Assay Detail
Binding
CHEMBL5729924
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Sandwich Immunoassay: This test is based on measurement of the expression of AKT protein phosphorylated on serine 473 (P-AKT-S473) in the PC3 human prostate carcinoma line, by the technique based on a sandwich immunoassay using the Kit MSD Multi-spot Biomarker Detection of Meso Scale Discovery: phospho-Akt kits (Ser473) whole cell lysate (# K151 CAD) or phospho-Akt (Ser473) / Akt whole cell lysate Total (# K15100D). The primary antibody specific for P-AKT-S473 (Kit # K151 CAD) is coated onto an electrode in each well of 96-well plates of the MSD kit: after adding a protein lysate in each well, the revelation of the signal done by the addition of a secondary antibody labeled with an electrochemiluminescent detection compound. The procedure is described in the kit.On day 1, the PC3 cells are inoculated in 96-well plates (TPP # 92096) at a concentration of 35000 cells / well in 200 uL DMEM medium (DMEM Gibco # 1 1960-044) containing 10% fetal calf serum (FBS Gibco, # 10500-056) and 1% glutamine.
504
Total Activities
117
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
RAC-alpha serine/threonine-protein kinase (CHEMBL4282) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Pyrimidine derivatives, preparation thereof, and pharmaceutical use thereof as akt(pkb) phosphorylation inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 168 | 7.41 | 9.00 |
| kon | 168 | - | - |
| k_off | 168 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3910755 | — | — | 6 | 9.00 |
| CHEMBL3930708 | — | — | 6 | 9.00 |
| CHEMBL3900870 | — | — | 3 | 9.00 |
| CHEMBL3970476 | — | — | 9 | 9.00 |
| CHEMBL3914007 | — | — | 6 | 8.70 |
| CHEMBL3940961 | — | — | 6 | 8.70 |
| CHEMBL3925163 | — | — | 6 | 8.70 |
| CHEMBL3932198 | — | — | 6 | 8.70 |
| CHEMBL3970127 | — | — | 3 | 8.70 |
| CHEMBL3931890 | — | — | 6 | 8.70 |
| CHEMBL3918391 | — | — | 6 | 8.52 |
| CHEMBL3971065 | — | — | 6 | 8.52 |
| CHEMBL3965878 | — | — | 6 | 8.40 |
| CHEMBL3918242 | — | — | 6 | 8.40 |
| CHEMBL3971967 | — | — | 3 | 8.40 |
| CHEMBL3112867 | — | — | 6 | 8.30 |
| CHEMBL3964685 | — | — | 6 | 8.30 |
| CHEMBL3945090 | — | — | 6 | 8.30 |
| CHEMBL3935564 | — | — | 6 | 8.22 |
| CHEMBL3928308 | — | — | 9 | 8.10 |
| CHEMBL3964324 | — | — | 6 | 8.10 |
| CHEMBL3898401 | — | — | 3 | 8.10 |
| CHEMBL3896158 | — | — | 6 | 8.05 |
| CHEMBL3112853 | — | — | 3 | 8.05 |
| CHEMBL3925391 | — | — | 3 | 7.96 |
| CHEMBL3112848 | — | — | 6 | 7.92 |
| CHEMBL3943810 | — | — | 3 | 7.92 |
| CHEMBL3926375 | — | — | 3 | 7.92 |
| CHEMBL3901730 | — | — | 6 | 7.89 |
| CHEMBL3916147 | — | — | 6 | 7.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3900870 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3930708 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3910755 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3970476 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3914007 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3970127 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3925163 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3932198 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3931890 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3940961 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3971065 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3918391 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3918242 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3971967 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3910755 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3965878 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3112867 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3945090 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3964685 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3970476 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3970476 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3940961 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3932198 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3935564 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3930708 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3964324 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3898401 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3928308 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3112853 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3896158 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3112867 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3918391 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3925391 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3112848 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3943810 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3926375 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3901730 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3968336 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3916147 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3917877 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3911266 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3959404 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3982597 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3931890 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3893935 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3968336 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3890826 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3982597 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3112866 | SAR-260301 | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3925163 | — | IC50 | = | 17.0 | nM | 7.77 |