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Assay Detail

CHEMBL4358399

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

Binding
Inhibition of recombinant human full-length N-terminal His-tagged p110alpha/p85alpha expressed in baculovirus expression system using PIP2 as substrate measured after 1 hr by kinase-glo assay
19
Total Activities
19
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-alpha/p85-alpha (CHEMBL2111367)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Design, Synthesis, and Biological Evaluation of Imidazo[1,2-a]pyridine Derivatives as Novel PI3K/mTOR Dual Inhibitors.
Yu Y, Han Y, Zhang F, Gao Z, Zhu T, Dong S, Ma M.
J Med Chem (2020) 63 : 3028 -3046
PubMed 32069401 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 9.52 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3218576 COPANLISIB 4.0 1 9.96
CHEMBL4455710 1 9.77
CHEMBL4470122 1 9.77
CHEMBL4475217 1 9.72
CHEMBL4440406 1 9.70
CHEMBL4534475 1 9.70
CHEMBL4516974 1 9.70
CHEMBL4439080 1 9.66
CHEMBL4437362 1 9.64
CHEMBL4577573 1 9.64
CHEMBL4580837 1 9.62
CHEMBL4444638 1 9.55
CHEMBL4449613 1 9.52
CHEMBL4213353 1 9.51
CHEMBL4536505 1 9.46
CHEMBL4441605 1 9.43
CHEMBL4461136 1 8.72
CHEMBL573339 PI-103 1 8.36
CHEMBL1765463 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3218576 COPANLISIB IC50 = 0.11 nM 9.96
CHEMBL4455710 IC50 = 0.17 nM 9.77
CHEMBL4470122 IC50 = 0.17 nM 9.77
CHEMBL4475217 IC50 = 0.19 nM 9.72
CHEMBL4440406 IC50 = 0.2 nM 9.70
CHEMBL4534475 IC50 = 0.2 nM 9.70
CHEMBL4516974 IC50 = 0.2 nM 9.70
CHEMBL4439080 IC50 = 0.22 nM 9.66
CHEMBL4437362 IC50 = 0.23 nM 9.64
CHEMBL4577573 IC50 = 0.23 nM 9.64
CHEMBL4580837 IC50 = 0.24 nM 9.62
CHEMBL4444638 IC50 = 0.28 nM 9.55
CHEMBL4449613 IC50 = 0.3 nM 9.52
CHEMBL4213353 IC50 = 0.31 nM 9.51
CHEMBL4536505 IC50 = 0.35 nM 9.46
CHEMBL4441605 IC50 = 0.37 nM 9.43
CHEMBL4461136 IC50 = 1.9 nM 8.72
CHEMBL573339 PI-103 IC50 = 4.4 nM 8.36
CHEMBL1765463 IC50 > 5.0 nM -