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Assay Detail

CHEMBL4836861

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

Binding
Inhibition of recombinant human full length His-tagged p110delta/p85alpha expressed in baculovirus expression system measured after 60 mins in presence of ATP by ATP-competitive binding assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and biological evaluation of novel purinyl quinazolinone derivatives as PI3Kδ-specific inhibitors for the treatment of hematologic malignancies.
Kim YS, Cheon MG, Boggu PR, Koh SY, Park GM, Kim G, Park SH, Park SL, Lee CW, Kim JW, Jung YH.
Bioorg Med Chem (2021) 45 : 116312 -116312
PubMed 34332211 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 9.09 10.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4868117 1 10.05
CHEMBL4852166 1 9.41
CHEMBL4871071 1 9.40
CHEMBL4845946 1 9.30
CHEMBL4876309 1 9.30
CHEMBL4853740 1 9.30
CHEMBL4862467 1 9.22
CHEMBL2216870 IDELALISIB 4.0 1 8.97
CHEMBL4874496 1 8.97
CHEMBL4858100 1 8.97
CHEMBL4874404 1 8.96
CHEMBL4852863 1 8.89
CHEMBL4876188 1 8.77
CHEMBL4847494 1 8.74
CHEMBL4870032 1 8.69
CHEMBL4854194 1 8.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4868117 IC50 = 0.09 nM 10.05
CHEMBL4852166 IC50 = 0.39 nM 9.41
CHEMBL4871071 IC50 = 0.4 nM 9.40
CHEMBL4845946 IC50 = 0.5 nM 9.30
CHEMBL4876309 IC50 = 0.5 nM 9.30
CHEMBL4853740 IC50 = 0.5 nM 9.30
CHEMBL4862467 IC50 = 0.6 nM 9.22
CHEMBL2216870 IDELALISIB IC50 = 1.08 nM 8.97
CHEMBL4874496 IC50 = 1.08 nM 8.97
CHEMBL4858100 IC50 = 1.07 nM 8.97
CHEMBL4874404 IC50 = 1.09 nM 8.96
CHEMBL4852863 IC50 = 1.3 nM 8.89
CHEMBL4876188 IC50 = 1.7 nM 8.77
CHEMBL4847494 IC50 = 1.82 nM 8.74
CHEMBL4870032 IC50 = 2.05 nM 8.69
CHEMBL4854194 IC50 = 3.23 nM 8.49