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Assay Detail

CHEMBL2341126

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human recombinant N-terminus His-tagged BRAF V600E mutant expressed in Sf9 cells coexpressing CDC37 using biotinylated MEK as substrate and MgCl2 incubated for 20 mins prior to MgCl2 addition measured after 1 hr in presence of 10 uM ATP
ChEMBL ↗
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase B-raf (CHEMBL5145) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors.
Vasbinder MM, Aquila B, Augustin M, Chen H, Cheung T, Cook D, Drew L, Fauber BP, Glossop S, Grondine M, Hennessy E, Johannes J, Lee S, Lyne P, Mörtl M, Omer C, Palakurthi S, Pontz T, Read J, Sha L, Shen M, Steinbacher S, Wang H, Wu A, Ye M.
J Med Chem (2013) 56 : 1996 -2015
PubMed 23398453 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 51 6.85 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2335863 — — 1 7.80
CHEMBL2335896 — — 1 7.72
CHEMBL2335871 — — 1 7.64
CHEMBL2335893 — — 1 7.57
CHEMBL2335882 — — 1 7.54
CHEMBL2335885 — — 1 7.50
CHEMBL2144069 — — 1 7.47
CHEMBL2335895 — — 1 7.44
CHEMBL2335903 — — 1 7.43
CHEMBL2335891 — — 1 7.42
CHEMBL2335906 — — 1 7.41
CHEMBL2335892 — — 1 7.40
CHEMBL2335894 — — 1 7.29
CHEMBL2335879 — — 1 7.28
CHEMBL2335907 — — 1 7.24
CHEMBL2335888 — — 1 7.24
CHEMBL2335889 — — 1 7.17
CHEMBL2335864 — — 1 7.11
CHEMBL2335912 — — 1 7.09
CHEMBL2335878 — — 1 7.05
CHEMBL2335904 — — 1 7.03
CHEMBL2335884 — — 1 7.00
CHEMBL2335899 — — 1 6.99
CHEMBL2335876 — — 1 6.92
CHEMBL2335880 — — 1 6.89
CHEMBL2335867 — — 1 6.88
CHEMBL2335908 — — 1 6.85
CHEMBL2335887 — — 1 6.82
CHEMBL2335905 — — 1 6.80
CHEMBL2335890 — — 1 6.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2335863 — IC50 = 16.0 nM 7.80
CHEMBL2335896 — IC50 = 19.0 nM 7.72
CHEMBL2335871 — IC50 = 23.0 nM 7.64
CHEMBL2335893 — IC50 = 27.0 nM 7.57
CHEMBL2335882 — IC50 = 29.0 nM 7.54
CHEMBL2335885 — IC50 = 32.0 nM 7.50
CHEMBL2144069 — IC50 = 34.0 nM 7.47
CHEMBL2335895 — IC50 = 36.0 nM 7.44
CHEMBL2335903 — IC50 = 37.0 nM 7.43
CHEMBL2335891 — IC50 = 38.0 nM 7.42
CHEMBL2335906 — IC50 = 39.0 nM 7.41
CHEMBL2335892 — IC50 = 40.0 nM 7.40
CHEMBL2335894 — IC50 = 51.0 nM 7.29
CHEMBL2335879 — IC50 = 53.0 nM 7.28
CHEMBL2335888 — IC50 = 57.0 nM 7.24
CHEMBL2335907 — IC50 = 57.0 nM 7.24
CHEMBL2335889 — IC50 = 67.0 nM 7.17
CHEMBL2335864 — IC50 = 77.0 nM 7.11
CHEMBL2335912 — IC50 = 81.0 nM 7.09
CHEMBL2335878 — IC50 = 89.0 nM 7.05
CHEMBL2335904 — IC50 = 94.0 nM 7.03
CHEMBL2335884 — IC50 = 101.0 nM 7.00
CHEMBL2335899 — IC50 = 102.0 nM 6.99
CHEMBL2335876 — IC50 = 120.0 nM 6.92
CHEMBL2335880 — IC50 = 130.0 nM 6.89
CHEMBL2335867 — IC50 = 132.0 nM 6.88
CHEMBL2335908 — IC50 = 140.0 nM 6.85
CHEMBL2335887 — IC50 = 150.0 nM 6.82
CHEMBL2335905 — IC50 = 158.0 nM 6.80
CHEMBL2335890 — IC50 = 168.0 nM 6.78
CHEMBL2335910 — IC50 = 187.0 nM 6.73
CHEMBL2335881 — IC50 = 192.0 nM 6.72
CHEMBL2335886 — IC50 = 210.0 nM 6.68
CHEMBL2335902 — IC50 = 214.0 nM 6.67
CHEMBL2335898 — IC50 = 223.0 nM 6.65
CHEMBL2335901 — IC50 = 230.0 nM 6.64
CHEMBL2335900 — IC50 = 256.0 nM 6.59
CHEMBL2335897 — IC50 = 254.0 nM 6.59
CHEMBL2335866 — IC50 = 265.0 nM 6.58
CHEMBL2335883 — IC50 = 300.0 nM 6.52
CHEMBL2335875 — IC50 = 330.0 nM 6.48
CHEMBL2335877 — IC50 = 344.0 nM 6.46
CHEMBL2335868 — IC50 = 369.0 nM 6.43
CHEMBL2335865 — IC50 = 399.0 nM 6.40
CHEMBL2335870 — IC50 = 601.0 nM 6.22
CHEMBL2335874 — IC50 = 777.0 nM 6.11
CHEMBL2335869 — IC50 = 917.0 nM 6.04
CHEMBL2335872 — IC50 = 2300.0 nM 5.64
CHEMBL2335909 — IC50 = 2290.0 nM 5.64
CHEMBL2335911 — IC50 = 2600.0 nM 5.58