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Assay Detail

CHEMBL4015804

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 anti-human CD28 antibody stimulated IL-6 secretion levels after 72 hrs by ELISA
7
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Atropisomerism and Conformational Equilibria: Impact on PI3Kδ Inhibition of 2-((6-Amino-9H-purin-9-yl)methyl)-5-methyl-3-(o-tolyl)quinazolin-4(3H)-one (IC87114) and Its Conformationally Restricted Analogs.
Lodola A, Bertolini S, Biagetti M, Capacchi S, Facchinetti F, Gallo PM, Pappani A, Mor M, Pala D, Rivara S, Visentini F, Corsi M, Capelli AM.
J Med Chem (2017) 60 : 4304 -4315
PubMed 28489362 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.86 8.90
pIC50 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4069027 2 8.90
CHEMBL1213082 2 7.60
CHEMBL4090825 1 7.30
CHEMBL4080605 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4069027 IC50 = 1.259 nM 8.90
CHEMBL4069027 IC50 = 6.31 nM 8.20
CHEMBL1213082 IC50 = 25.12 nM 7.60
CHEMBL1213082 IC50 = 50.12 nM 7.30
CHEMBL4090825 IC50 = 50.12 nM 7.30
CHEMBL4080605 pIC50 - -
CHEMBL4080605 pIC50 - -