Assay Detail
Binding
CHEMBL3706189
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory Assay: This test is based on measuring the expression of the AKT protein phosphorylated on serine 473 (P-AKT-S473), in the PC3 human prostate carcinoma line, by means of the technique based on a sandwich immunoassay using the MSD Multi-spot Biomarker Detection kit from Meso Scale Discovery: phospho-Akt (Ser473) whole cell lysate kit (#K151CAD) or phospho-Akt (Ser473)/Total Akt whole cell lysate kit (#K15100D). The primary antibody specific for P-AKT-S473 (Kit #K151CAD) is coated on to an electrode in each well of the 96-well plates of the MSD, kit: after the addition of a protein lysate to each well, the signal is visualised by adding a secondary detection antibody labelled with an electrochemoluminescent compound. The procedure followed is that described in the kit.On day 1, the PC3 cells are seeded into 96-well plates (TPP, #92096) at the concentration of 35 000 cells/well in 200 ul of DMEM medium (DMEM Gibco #11960-044) containing 10% of foetal calf serum (FCS Gibco, #10500-056).
106
Total Activities
106
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PC-3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
RAC-alpha serine/threonine-protein kinase (CHEMBL4282) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
(6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives, preparation thereof and pharmaceutical use thereof as AKT(PKB) phosphorylation inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 106 | 7.15 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3112850 | — | — | 1 | 9.00 |
| CHEMBL3112849 | — | — | 1 | 8.52 |
| CHEMBL3112851 | — | — | 1 | 8.52 |
| CHEMBL3699804 | — | — | 1 | 8.40 |
| CHEMBL3112848 | — | — | 1 | 8.30 |
| CHEMBL3112862 | — | — | 1 | 8.22 |
| CHEMBL3112847 | — | — | 1 | 8.15 |
| CHEMBL3696287 | — | — | 1 | 8.00 |
| CHEMBL3699780 | — | — | 1 | 8.00 |
| CHEMBL3696300 | — | — | 1 | 7.96 |
| CHEMBL3699783 | — | — | 1 | 7.96 |
| CHEMBL3112867 | — | — | 1 | 7.92 |
| CHEMBL3112864 | — | — | 1 | 7.89 |
| CHEMBL3696296 | — | — | 1 | 7.85 |
| CHEMBL3696307 | — | — | 1 | 7.82 |
| CHEMBL3699788 | — | — | 1 | 7.80 |
| CHEMBL3696293 | — | — | 1 | 7.77 |
| CHEMBL3112866 | SAR-260301 | 1.0 | 1 | 7.72 |
| CHEMBL3112861 | — | — | 1 | 7.70 |
| CHEMBL3699800 | — | — | 1 | 7.66 |
| CHEMBL3696237 | — | — | 1 | 7.64 |
| CHEMBL3696314 | — | — | 1 | 7.64 |
| CHEMBL3696309 | — | — | 1 | 7.62 |
| CHEMBL3696294 | — | — | 1 | 7.58 |
| CHEMBL3699779 | — | — | 1 | 7.58 |
| CHEMBL3699796 | — | — | 1 | 7.58 |
| CHEMBL3696308 | — | — | 1 | 7.57 |
| CHEMBL3112865 | — | — | 1 | 7.55 |
| CHEMBL3699808 | — | — | 1 | 7.54 |
| CHEMBL3696301 | — | — | 1 | 7.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3112850 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3112851 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3112849 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3699804 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3112848 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3112862 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3112847 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3699780 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3696287 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3699783 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3696300 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3112867 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3112864 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3696296 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3696307 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3699788 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3696293 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3112866 | SAR-260301 | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3112861 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3699800 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3696237 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3696314 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3696309 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3696294 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3699796 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3699779 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3696308 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3112865 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3699808 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3699797 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3696301 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3639986 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3699793 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3696241 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3696306 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3696311 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3699806 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3696305 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3699784 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3699810 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3696274 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3696236 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3699781 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3696310 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3699811 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3696298 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3696249 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL3112852 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3696258 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3699789 | — | IC50 | = | 61.0 | nM | 7.21 |