Assay Detail
Binding
CHEMBL2033392
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Inhibition of BRAF V600E mutant-mediated MEK phosphorylation in human A375 cells after 2 hrs
36
Total Activities
36
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
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 6.58 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2029997 | — | — | 1 | 7.68 |
| CHEMBL2029999 | — | — | 1 | 7.21 |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | 7.09 |
| CHEMBL2029993 | — | — | 1 | 7.08 |
| CHEMBL2029990 | — | — | 1 | 7.03 |
| CHEMBL2029967 | — | — | 1 | 7.00 |
| CHEMBL2029987 | — | — | 1 | 6.96 |
| CHEMBL1824069 | — | — | 1 | 6.92 |
| CHEMBL2029972 | — | — | 1 | 6.87 |
| CHEMBL2029991 | — | — | 1 | 6.85 |
| CHEMBL2029981 | — | — | 1 | 6.81 |
| CHEMBL2029983 | — | — | 1 | 6.76 |
| CHEMBL2029989 | — | — | 1 | 6.74 |
| CHEMBL2029986 | — | — | 1 | 6.56 |
| CHEMBL1824076 | — | — | 1 | 6.54 |
| CHEMBL2029984 | — | — | 1 | 6.51 |
| CHEMBL2029978 | — | — | 1 | 6.49 |
| CHEMBL2029985 | — | — | 1 | 6.48 |
| CHEMBL1824073 | — | — | 1 | 6.48 |
| CHEMBL2029982 | — | — | 1 | 6.47 |
| CHEMBL2029969 | — | — | 1 | 6.47 |
| CHEMBL2029974 | — | — | 1 | 6.47 |
| CHEMBL2029971 | — | — | 1 | 6.45 |
| CHEMBL2029992 | — | — | 1 | 6.33 |
| CHEMBL2029998 | — | — | 1 | 6.32 |
| CHEMBL2029994 | — | — | 1 | 6.30 |
| CHEMBL2029977 | — | — | 1 | 6.19 |
| CHEMBL2029980 | — | — | 1 | 6.19 |
| CHEMBL2029995 | — | — | 1 | 6.17 |
| CHEMBL2029973 | — | — | 1 | 6.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2029997 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2029999 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL2029988 | CEP-32496 | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL2029993 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL2029990 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL2029967 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL2029987 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL1824069 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL2029972 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL2029991 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL2029981 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL2029983 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL2029989 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL2029986 | — | IC50 | = | 276.0 | nM | 6.56 |
| CHEMBL1824076 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL2029984 | — | IC50 | = | 308.0 | nM | 6.51 |
| CHEMBL2029978 | — | IC50 | = | 324.0 | nM | 6.49 |
| CHEMBL1824073 | — | IC50 | = | 333.0 | nM | 6.48 |
| CHEMBL2029985 | — | IC50 | = | 332.0 | nM | 6.48 |
| CHEMBL2029982 | — | IC50 | = | 339.0 | nM | 6.47 |
| CHEMBL2029969 | — | IC50 | = | 336.0 | nM | 6.47 |
| CHEMBL2029974 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL2029971 | — | IC50 | = | 355.0 | nM | 6.45 |
| CHEMBL2029992 | — | IC50 | = | 469.0 | nM | 6.33 |
| CHEMBL2029998 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL2029994 | — | IC50 | = | 505.0 | nM | 6.30 |
| CHEMBL2029980 | — | IC50 | = | 645.0 | nM | 6.19 |
| CHEMBL2029977 | — | IC50 | = | 649.0 | nM | 6.19 |
| CHEMBL2029995 | — | IC50 | = | 681.0 | nM | 6.17 |
| CHEMBL2029973 | — | IC50 | = | 956.0 | nM | 6.02 |
| CHEMBL2029975 | — | IC50 | = | 1134.0 | nM | 5.95 |
| CHEMBL2029968 | — | IC50 | = | 1131.0 | nM | 5.95 |
| CHEMBL2029979 | — | IC50 | = | 2229.0 | nM | 5.65 |
| CHEMBL2029976 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL2029970 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL2029996 | — | IC50 | > | 1667.0 | nM | - |