Assay Detail
Binding
CHEMBL3804127
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of B-Raf V600E mutant (unknown origin) assessed as MEK1 phosphorylation using MEK1-Avitag as substrate after 1 hr by HTRF assay
39
Total Activities
39
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 | 39 | 8.07 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3797403 | — | — | 1 | 9.70 |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 9.00 |
| CHEMBL3798195 | — | — | 1 | 9.00 |
| CHEMBL3798780 | — | — | 1 | 9.00 |
| CHEMBL3800081 | — | — | 1 | 9.00 |
| CHEMBL3799949 | — | — | 1 | 8.70 |
| CHEMBL3800364 | — | — | 1 | 8.70 |
| CHEMBL1197798 | — | — | 1 | 8.70 |
| CHEMBL3800226 | — | — | 1 | 8.52 |
| CHEMBL3799014 | — | — | 1 | 8.52 |
| CHEMBL3800014 | — | — | 1 | 8.52 |
| CHEMBL1229517 | VEMURAFENIB | 4.0 | 1 | 8.40 |
| CHEMBL3798630 | — | — | 1 | 8.40 |
| CHEMBL3798235 | — | — | 1 | 8.30 |
| CHEMBL3799488 | — | — | 1 | 8.22 |
| CHEMBL3799342 | — | — | 1 | 8.22 |
| CHEMBL3800227 | — | — | 1 | 8.15 |
| CHEMBL3798308 | — | — | 1 | 8.15 |
| CHEMBL3798570 | — | — | 1 | 8.10 |
| CHEMBL3799568 | — | — | 1 | 8.10 |
| CHEMBL3798256 | — | — | 1 | 8.10 |
| CHEMBL3798357 | — | — | 1 | 8.05 |
| CHEMBL3800002 | — | — | 1 | 8.05 |
| CHEMBL3798327 | — | — | 1 | 7.85 |
| CHEMBL3798505 | — | — | 1 | 7.82 |
| CHEMBL3797494 | — | — | 1 | 7.80 |
| CHEMBL3799288 | — | — | 1 | 7.75 |
| CHEMBL3799451 | — | — | 1 | 7.75 |
| CHEMBL3799483 | — | — | 1 | 7.68 |
| CHEMBL3797223 | — | — | 1 | 7.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3797403 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL2028663 | DABRAFENIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3800081 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3798195 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3798780 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3799949 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3800364 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1197798 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3800226 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3799014 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3800014 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1229517 | VEMURAFENIB | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3798630 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3798235 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3799342 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3799488 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3800227 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3798308 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3798256 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3799568 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3798570 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3798357 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3800002 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3798327 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3798505 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3797494 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3799288 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3799451 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3799483 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3797223 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3798516 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3798423 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3799241 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3797353 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3799996 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3800157 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL3800378 | — | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL3798635 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL3799046 | — | IC50 | > | 1000.0 | nM | - |