Assay Detail
Binding
CHEMBL1217119
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Inhibition of B-Raf V600E mutant
85
Total Activities
85
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
Novel hinge binder improves activity and pharmacokinetic properties of BRAF inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 85 | 7.05 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1214000 | — | — | 1 | 8.70 |
| CHEMBL1214001 | — | — | 1 | 8.70 |
| CHEMBL1214614 | — | — | 1 | 8.52 |
| CHEMBL1213998 | — | — | 1 | 8.52 |
| CHEMBL1214612 | — | — | 1 | 8.40 |
| CHEMBL1214058 | — | — | 1 | 8.40 |
| CHEMBL1213999 | — | — | 1 | 8.40 |
| CHEMBL1213952 | — | — | 1 | 8.40 |
| CHEMBL1214129 | — | — | 1 | 8.30 |
| CHEMBL1213691 | — | — | 1 | 8.30 |
| CHEMBL1213824 | — | — | 1 | 8.22 |
| CHEMBL1214617 | — | — | 1 | 8.15 |
| CHEMBL1214619 | — | — | 1 | 8.00 |
| CHEMBL1213821 | — | — | 1 | 7.96 |
| CHEMBL1212949 | — | — | 1 | 7.77 |
| CHEMBL1213884 | — | — | 1 | 7.77 |
| CHEMBL1214056 | — | — | 1 | 7.72 |
| CHEMBL1214055 | — | — | 1 | 7.70 |
| CHEMBL1213822 | — | — | 1 | 7.68 |
| CHEMBL1214563 | — | — | 1 | 7.68 |
| CHEMBL1214616 | — | — | 1 | 7.62 |
| CHEMBL1214057 | — | — | 1 | 7.62 |
| CHEMBL1213754 | — | — | 1 | 7.60 |
| CHEMBL1213689 | — | — | 1 | 7.52 |
| CHEMBL1214618 | — | — | 1 | 7.47 |
| CHEMBL1214441 | — | — | 1 | 7.40 |
| CHEMBL1213753 | — | — | 1 | 7.38 |
| CHEMBL1214378 | — | — | 1 | 7.37 |
| CHEMBL1214440 | — | — | 1 | 7.29 |
| CHEMBL1214439 | — | — | 1 | 7.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1214000 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1214001 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1213998 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1214614 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1214612 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1214058 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1213999 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1213952 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1214129 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1213691 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1213824 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1214617 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1214619 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1213821 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1213884 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1212949 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1214056 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1214055 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1213822 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1214563 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1214616 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL1214057 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL1213754 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1213689 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1214618 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1214441 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1213753 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL1214378 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL1214440 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL1214439 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1214505 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL1214139 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL1213951 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL1214132 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL1213692 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL1214251 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL1092541 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL1214613 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL1214131 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL1214134 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1214325 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL1214133 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL1214507 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL1212951 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1213757 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL1214135 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL1214504 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL1213760 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL1214326 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL1091849 | — | IC50 | = | 110.0 | nM | 6.96 |