Assay Detail
Binding
CHEMBL3804129
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Inhibition of B-Raf V600E mutant in human A375 cells assessed as ERK phosphorylation preincubated for 1 hr by Western blot method
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A-375 |
| 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 | 7.31 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 9.00 |
| CHEMBL1197798 | — | — | 1 | 8.70 |
| CHEMBL3797403 | — | — | 1 | 8.22 |
| CHEMBL3798780 | — | — | 1 | 8.15 |
| CHEMBL3798195 | — | — | 1 | 8.00 |
| CHEMBL3800364 | — | — | 1 | 7.96 |
| CHEMBL3800226 | — | — | 1 | 7.92 |
| CHEMBL3799014 | — | — | 1 | 7.82 |
| CHEMBL1229517 | VEMURAFENIB | 4.0 | 1 | 7.77 |
| CHEMBL3799488 | — | — | 1 | 7.77 |
| CHEMBL3798357 | — | — | 1 | 7.62 |
| CHEMBL3800227 | — | — | 1 | 7.57 |
| CHEMBL3798308 | — | — | 1 | 7.55 |
| CHEMBL3800081 | — | — | 1 | 7.51 |
| CHEMBL3798235 | — | — | 1 | 7.51 |
| CHEMBL3798570 | — | — | 1 | 7.48 |
| CHEMBL3800014 | — | — | 1 | 7.40 |
| CHEMBL3799451 | — | — | 1 | 7.40 |
| CHEMBL3798630 | — | — | 1 | 7.39 |
| CHEMBL3799949 | — | — | 1 | 7.36 |
| CHEMBL3798327 | — | — | 1 | 7.35 |
| CHEMBL3798256 | — | — | 1 | 7.27 |
| CHEMBL3799342 | — | — | 1 | 7.20 |
| CHEMBL3798505 | — | — | 1 | 7.19 |
| CHEMBL3797223 | — | — | 1 | 7.06 |
| CHEMBL3799288 | — | — | 1 | 6.89 |
| CHEMBL3799241 | — | — | 1 | 6.76 |
| CHEMBL3799483 | — | — | 1 | 6.75 |
| CHEMBL3800002 | — | — | 1 | 6.70 |
| CHEMBL3797494 | — | — | 1 | 6.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2028663 | DABRAFENIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1197798 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3797403 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3798780 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3798195 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3800364 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3800226 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3799014 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1229517 | VEMURAFENIB | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3799488 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3798357 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3800227 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3798308 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3800081 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3798235 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3798570 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3800014 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3799451 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3798630 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3799949 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3798327 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3798256 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3799342 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL3798505 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3797223 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL3799288 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3799241 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL3799483 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL3800002 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL3797494 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL3798423 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL3799996 | — | IC50 | = | 293.0 | nM | 6.53 |
| CHEMBL3798516 | — | IC50 | = | 356.0 | nM | 6.45 |
| CHEMBL3798635 | — | IC50 | = | 356.0 | nM | 6.45 |
| CHEMBL3797353 | — | IC50 | = | 603.0 | nM | 6.22 |
| CHEMBL3799568 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL3799046 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3800378 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3800157 | — | IC50 | > | 1000.0 | nM | - |