Assay Detail
Binding
CHEMBL3804126
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Inhibition of wild type B-Raf (unknown origin) assessed as MEK1 phosphorylation using MEK1-Avitag as substrate after 1 hr by HTRF assay
38
Total Activities
38
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
Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 7.64 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 9.40 |
| CHEMBL3798780 | — | — | 1 | 9.30 |
| CHEMBL3798195 | — | — | 1 | 9.00 |
| CHEMBL3797403 | — | — | 1 | 9.00 |
| CHEMBL1197798 | — | — | 1 | 8.70 |
| CHEMBL3800081 | — | — | 1 | 8.70 |
| CHEMBL3799014 | — | — | 1 | 8.40 |
| CHEMBL3799342 | — | — | 1 | 8.30 |
| CHEMBL3800226 | — | — | 1 | 8.00 |
| CHEMBL3800014 | — | — | 1 | 8.00 |
| CHEMBL3798357 | — | — | 1 | 7.92 |
| CHEMBL3799488 | — | — | 1 | 7.80 |
| CHEMBL3798308 | — | — | 1 | 7.77 |
| CHEMBL3799568 | — | — | 1 | 7.72 |
| CHEMBL1229517 | VEMURAFENIB | 4.0 | 1 | 7.70 |
| CHEMBL3800364 | — | — | 1 | 7.68 |
| CHEMBL3798570 | — | — | 1 | 7.58 |
| CHEMBL3798235 | — | — | 1 | 7.58 |
| CHEMBL3799949 | — | — | 1 | 7.51 |
| CHEMBL3800227 | — | — | 1 | 7.42 |
| CHEMBL3798505 | — | — | 1 | 7.42 |
| CHEMBL3799483 | — | — | 1 | 7.39 |
| CHEMBL3798630 | — | — | 1 | 7.34 |
| CHEMBL3799451 | — | — | 1 | 7.29 |
| CHEMBL3798327 | — | — | 1 | 7.18 |
| CHEMBL3797494 | — | — | 1 | 7.17 |
| CHEMBL3798423 | — | — | 1 | 7.08 |
| CHEMBL3798256 | — | — | 1 | 7.05 |
| CHEMBL3799996 | — | — | 1 | 6.99 |
| CHEMBL3800157 | — | — | 1 | 6.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2028663 | DABRAFENIB | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3798780 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3797403 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3798195 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1197798 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3800081 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3799014 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3799342 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3800226 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3800014 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3798357 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3799488 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3798308 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3799568 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1229517 | VEMURAFENIB | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3800364 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3798570 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3798235 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3799949 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3800227 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3798505 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3799483 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3798630 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3799451 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3798327 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL3797494 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL3798423 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL3798256 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3799996 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL3800157 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL3799288 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL3800002 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL3799241 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL3797223 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL3797353 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL3798516 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL3798635 | — | IC50 | = | 412.0 | nM | 6.38 |
| CHEMBL3799046 | — | IC50 | > | 1000.0 | nM | - |