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Assay Detail

CHEMBL4193872

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

Binding
Inhibition of recombinant full length N-terminal His-tagged human PI3K p110alpha/p85alpha expressed in baculovirus expression system using PIP2/PS as substrate after 1 hr by ADP-Glo luminescence assay
8
Total Activities
8
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-alpha/p85-alpha (CHEMBL2111367)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity.
Yang C, Zhang X, Wang Y, Yang Y, Liu X, Deng M, Jia Y, Ling Y, Meng LH, Zhou Y.
ACS Med Chem Lett (2017) 8 : 875 -880
PubMed 28835805 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.52 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4217725 1 9.00
CHEMBL4212775 1 9.00
CHEMBL4213317 1 9.00
CHEMBL4208385 1 9.00
CHEMBL4204586 1 8.70
CHEMBL4216255 1 8.70
CHEMBL4214320 1 7.46
CHEMBL4204119 1 7.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4217725 IC50 = 1.0 nM 9.00
CHEMBL4212775 IC50 = 1.0 nM 9.00
CHEMBL4213317 IC50 = 1.0 nM 9.00
CHEMBL4208385 IC50 = 1.0 nM 9.00
CHEMBL4204586 IC50 = 2.0 nM 8.70
CHEMBL4216255 IC50 = 2.0 nM 8.70
CHEMBL4214320 IC50 = 35.0 nM 7.46
CHEMBL4204119 IC50 = 51.0 nM 7.29