Assay Detail
Binding
CHEMBL2148366
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Inhibition of full length GST-tagged mouse B-Raf V600E mutant-mediated MEK1 phosphorylation after 1 hr by gel electrophoresis
32
Total Activities
32
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design, modification and 3D QSAR studies of novel 2,3-dihydrobenzo[b][1,4]dioxin-containing 4,5-dihydro-1H-pyrazole derivatives as inhibitors of B-Raf kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 5.62 | 7.22 |
| Ki | 1 | 9.80 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL477989 | SB590885 | — | 1 | 9.80 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 7.22 |
| CHEMBL2146827 | — | — | 1 | 6.96 |
| CHEMBL2146824 | — | — | 1 | 6.57 |
| CHEMBL2146825 | — | — | 1 | 6.48 |
| CHEMBL2146814 | — | — | 1 | 5.93 |
| CHEMBL2146815 | — | — | 1 | 5.86 |
| CHEMBL2146838 | — | — | 1 | 5.77 |
| CHEMBL2146841 | — | — | 1 | 5.76 |
| CHEMBL2146823 | — | — | 1 | 5.72 |
| CHEMBL2146816 | — | — | 1 | 5.71 |
| CHEMBL2146826 | — | — | 1 | 5.67 |
| CHEMBL2146835 | — | — | 1 | 5.57 |
| CHEMBL2146821 | — | — | 1 | 5.57 |
| CHEMBL2146828 | — | — | 1 | 5.53 |
| CHEMBL2146829 | — | — | 1 | 5.52 |
| CHEMBL2146822 | — | — | 1 | 5.49 |
| CHEMBL2146832 | — | — | 1 | 5.40 |
| CHEMBL2146820 | — | — | 1 | 5.38 |
| CHEMBL2146843 | — | — | 1 | 5.36 |
| CHEMBL2146836 | — | — | 1 | 5.36 |
| CHEMBL2146818 | — | — | 1 | 5.32 |
| CHEMBL2146830 | — | — | 1 | 5.29 |
| CHEMBL2146837 | — | — | 1 | 5.28 |
| CHEMBL2146831 | — | — | 1 | 5.28 |
| CHEMBL2146840 | — | — | 1 | 5.25 |
| CHEMBL2146839 | — | — | 1 | 5.23 |
| CHEMBL2146842 | — | — | 1 | 5.20 |
| CHEMBL2146817 | — | — | 1 | 5.18 |
| CHEMBL2146833 | — | — | 1 | 5.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL477989 | SB590885 | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2146827 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2146824 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL2146825 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL2146814 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL2146815 | — | IC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL2146838 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL2146841 | — | IC50 | = | 1720.0 | nM | 5.76 |
| CHEMBL2146823 | — | IC50 | = | 1890.0 | nM | 5.72 |
| CHEMBL2146816 | — | IC50 | = | 1970.0 | nM | 5.71 |
| CHEMBL2146826 | — | IC50 | = | 2130.0 | nM | 5.67 |
| CHEMBL2146835 | — | IC50 | = | 2670.0 | nM | 5.57 |
| CHEMBL2146821 | — | IC50 | = | 2710.0 | nM | 5.57 |
| CHEMBL2146828 | — | IC50 | = | 2970.0 | nM | 5.53 |
| CHEMBL2146829 | — | IC50 | = | 3020.0 | nM | 5.52 |
| CHEMBL2146822 | — | IC50 | = | 3230.0 | nM | 5.49 |
| CHEMBL2146832 | — | IC50 | = | 4010.0 | nM | 5.40 |
| CHEMBL2146820 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL2146843 | — | IC50 | = | 4390.0 | nM | 5.36 |
| CHEMBL2146836 | — | IC50 | = | 4350.0 | nM | 5.36 |
| CHEMBL2146818 | — | IC50 | = | 4750.0 | nM | 5.32 |
| CHEMBL2146830 | — | IC50 | = | 5160.0 | nM | 5.29 |
| CHEMBL2146837 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL2146831 | — | IC50 | = | 5270.0 | nM | 5.28 |
| CHEMBL2146840 | — | IC50 | = | 5570.0 | nM | 5.25 |
| CHEMBL2146839 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL2146842 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL2146817 | — | IC50 | = | 6550.0 | nM | 5.18 |
| CHEMBL2146833 | — | IC50 | = | 7310.0 | nM | 5.14 |
| CHEMBL2146819 | — | IC50 | = | 8770.0 | nM | 5.06 |
| CHEMBL2146834 | — | IC50 | = | 9320.0 | nM | 5.03 |