Assay Detail
Binding
CHEMBL3887883
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In Vitro Enzyme Assay: Final assay conditions were 4 pM cRaf, 3 uM ATP, 10 nM biotin tagged MEK1 kinase dead protein substrate. Reactions were performed in Greiner384 well plates, catalog #784075. Reaction buffer was 50 mM Tris, pH 7.5, 50 mM NaCl, 10 mM MgCl2, 0.01% Tween-20, 0.05% BSA and 1 mM DTT. 5 ul of 2×cRaf plus MEK1 were dispensed into plates containing 0.25 ul of compound in 100% DMSO and incubated at room temperature for 30 minutes. Reactions were started by addition of 5 ul of 2×ATP. Reactions were run for two hours and terminated by addition of 10 ul of 2× antibody and Alphascreen bead mixture in Stop Buffer. Stop Buffer was 50 mM Tris, pH 7.5, 0.005% Tween-20, 25 mM EDTA.
197
Total Activities
196
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 |
Target
Serine/threonine-protein kinase B-raf (CHEMBL5145) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Biaryl amide compounds as kinase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 197 | 8.46 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3933272 | — | — | 1 | 9.82 |
| CHEMBL3967893 | — | — | 1 | 9.48 |
| CHEMBL3951474 | — | — | 1 | 9.41 |
| CHEMBL3905257 | — | — | 1 | 9.41 |
| CHEMBL3956654 | — | — | 1 | 9.39 |
| CHEMBL3959581 | — | — | 1 | 9.38 |
| CHEMBL3976881 | — | — | 1 | 9.34 |
| CHEMBL3928030 | — | — | 1 | 9.34 |
| CHEMBL3962812 | — | — | 1 | 9.32 |
| CHEMBL3984282 | — | — | 1 | 9.29 |
| CHEMBL3946003 | — | — | 1 | 9.23 |
| CHEMBL3987177 | — | — | 1 | 9.22 |
| CHEMBL3942721 | — | — | 1 | 9.20 |
| CHEMBL3960775 | — | — | 1 | 9.19 |
| CHEMBL3907015 | — | — | 1 | 9.19 |
| CHEMBL3914464 | — | — | 1 | 9.15 |
| CHEMBL3955743 | — | — | 1 | 9.13 |
| CHEMBL3966766 | — | — | 1 | 9.12 |
| CHEMBL3966243 | — | — | 1 | 9.11 |
| CHEMBL3930929 | — | — | 1 | 9.11 |
| CHEMBL3919205 | — | — | 1 | 9.10 |
| CHEMBL3963090 | — | — | 1 | 9.09 |
| CHEMBL3969121 | — | — | 2 | 9.08 |
| CHEMBL3969555 | — | — | 1 | 9.08 |
| CHEMBL3972141 | — | — | 1 | 9.07 |
| CHEMBL3945935 | — | — | 1 | 9.06 |
| CHEMBL3955103 | — | — | 1 | 9.05 |
| CHEMBL3909119 | — | — | 1 | 9.04 |
| CHEMBL3927963 | — | — | 1 | 9.03 |
| CHEMBL3906652 | — | — | 1 | 9.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3933272 | — | IC50 | = | 0.152 | nM | 9.82 |
| CHEMBL3967893 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL3905257 | — | IC50 | = | 0.389 | nM | 9.41 |
| CHEMBL3951474 | — | IC50 | = | 0.385 | nM | 9.41 |
| CHEMBL3956654 | — | IC50 | = | 0.408 | nM | 9.39 |
| CHEMBL3959581 | — | IC50 | = | 0.422 | nM | 9.38 |
| CHEMBL3976881 | — | IC50 | = | 0.456 | nM | 9.34 |
| CHEMBL3928030 | — | IC50 | = | 0.455 | nM | 9.34 |
| CHEMBL3962812 | — | IC50 | = | 0.483 | nM | 9.32 |
| CHEMBL3984282 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL3946003 | — | IC50 | = | 0.585 | nM | 9.23 |
| CHEMBL3987177 | — | IC50 | = | 0.601 | nM | 9.22 |
| CHEMBL3942721 | — | IC50 | = | 0.632 | nM | 9.20 |
| CHEMBL3960775 | — | IC50 | = | 0.652 | nM | 9.19 |
| CHEMBL3907015 | — | IC50 | = | 0.64 | nM | 9.19 |
| CHEMBL3914464 | — | IC50 | = | 0.706 | nM | 9.15 |
| CHEMBL3955743 | — | IC50 | = | 0.737 | nM | 9.13 |
| CHEMBL3966766 | — | IC50 | = | 0.756 | nM | 9.12 |
| CHEMBL3930929 | — | IC50 | = | 0.775 | nM | 9.11 |
| CHEMBL3966243 | — | IC50 | = | 0.773 | nM | 9.11 |
| CHEMBL3919205 | — | IC50 | = | 0.802 | nM | 9.10 |
| CHEMBL3963090 | — | IC50 | = | 0.816 | nM | 9.09 |
| CHEMBL3969121 | — | IC50 | = | 0.837 | nM | 9.08 |
| CHEMBL3969555 | — | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL3972141 | — | IC50 | = | 0.86 | nM | 9.07 |
| CHEMBL3945935 | — | IC50 | = | 0.862 | nM | 9.06 |
| CHEMBL3955103 | — | IC50 | = | 0.884 | nM | 9.05 |
| CHEMBL3909119 | — | IC50 | = | 0.905 | nM | 9.04 |
| CHEMBL3927963 | — | IC50 | = | 0.941 | nM | 9.03 |
| CHEMBL3903274 | — | IC50 | = | 0.994 | nM | 9.00 |
| CHEMBL3889721 | — | IC50 | = | 1.003 | nM | 9.00 |
| CHEMBL3906652 | — | IC50 | = | 1.001 | nM | 9.00 |
| CHEMBL4111816 | — | IC50 | = | 1.023 | nM | 8.99 |
| CHEMBL3912148 | — | IC50 | = | 1.08 | nM | 8.97 |
| CHEMBL3956383 | — | IC50 | = | 1.07 | nM | 8.97 |
| CHEMBL3924576 | — | IC50 | = | 1.067 | nM | 8.97 |
| CHEMBL3959652 | — | IC50 | = | 1.131 | nM | 8.95 |
| CHEMBL3905047 | — | IC50 | = | 1.137 | nM | 8.94 |
| CHEMBL3960436 | — | IC50 | = | 1.142 | nM | 8.94 |
| CHEMBL3960515 | — | IC50 | = | 1.17 | nM | 8.93 |
| CHEMBL3971301 | — | IC50 | = | 1.214 | nM | 8.92 |
| CHEMBL3932011 | — | IC50 | = | 1.197 | nM | 8.92 |
| CHEMBL3928581 | — | IC50 | = | 1.241 | nM | 8.91 |
| CHEMBL3894542 | — | IC50 | = | 1.254 | nM | 8.90 |
| CHEMBL4108504 | — | IC50 | = | 1.286 | nM | 8.89 |
| CHEMBL3946071 | — | IC50 | = | 1.278 | nM | 8.89 |
| CHEMBL3903846 | — | IC50 | = | 1.277 | nM | 8.89 |
| CHEMBL3947016 | — | IC50 | = | 1.306 | nM | 8.88 |
| CHEMBL3889893 | — | IC50 | = | 1.332 | nM | 8.88 |
| CHEMBL3975759 | — | IC50 | = | 1.356 | nM | 8.87 |