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Assay Detail

CHEMBL3888976

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

Binding
Cell Proliferation Inhibition Assay: In order to make human PIK3 CA mutation-positive breast cancer cell line MDA-MB-453 cells become 500 cells per well in a 384 well non-adhesive plate (Lipidure-Coat plate AT-384; manufactured by NOF Corporation), 36 μl/well was seeded in Leibovitz's L-15 medium including 10% fetal bovine serum (manufactured by Life technologies Corp.), followed by culturing at 37° C. overnight in the presence of CO2. The following day, the test compound (the test compound had 11 steps in a final concentration from 10000 nM to 0.1 nM), and DMSO which is a solvent for the test compound as a negative control were diluted with the medium, and 4 μl was added to cells. Thereafter, the cells were cultured for 4 days at 37° C. in the absence of CO2, and a cytometric reagent (CellTiter-Glo Luminescent Cell Viability assay manufactured by Promega Corporation) was added. The resultant product was stirred for 30 minutes, and then measurement was carried out using a luminescence measurement apparatus
19
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Cancer cell lines
Confidence 8 — Homologous single protein target
Curated By Autocuration

Publication

Bicyclic nitrogen-containing aromatic heterocyclic amide compound
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 8.24 9.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3969654 1 9.26
CHEMBL3970694 1 9.19
CHEMBL3955631 1 8.60
CHEMBL3978948 1 8.55
CHEMBL3955171 1 8.49
CHEMBL3941150 1 8.40
CHEMBL3946485 1 8.38
CHEMBL3904401 1 8.28
CHEMBL3895006 1 8.21
CHEMBL3892677 1 8.12
CHEMBL3983813 1 8.11
CHEMBL3986674 1 8.09
CHEMBL3895466 1 8.07
CHEMBL3916942 1 8.05
CHEMBL3929875 1 7.96
CHEMBL3968294 1 7.92
CHEMBL3950327 2 7.92
CHEMBL3966762 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3969654 IC50 = 0.55 nM 9.26
CHEMBL3970694 IC50 = 0.65 nM 9.19
CHEMBL3955631 IC50 = 2.5 nM 8.60
CHEMBL3978948 IC50 = 2.8 nM 8.55
CHEMBL3955171 IC50 = 3.2 nM 8.49
CHEMBL3941150 IC50 = 4.0 nM 8.40
CHEMBL3946485 IC50 = 4.2 nM 8.38
CHEMBL3904401 IC50 = 5.2 nM 8.28
CHEMBL3895006 IC50 = 6.2 nM 8.21
CHEMBL3892677 IC50 = 7.6 nM 8.12
CHEMBL3983813 IC50 = 7.8 nM 8.11
CHEMBL3986674 IC50 = 8.1 nM 8.09
CHEMBL3895466 IC50 = 8.5 nM 8.07
CHEMBL3916942 IC50 = 8.9 nM 8.05
CHEMBL3929875 IC50 = 11.0 nM 7.96
CHEMBL3968294 IC50 = 12.0 nM 7.92
CHEMBL3950327 IC50 = 12.0 nM 7.92
CHEMBL3950327 IC50 = 26.0 nM 7.58
CHEMBL3966762 IC50 = 40.0 nM 7.40