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Assay Detail

CHEMBL4193524

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

Binding
Inhibition of N-terminal His6-tagged recombinant full-length human p110alpha/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate by HTRF colorimetric assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
Confidence 7 — Homologous single protein target
Curated By Intermediate

Target

PI3-kinase p110-alpha/p85-alpha (CHEMBL2111367)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of novel 3-substituted imidazo[1,2-a]pyridine and quinazolin-4(3H)-one derivatives as PI3Kα inhibitors.
Fan YH, Li W, Liu DD, Bai MX, Song HR, Xu YN, Lee S, Zhou ZP, Wang J, Ding HW.
Eur J Med Chem (2017) 139 : 95 -106
PubMed 28800461 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.72 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4213353 1 9.30
CHEMBL1765463 1 8.96
CHEMBL4207685 1 8.42
CHEMBL4207150 1 8.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4213353 IC50 = 0.5 nM 9.30
CHEMBL1765463 IC50 = 1.1 nM 8.96
CHEMBL4207685 IC50 = 3.8 nM 8.42
CHEMBL4207150 IC50 = 6.5 nM 8.19