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Assay Detail

CHEMBL4479336

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

Binding
Inhibition of PI3Kdelta in human PBMC assessed as reduction in cytostim-induced IFNgamma production after 20 hrs by electrochemiluminescence assay
5
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.
Amour A, Barton N, Cooper AW, Inglis G, Jamieson C, Luscombe CN, Morrell J, Peace S, Perez D, Rowland P, Tame CJ, Uddin S, Vitulli G, Wellaway N.
J Med Chem (2016) 59 : 7239 -7251
PubMed 27429068 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.00 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4434674 1 8.40
CHEMBL4593011 1 6.70
CHEMBL4564931 1 6.70
CHEMBL4561692 2 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4434674 IC50 = 3.981 nM 8.40
CHEMBL4593011 IC50 = 199.53 nM 6.70
CHEMBL4564931 IC50 = 199.53 nM 6.70
CHEMBL4561692 IC50 = 251.19 nM 6.60
CHEMBL4561692 IC50 = 250.0 nM 6.60