Assay Detail
Binding
CHEMBL3889261
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Kinase Assay: The kinase assay was performed in V-bottom 384-well plates. The final assay volume was 30 ul prepared from 15 ul additions of enzyme, substrates (fluoresceinated peptide FL-AHA-KRRRAL-PSER-VASLPGL-OH and ATP) and test compounds in assay buffer (20 mM HEPES pH 7.4, 30 mM MgCl2, 0.015% Brij35 and 4 mM DTT). The reaction was incubated at room temperature for 22 hours and terminated by adding 45 ul of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP®3000 (Caliper, Hopkinton, Mass.) by electrophoretic separation of the unphosphorylated substrate and phosphorylated product Inhibition data were calculated by comparison of the no enzyme control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assay were 200 pM CK1ε or CK1δ, 50 uM ATP, 1.5 uM FL-AHA-KRRRAL-PSER-VASLPGL-OH, and 1.6% DMSO. Dose response curves were generated to determine the concentration required to inhibit 50% of the kinase activity (IC50). Compounds were dissolved at 10 mM in dimethylsulfoxide (DMSO) and evaluated at eleven concentrations. IC50 values were derived by non-linear regression analysis.
200
Total Activities
199
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Pyrazole substituted imidazopyrazines as casein kinase 1 d/e inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 200 | 7.89 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3962177 | — | — | 1 | 9.70 |
| CHEMBL3978116 | — | — | 1 | 9.52 |
| CHEMBL4108038 | — | — | 1 | 9.52 |
| CHEMBL3912884 | — | — | 1 | 9.40 |
| CHEMBL3944464 | — | — | 1 | 9.22 |
| CHEMBL3981677 | — | — | 1 | 9.10 |
| CHEMBL3910319 | — | — | 1 | 9.05 |
| CHEMBL3902265 | — | — | 1 | 9.00 |
| CHEMBL3902838 | — | — | 1 | 9.00 |
| CHEMBL3981952 | — | — | 1 | 8.92 |
| CHEMBL3939027 | — | — | 1 | 8.89 |
| CHEMBL3922511 | — | — | 1 | 8.89 |
| CHEMBL3900391 | — | — | 1 | 8.89 |
| CHEMBL3894506 | — | — | 1 | 8.85 |
| CHEMBL3957543 | — | — | 1 | 8.82 |
| CHEMBL3895083 | — | — | 1 | 8.82 |
| CHEMBL3961316 | — | — | 1 | 8.74 |
| CHEMBL3907925 | — | — | 1 | 8.74 |
| CHEMBL3893731 | — | — | 1 | 8.74 |
| CHEMBL3910924 | — | — | 1 | 8.74 |
| CHEMBL3922012 | — | — | 1 | 8.72 |
| CHEMBL3932533 | — | — | 1 | 8.72 |
| CHEMBL3926405 | — | — | 1 | 8.70 |
| CHEMBL3971152 | — | — | 1 | 8.66 |
| CHEMBL3915816 | — | — | 1 | 8.66 |
| CHEMBL3913933 | — | — | 2 | 8.64 |
| CHEMBL3986585 | — | — | 1 | 8.64 |
| CHEMBL3936095 | — | — | 1 | 8.62 |
| CHEMBL3947732 | — | — | 1 | 8.62 |
| CHEMBL3942825 | — | — | 1 | 8.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3962177 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3978116 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4108038 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3912884 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3944464 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3981677 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3910319 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3902265 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3902838 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3981952 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3939027 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3922511 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3900391 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3894506 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3957543 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3895083 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3961316 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3907925 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3910924 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3893731 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3932533 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3922012 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3926405 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3971152 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3915816 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3913933 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3986585 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3936095 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3947732 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3942825 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3913933 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3943491 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3906580 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3935382 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3948521 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL3889846 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3916526 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3933835 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3952882 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3926825 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3982756 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3953610 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3959158 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3907142 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3938867 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3893281 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL3925387 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3958671 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3895318 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3924829 | — | IC50 | = | 6.0 | nM | 8.22 |