Assay Detail
Binding
CHEMBL1811532
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Inhibition of B-Raf V600E mutant in human SK-MEL-28 cells assessed as reduction of ERK phosphorylation after 1 hr
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SK-MEL-28 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase B-raf (CHEMBL5145) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 19 | 7.57 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1808255 | — | — | 1 | 8.40 |
| CHEMBL1808261 | — | — | 1 | 8.15 |
| CHEMBL1807711 | — | — | 1 | 8.15 |
| CHEMBL1808259 | — | — | 1 | 8.10 |
| CHEMBL1808257 | — | — | 1 | 8.05 |
| CHEMBL1808260 | — | — | 1 | 8.00 |
| CHEMBL1808256 | — | — | 1 | 8.00 |
| CHEMBL1808262 | — | — | 1 | 7.96 |
| CHEMBL1808258 | — | — | 1 | 7.68 |
| CHEMBL1808264 | — | — | 1 | 7.64 |
| CHEMBL1808263 | — | — | 1 | 7.62 |
| CHEMBL1807710 | — | — | 1 | 7.28 |
| CHEMBL1807708 | — | — | 1 | 7.00 |
| CHEMBL1807709 | — | — | 1 | 6.24 |
| CHEMBL1807712 | — | — | 1 | 5.33 |
| CHEMBL1808254 | — | — | 1 | - |
| CHEMBL1807705 | — | — | 1 | - |
| CHEMBL1807706 | — | — | 1 | - |
| CHEMBL1807707 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1808255 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1808261 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1807711 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1808259 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1808257 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1808260 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1808256 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1808262 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1808258 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1808264 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1808263 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL1807710 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL1807708 | — | EC50 | = | 99.0 | nM | 7.00 |
| CHEMBL1807709 | — | EC50 | = | 580.0 | nM | 6.24 |
| CHEMBL1807712 | — | EC50 | = | 4731.0 | nM | 5.33 |
| CHEMBL1808254 | — | EC50 | > | 20000.0 | nM | - |
| CHEMBL1807705 | — | EC50 | > | 2200.0 | nM | - |
| CHEMBL1807706 | — | EC50 | > | 20000.0 | nM | - |
| CHEMBL1807707 | — | EC50 | > | 10000.0 | nM | - |