
PubMed 28947947 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
fEC50 1 - -
EC50 1 7.08 7.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3643413 LENIOLISIB 4.0 2 7.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3643413 LENIOLISIB EC50 = 83.0 nM 7.08
CHEMBL3643413 LENIOLISIB fEC50 = 5.0 nM -