Assay Detail
Binding
CHEMBL3706188
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. The phosphorylation of AKT (pAKT) is measured by western blotting in the PC3 human prostate carcinoma line (ATCC CRL-1435), using an antibody that specifically recognises pAKT-S473.On day 1, the PC3 cells are seeded into 6-well plates (TPP, #92006) at the concentration of 0.8x106 cells/well in 1800 ul of DMEM medium (DMEM Gibco #11960-044) containing 10% of foetal calf serum (SVF Gibco, #10500-056) and 1% glutamine (L-Glu Gibco #25030-024), and incubated at 37 C., 5% CO2, overnight.On day 2, the cells are incubated in the presence or absence of the test products for 1 to 2 hours at 37 C. in the presence of 5% CO2. The molecules, diluted in dimethyl sulphoxide (DMSO Sigma #D2650), are added from a 10-times concentrated stock solution, the final percentage of DMSO being 0.1%. The molecules are tested either at a single concentration of less than or equal to 10 uM, or ....
55
Total Activities
55
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 | 55 | 6.18 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2151923 | — | — | 1 | 7.64 |
| CHEMBL2151924 | — | — | 1 | 7.64 |
| CHEMBL2151919 | — | — | 1 | 7.41 |
| CHEMBL2151048 | — | — | 1 | 7.03 |
| CHEMBL2151921 | — | — | 1 | 7.00 |
| CHEMBL3696234 | — | — | 1 | 6.99 |
| CHEMBL2151926 | — | — | 1 | 6.94 |
| CHEMBL3112690 | — | — | 1 | 6.88 |
| CHEMBL3696272 | — | — | 1 | 6.86 |
| CHEMBL2151925 | — | — | 1 | 6.77 |
| CHEMBL3696265 | — | — | 1 | 6.74 |
| CHEMBL2151935 | — | — | 1 | 6.70 |
| CHEMBL3696253 | — | — | 1 | 6.70 |
| CHEMBL3696268 | — | — | 1 | 6.64 |
| CHEMBL3696282 | — | — | 1 | 6.60 |
| CHEMBL3696262 | — | — | 1 | 6.58 |
| CHEMBL3696258 | — | — | 1 | 6.54 |
| CHEMBL3696261 | — | — | 1 | 6.51 |
| CHEMBL2151927 | — | — | 1 | 6.50 |
| CHEMBL2151821 | — | — | 1 | 6.49 |
| CHEMBL3696244 | — | — | 1 | 6.46 |
| CHEMBL3696264 | — | — | 1 | 6.46 |
| CHEMBL3696259 | — | — | 1 | 6.40 |
| CHEMBL3696274 | — | — | 1 | 6.38 |
| CHEMBL3696255 | — | — | 1 | 6.32 |
| CHEMBL3696277 | — | — | 1 | 6.28 |
| CHEMBL3696260 | — | — | 1 | 6.26 |
| CHEMBL2151820 | — | — | 1 | 6.24 |
| CHEMBL3696251 | — | — | 1 | 6.21 |
| CHEMBL3696238 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2151923 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2151924 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2151919 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL2151048 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL2151921 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3696234 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL2151926 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL3112690 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL3696272 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL2151925 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL3696265 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL2151935 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL3696253 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3696268 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL3696282 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3696262 | — | IC50 | = | 261.0 | nM | 6.58 |
| CHEMBL3696258 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3696261 | — | IC50 | = | 308.0 | nM | 6.51 |
| CHEMBL2151927 | — | IC50 | = | 318.0 | nM | 6.50 |
| CHEMBL2151821 | — | IC50 | = | 321.0 | nM | 6.49 |
| CHEMBL3696244 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3696264 | — | IC50 | = | 346.0 | nM | 6.46 |
| CHEMBL3696259 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3696274 | — | IC50 | = | 417.0 | nM | 6.38 |
| CHEMBL3696255 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3696277 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL3696260 | — | IC50 | = | 549.0 | nM | 6.26 |
| CHEMBL2151820 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL3696251 | — | IC50 | = | 609.0 | nM | 6.21 |
| CHEMBL3696238 | — | IC50 | = | 632.0 | nM | 6.20 |
| CHEMBL3696286 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL2151819 | — | IC50 | = | 727.0 | nM | 6.14 |
| CHEMBL3639951 | — | IC50 | = | 737.0 | nM | 6.13 |
| CHEMBL3696273 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL3696270 | — | IC50 | = | 807.0 | nM | 6.09 |
| CHEMBL2151922 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL3696242 | — | IC50 | = | 1314.0 | nM | 5.88 |
| CHEMBL2151920 | — | IC50 | = | 1420.0 | nM | 5.85 |
| CHEMBL3696240 | — | IC50 | = | 1481.0 | nM | 5.83 |
| CHEMBL3696257 | — | IC50 | = | 1494.0 | nM | 5.83 |
| CHEMBL3696256 | — | IC50 | = | 1763.0 | nM | 5.75 |
| CHEMBL3696281 | — | IC50 | = | 2207.0 | nM | 5.66 |
| CHEMBL3696246 | — | IC50 | = | 2287.0 | nM | 5.64 |
| CHEMBL3696263 | — | IC50 | = | 2498.0 | nM | 5.60 |
| CHEMBL2151822 | — | IC50 | = | 3498.0 | nM | 5.46 |
| CHEMBL3696250 | — | IC50 | = | 3635.0 | nM | 5.44 |
| CHEMBL3696284 | — | IC50 | = | 5375.0 | nM | 5.27 |
| CHEMBL2151928 | — | IC50 | = | 5865.0 | nM | 5.23 |
| CHEMBL2151929 | — | IC50 | = | 6155.0 | nM | 5.21 |
| CHEMBL3696279 | — | IC50 | = | 6460.0 | nM | 5.19 |