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Assay Detail

CHEMBL4267982

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

Binding
Inhibition of PI3KCdelta/PIK3R1 (unknown origin)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Intermediate

Target

PI3-kinase p110-delta/p85-alpha (CHEMBL2111432)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Piperidinyl-embeded chalcones possessing anti PI3Kδ inhibitory properties exhibit anti-atopic properties in preclinical models.
Dumontet C, Beck G, Gardebien F, Haudecoeur R, Mathé D, Matera EL, Tourette A, Mattei E, Esmenjaud J, Boyère C, Nurisso A, Peuchmaur M, Pérès B, Bouchaud G, Magnan A, Monneret G, Boumendjel A.
Eur J Med Chem (2018) 158 : 405 -413
PubMed 30237123 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.18 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3039502 DUVELISIB 4.0 1 8.64
CHEMBL2216870 IDELALISIB 4.0 1 7.77
CHEMBL4287949 1 5.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3039502 DUVELISIB IC50 = 2.3 nM 8.64
CHEMBL2216870 IDELALISIB IC50 = 17.0 nM 7.77
CHEMBL4287949 IC50 = 7200.0 nM 5.14