Assay Detail
Binding
CHEMBL3887296
Review assay metadata, readout intent, target linkage, and publication context from the same page.
P70S6K Enzyme Assay: P70S6K inhibitor compounds are diluted and plated in 96 well plates. A reaction mixture including the following components is then added to the compound plate to initiate the enzyme reaction; P70S6K (3 nM, T412E mutant, Millipore) is mixed with 24 uM ATP in an assay buffer containing 100 mM Hepes (pH 7.5), 5 mM MgCl2, 1 mM DTT, 0.015% Brij and 1 uM of the substrate peptide FITC-AHA-AKRRRLSSLRA-OH (derived from the S6 ribosomal protein sequence, FITC=fluorescein isothiocyanate, AHA=6-aminohexanoic acid). The reaction is incubated for 90 min at 25.degree. C., before the addition of 10 mM EDTA to stop the reaction. The proportion of substrate and product (phosphorylated) peptide is analysed on a Caliper Life Sciences Lab Chip 3000, using a pressure of -1.4 psi, and upstream and downstream voltages of -3000 and -700 respectively. Product peaks are resolved before substrate peaks on the resulting chromatograms.
400
Total Activities
399
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Imidazole amines as modulators of kinase activity
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 400 | 8.33 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3936990 | — | — | 1 | 10.22 |
| CHEMBL3899716 | — | — | 1 | 10.00 |
| CHEMBL3966806 | — | — | 1 | 9.96 |
| CHEMBL3906990 | — | — | 1 | 9.70 |
| CHEMBL3980521 | — | — | 1 | 9.70 |
| CHEMBL3981085 | — | — | 1 | 9.59 |
| CHEMBL3894849 | — | — | 1 | 9.40 |
| CHEMBL3943127 | — | — | 1 | 9.36 |
| CHEMBL3977147 | — | — | 1 | 9.30 |
| CHEMBL3971598 | — | — | 1 | 9.30 |
| CHEMBL3978595 | — | — | 1 | 9.30 |
| CHEMBL3904322 | — | — | 1 | 9.22 |
| CHEMBL3910789 | — | — | 1 | 9.22 |
| CHEMBL3919089 | — | — | 1 | 9.22 |
| CHEMBL3941283 | — | — | 1 | 9.22 |
| CHEMBL3965271 | — | — | 1 | 9.15 |
| CHEMBL3891980 | — | — | 1 | 9.15 |
| CHEMBL3961056 | — | — | 1 | 9.15 |
| CHEMBL3957657 | — | — | 1 | 9.14 |
| CHEMBL3966203 | — | — | 1 | 9.10 |
| CHEMBL3912632 | — | — | 1 | 9.10 |
| CHEMBL3928772 | — | — | 1 | 9.10 |
| CHEMBL3967010 | — | — | 1 | 9.10 |
| CHEMBL3949201 | — | — | 1 | 9.10 |
| CHEMBL3913464 | — | — | 1 | 9.10 |
| CHEMBL3972479 | — | — | 1 | 9.10 |
| CHEMBL3963056 | — | — | 1 | 9.10 |
| CHEMBL3962020 | — | — | 1 | 9.05 |
| CHEMBL3941451 | — | — | 1 | 9.05 |
| CHEMBL3906695 | — | — | 1 | 9.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3936990 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL3899716 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3966806 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL3980521 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3906990 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3981085 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL3894849 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3943127 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL3971598 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3977147 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3978595 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3910789 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3941283 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3919089 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3904322 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3891980 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3961056 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3965271 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3957657 | — | IC50 | = | 0.73 | nM | 9.14 |
| CHEMBL3928772 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3913464 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3912632 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3967010 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3949201 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3963056 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3972479 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3966203 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3906695 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3919834 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3969016 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3941451 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3940627 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3928074 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3962020 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3927358 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3933597 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3948085 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3890352 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3940867 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3938454 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3951747 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3983282 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3912769 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3980922 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3968744 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3974201 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3960355 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3954781 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3962807 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3916178 | — | IC50 | = | 1.2 | nM | 8.92 |