Assay Detail
Binding
CHEMBL5046400
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human BRAF V600E mutant using myelin basic protein as substrate in presence of [gamma-33P]ATP incubated for 40 mins by scintillation counting method
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase B-raf (CHEMBL5145) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of New Imidazo[2,1-<i>b</i>]thiazole Derivatives as Potent Pan-RAF Inhibitors with Promising <i>In Vitro</i> and <i>In Vivo</i> Anti-melanoma Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 46 | 7.30 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5087577 | — | — | 1 | 10.15 |
| CHEMBL5086749 | — | — | 1 | 9.01 |
| CHEMBL5083036 | — | — | 1 | 9.00 |
| CHEMBL5080553 | — | — | 1 | 8.82 |
| CHEMBL5073246 | — | — | 1 | 8.58 |
| CHEMBL5079413 | — | — | 1 | 8.42 |
| CHEMBL5076688 | — | — | 1 | 8.34 |
| CHEMBL5079502 | — | — | 1 | 8.28 |
| CHEMBL5088891 | — | — | 1 | 8.20 |
| CHEMBL5092329 | — | — | 1 | 8.14 |
| CHEMBL5088157 | — | — | 1 | 8.08 |
| CHEMBL5092112 | — | — | 1 | 8.06 |
| CHEMBL5077391 | — | — | 1 | 8.05 |
| CHEMBL5077895 | — | — | 1 | 8.02 |
| CHEMBL5089022 | — | — | 1 | 8.00 |
| CHEMBL5075811 | — | — | 1 | 7.98 |
| CHEMBL5076765 | — | — | 1 | 7.90 |
| CHEMBL5077573 | — | — | 1 | 7.72 |
| CHEMBL5094173 | — | — | 1 | 7.70 |
| CHEMBL5080054 | — | — | 1 | 7.26 |
| CHEMBL5086379 | — | — | 1 | 7.24 |
| CHEMBL5092007 | — | — | 1 | 7.19 |
| CHEMBL5088456 | — | — | 1 | 7.18 |
| CHEMBL5090684 | — | — | 1 | 7.16 |
| CHEMBL5075200 | — | — | 1 | 7.11 |
| CHEMBL5073098 | — | — | 1 | 7.07 |
| CHEMBL5072570 | — | — | 1 | 7.05 |
| CHEMBL5093355 | — | — | 1 | 7.04 |
| CHEMBL5073858 | — | — | 1 | 7.01 |
| CHEMBL5081210 | — | — | 1 | 6.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5087577 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL5086749 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL5083036 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5080553 | — | IC50 | = | 1.51 | nM | 8.82 |
| CHEMBL5073246 | — | IC50 | = | 2.62 | nM | 8.58 |
| CHEMBL5079413 | — | IC50 | = | 3.77 | nM | 8.42 |
| CHEMBL5076688 | — | IC50 | = | 4.56 | nM | 8.34 |
| CHEMBL5079502 | — | IC50 | = | 5.21 | nM | 8.28 |
| CHEMBL5088891 | — | IC50 | = | 6.35 | nM | 8.20 |
| CHEMBL5092329 | — | IC50 | = | 7.25 | nM | 8.14 |
| CHEMBL5088157 | — | IC50 | = | 8.36 | nM | 8.08 |
| CHEMBL5092112 | — | IC50 | = | 8.65 | nM | 8.06 |
| CHEMBL5077391 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5077895 | — | IC50 | = | 9.57 | nM | 8.02 |
| CHEMBL5089022 | — | IC50 | = | 9.96 | nM | 8.00 |
| CHEMBL5075811 | — | IC50 | = | 10.51 | nM | 7.98 |
| CHEMBL5076765 | — | IC50 | = | 12.57 | nM | 7.90 |
| CHEMBL5077573 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5094173 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5080054 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5086379 | — | IC50 | = | 57.7 | nM | 7.24 |
| CHEMBL5092007 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL5088456 | — | IC50 | = | 66.1 | nM | 7.18 |
| CHEMBL5090684 | — | IC50 | = | 69.1 | nM | 7.16 |
| CHEMBL5075200 | — | IC50 | = | 77.5 | nM | 7.11 |
| CHEMBL5073098 | — | IC50 | = | 85.3 | nM | 7.07 |
| CHEMBL5072570 | — | IC50 | = | 89.3 | nM | 7.05 |
| CHEMBL5093355 | — | IC50 | = | 90.3 | nM | 7.04 |
| CHEMBL5073858 | — | IC50 | = | 98.1 | nM | 7.01 |
| CHEMBL5081210 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL5090199 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL5082423 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL5077093 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL5087580 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5087208 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL5079253 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5092853 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL5078889 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL5086784 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL5084985 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL5075700 | — | IC50 | = | 13250.0 | nM | 4.88 |
| CHEMBL5079845 | — | IC50 | = | 21330.0 | nM | 4.67 |
| CHEMBL5076831 | — | IC50 | = | 25120.0 | nM | 4.60 |
| CHEMBL5077227 | — | IC50 | = | 26560.0 | nM | 4.58 |
| CHEMBL5088659 | — | IC50 | = | 26310.0 | nM | 4.58 |
| CHEMBL5075902 | — | IC50 | > | 35000.0 | nM | - |