Assay Detail
Binding
CHEMBL3889159
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In Vitro Inhibition Activity Assay: The compounds of formula I were tested for their activity on different PKC isoforms according to a published method (D. Geiges et al. Biochem. Pharmacol. 1997; 53:865-875) The assay is performed in a 96-well polypropylene microtiterplate (Costar 3794) that has been previously siliconized with Sigmacote (Sigma SL-2). The reaction mixture (50 μL) contains 10 μL of the relevant PKC isozyme together with 25 μL of the PKC inhibitor compound and 15 μL of a mix solution that contains 200 μg/mL protamine sulfate, 10 mM Mg(NO3)2, 10 μM ATP (Boehringer 519987) and 3750 Bq of 33P-ATP (Hartmann Analytic SFC301, 110 TBq/mmol) in 20 mM Tris-buffer pH 7.4+0.1% BSA. Incubation was performed for 15 minutes at 32° C. in a microtiterplate shaking incubator (Biolabo Scientific Instruments). Reaction was stopped by adding 10 μl of 0.5 M Na2EDTA, pH 7.4. 50 μl of mixture are pipetted onto a pre-wetted phosphocellulose paper (Whatmann 3698-915) under gentle pressure.
123
Total Activities
116
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
Protein kinase C inhibitors and methods of their use
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 123 | 8.62 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3920517 | — | — | 1 | 9.89 |
| CHEMBL3921551 | — | — | 1 | 9.89 |
| CHEMBL3893533 | — | — | 1 | 9.80 |
| CHEMBL3966595 | — | — | 2 | 9.70 |
| CHEMBL3982497 | — | — | 1 | 9.64 |
| CHEMBL3907088 | — | — | 1 | 9.62 |
| CHEMBL3943813 | — | — | 1 | 9.60 |
| CHEMBL3984070 | — | — | 1 | 9.57 |
| CHEMBL3937993 | — | — | 1 | 9.57 |
| CHEMBL3987185 | — | — | 1 | 9.54 |
| CHEMBL3892099 | — | — | 1 | 9.52 |
| CHEMBL3967601 | — | — | 1 | 9.48 |
| CHEMBL3895998 | — | — | 1 | 9.48 |
| CHEMBL3969856 | — | — | 1 | 9.44 |
| CHEMBL3966643 | — | — | 2 | 9.44 |
| CHEMBL3982723 | DAROVASERTIB | 2.0 | 1 | 9.40 |
| CHEMBL3958917 | — | — | 1 | 9.37 |
| CHEMBL3899197 | — | — | 1 | 9.35 |
| CHEMBL3889877 | — | — | 1 | 9.20 |
| CHEMBL3945647 | — | — | 1 | 9.17 |
| CHEMBL3983009 | — | — | 1 | 9.17 |
| CHEMBL3957715 | — | — | 1 | 9.17 |
| CHEMBL3981769 | — | — | 1 | 9.16 |
| CHEMBL3975025 | — | — | 1 | 9.15 |
| CHEMBL3914762 | — | — | 1 | 9.10 |
| CHEMBL3963605 | — | — | 1 | 9.08 |
| CHEMBL3970090 | — | — | 1 | 9.07 |
| CHEMBL3935341 | — | — | 1 | 9.07 |
| CHEMBL3980746 | — | — | 2 | 9.06 |
| CHEMBL3943147 | — | — | 1 | 9.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3921551 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL3920517 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL3893533 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL3966595 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3966595 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3982497 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL3907088 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL3943813 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL3984070 | — | IC50 | = | 0.27 | nM | 9.57 |
| CHEMBL3937993 | — | IC50 | = | 0.27 | nM | 9.57 |
| CHEMBL3987185 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL3892099 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3895998 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL3967601 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL3966643 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL3969856 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL3966643 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL3982723 | DAROVASERTIB | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3958917 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL3899197 | — | IC50 | = | 0.45 | nM | 9.35 |
| CHEMBL3889877 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL3957715 | — | IC50 | = | 0.67 | nM | 9.17 |
| CHEMBL3983009 | — | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL3945647 | — | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL3981769 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL3975025 | — | IC50 | = | 0.71 | nM | 9.15 |
| CHEMBL3914762 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL3963605 | — | IC50 | = | 0.84 | nM | 9.08 |
| CHEMBL3935341 | — | IC50 | = | 0.86 | nM | 9.07 |
| CHEMBL3970090 | — | IC50 | = | 0.85 | nM | 9.07 |
| CHEMBL3980746 | — | IC50 | = | 0.88 | nM | 9.06 |
| CHEMBL3943147 | — | IC50 | = | 0.87 | nM | 9.06 |
| CHEMBL3980746 | — | IC50 | = | 0.88 | nM | 9.06 |
| CHEMBL3892736 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3951893 | — | IC50 | = | 0.99 | nM | 9.00 |
| CHEMBL3920740 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3919244 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3960459 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3942560 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3891166 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3970381 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3915489 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3957149 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3968031 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3935905 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3961086 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3942619 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3932204 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3976541 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3896330 | — | IC50 | = | 1.5 | nM | 8.82 |