Assay Detail
Binding
CHEMBL3888976
Review assay metadata, readout intent, target linkage, and publication context from the same page.
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 |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL4005) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Bicyclic nitrogen-containing aromatic heterocyclic amide compound
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 |