Assay Detail
Binding
CHEMBL3887822
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cascade Assay: A BRAF-MEK-ERK cascade assay is used to evaluate the effects of these compounds as inhibitors of the MAP kinase pathway. An enzymatic cascade assay is set up using recombinant human activated BRAF (V599E) kinase (Cat No. 14-557), human full length MEK1 kinase (Cat No. 14-706) and human full length active MAP Kinase 2/ERK2 (Cat No. 14-536) enzymes procured from Upstate. TR-FRET (Time resolved fluorescence resonance energy transfer) detection technology is used for the read out. The assay buffer solution contains 50 mM Tris pH 7.5, 10 mM MgCl2, 1 mM DTT, 0.01% Tween 20, 0.1 nM activated BRAF, 2 nM inactive MEK1, 10 nM inactive ERK2, 1 mM ATP and 500 nM long chain biotin-peptide substrate (LCB-FFKNIVTPRTPPP) in a 384 well format. The kinase reaction is stopped after 90 minutes with 10 mM EDTA and Lance detection mix (2 nM Eu-labeled phospho-serine/threonine antibody (Cat. No. AD0176-Perkin Elmer), 20 nM SA-APC (Cat No. CR130-100-Perkin Elmer) is added.
101
Total Activities
99
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase RAF and Dual specificity mitogen-activated protein kinase kinase 1 (Raf/MEK) (CHEMBL2111351) ↗| Type | PROTEIN FAMILY |
| 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 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3946736 | — | — | 1 | 9.00 |
| CHEMBL3980017 | — | — | 1 | 8.82 |
| CHEMBL3930250 | — | — | 1 | 8.77 |
| CHEMBL3943311 | — | — | 1 | 8.70 |
| CHEMBL3916718 | — | — | 1 | 8.62 |
| CHEMBL3955338 | — | — | 1 | 8.59 |
| CHEMBL3974369 | — | — | 1 | 8.59 |
| CHEMBL3971701 | — | — | 1 | 8.57 |
| CHEMBL3934047 | — | — | 1 | 8.57 |
| CHEMBL3958688 | — | — | 1 | 8.52 |
| CHEMBL3918610 | — | — | 1 | 8.52 |
| CHEMBL3936697 | — | — | 1 | 8.44 |
| CHEMBL3926742 | — | — | 1 | 8.43 |
| CHEMBL3961528 | — | — | 1 | 8.43 |
| CHEMBL3934040 | — | — | 1 | 8.42 |
| CHEMBL3967019 | — | — | 1 | 8.37 |
| CHEMBL3894284 | — | — | 1 | 8.37 |
| CHEMBL3937201 | — | — | 1 | 8.35 |
| CHEMBL3913667 | — | — | 1 | 8.34 |
| CHEMBL3951042 | — | — | 1 | 8.33 |
| CHEMBL3904439 | — | — | 1 | 8.30 |
| CHEMBL3963847 | — | — | 1 | 8.28 |
| CHEMBL3980388 | — | — | 1 | 8.24 |
| CHEMBL3913739 | — | — | 2 | 8.21 |
| CHEMBL3936680 | — | — | 1 | 8.15 |
| CHEMBL3909274 | — | — | 1 | 8.15 |
| CHEMBL3960631 | — | — | 1 | 8.14 |
| CHEMBL3904177 | — | — | 1 | 8.07 |
| CHEMBL3940408 | — | — | 1 | 8.07 |
| CHEMBL3932078 | — | — | 1 | 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 |
| CHEMBL3918610 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3958688 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3936697 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3961528 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3926742 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3934040 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3967019 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3894284 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3937201 | — | 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 |
| CHEMBL3980388 | — | 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 |
| CHEMBL3909274 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3960631 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL3904177 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3940408 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3932078 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3914635 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL3933193 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3941176 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3908754 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3951376 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3922238 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3923663 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3936824 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3918375 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3924335 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3957047 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3946095 | — | 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 |
| CHEMBL3906048 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3935342 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4113313 | — | IC50 | = | 19.0 | nM | 7.72 |