Assay Detail
Binding
CHEMBL5732253
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Radioactive Binding Assay: The radioactive filter binding assay is standardized using recombinant human activated BRAF (V599E) kinase (Cat No. 14-557) and kinase dead MEK1 (K97R) (Cat No. 14-737) procured from Upstate. The incorporation of 32P into MEK1 (K97R) by BRAF (V599E) is measured with final assay buffer conditions of 50 mM Tris pH 7.5, 10 mM MgCl2, 1 mM DTT, 100 mM sucrose, 100 μM sodium orthovanadate, 5 μM ATP and 2 μCi [γ 32P] ATP and 500 mg MEK1 Kinase dead substrate. The enzymatic reaction is stopped after 120 minutes with 8N HCl (hydrochloric acid) and 1 mM ATP. The solution is spotted on P81 filter paper and washed 4 times with 0.75% orthophosphoric acid and lastly with acetone. The dried P81 filter papers are read in a Micro-beta Trilux scintillation counter. The final concentration of DMSO is 1% in the assay. Compounds are screened at 10 μM concentration with pre-incubation of the enzymes in the presence of test compound for 45 minutes. Compounds of the invention were found to be inactive in this assy, e.g. ex. 33 (13% inhibition at 10 uM), ex. 1A (0% inhibition at 10 uM).
303
Total Activities
100
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Dual specificity mitogen-activated protein kinase kinase 1 (CHEMBL3587) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Compounds and compositions as inhibitors of MEK
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 101 | 7.58 | 9.00 |
| kon | 101 | - | - |
| k_off | 101 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3946736 | — | — | 3 | 9.00 |
| CHEMBL3980017 | — | — | 3 | 8.82 |
| CHEMBL3930250 | — | — | 3 | 8.77 |
| CHEMBL3943311 | — | — | 3 | 8.70 |
| CHEMBL3916718 | — | — | 3 | 8.62 |
| CHEMBL3974369 | — | — | 3 | 8.59 |
| CHEMBL3955338 | — | — | 3 | 8.59 |
| CHEMBL3971701 | — | — | 3 | 8.57 |
| CHEMBL3934047 | — | — | 3 | 8.57 |
| CHEMBL3918610 | — | — | 3 | 8.52 |
| CHEMBL5970584 | — | — | 3 | 8.52 |
| CHEMBL3936697 | — | — | 3 | 8.44 |
| CHEMBL5939759 | — | — | 3 | 8.43 |
| CHEMBL3961528 | — | — | 3 | 8.43 |
| CHEMBL3934040 | — | — | 3 | 8.42 |
| CHEMBL3967019 | — | — | 3 | 8.37 |
| CHEMBL3894284 | — | — | 3 | 8.37 |
| CHEMBL5882359 | — | — | 3 | 8.35 |
| CHEMBL3913667 | — | — | 3 | 8.34 |
| CHEMBL3951042 | — | — | 3 | 8.33 |
| CHEMBL3904439 | — | — | 3 | 8.30 |
| CHEMBL3963847 | — | — | 3 | 8.28 |
| CHEMBL5744841 | — | — | 3 | 8.24 |
| CHEMBL3913739 | — | — | 6 | 8.21 |
| CHEMBL5866714 | — | — | 3 | 8.15 |
| CHEMBL3936680 | — | — | 3 | 8.15 |
| CHEMBL3960631 | — | — | 3 | 8.14 |
| CHEMBL3904177 | — | — | 3 | 8.07 |
| CHEMBL3940408 | — | — | 3 | 8.07 |
| CHEMBL5980351 | — | — | 3 | 8.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3946736 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3980017 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3930250 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3943311 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3916718 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3955338 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3974369 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3971701 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3934047 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5970584 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3918610 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3936697 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5939759 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3961528 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3934040 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3894284 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3967019 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5882359 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL3913667 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3951042 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3904439 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3963847 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL5744841 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3913739 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL3913739 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL3936680 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL5866714 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3960631 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL3940408 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3904177 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL5980351 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3914635 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL3941176 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3908754 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3933193 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3936824 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3918375 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3922238 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3923663 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3951376 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5790979 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3946095 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3957047 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3927711 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3966473 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3889657 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3946632 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5741764 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3935342 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3906048 | — | IC50 | = | 19.0 | nM | 7.72 |