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Assay Detail

CHEMBL2341125

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

Binding
Inhibition of BRAF V600E mutant-mediated ERK phosphorylation in human A375 cells after 75 mins
ChEMBL ↗
52
Total Activities
52
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

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 52 6.82 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2335903 — — 1 8.40
CHEMBL2335904 — — 1 8.30
CHEMBL2335905 — — 1 8.10
CHEMBL2335907 — — 1 8.00
CHEMBL2144069 — — 1 7.82
CHEMBL2335910 — — 1 7.70
CHEMBL2335912 — — 1 7.60
CHEMBL2335908 — — 1 7.60
CHEMBL2335899 — — 1 7.60
CHEMBL2335896 — — 1 7.47
CHEMBL2335863 — — 1 7.40
CHEMBL2335885 — — 1 7.35
CHEMBL2335898 — — 1 7.35
CHEMBL2335897 — — 1 7.35
CHEMBL2335891 — — 1 7.31
CHEMBL2335895 — — 1 7.24
CHEMBL2335893 — — 1 7.22
CHEMBL2335906 — — 1 7.20
CHEMBL2335888 — — 1 7.20
CHEMBL2335892 — — 1 7.15
CHEMBL2335902 — — 1 7.13
CHEMBL2335871 — — 1 7.05
CHEMBL2335900 — — 1 6.85
CHEMBL2335894 — — 1 6.80
CHEMBL2335879 — — 1 6.77
CHEMBL2335864 — — 1 6.72
CHEMBL2335504 — — 1 6.72
CHEMBL2335882 — — 1 6.64
CHEMBL2335878 — — 1 6.64
CHEMBL2335877 — — 1 6.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2335903 — IC50 = 4.0 nM 8.40
CHEMBL2335904 — IC50 = 5.0 nM 8.30
CHEMBL2335905 — IC50 = 8.0 nM 8.10
CHEMBL2335907 — IC50 = 10.0 nM 8.00
CHEMBL2144069 — IC50 = 15.0 nM 7.82
CHEMBL2335910 — IC50 = 20.0 nM 7.70
CHEMBL2335912 — IC50 = 25.0 nM 7.60
CHEMBL2335908 — IC50 = 25.0 nM 7.60
CHEMBL2335899 — IC50 = 25.0 nM 7.60
CHEMBL2335896 — IC50 = 34.0 nM 7.47
CHEMBL2335863 — IC50 = 40.0 nM 7.40
CHEMBL2335885 — IC50 = 45.0 nM 7.35
CHEMBL2335898 — IC50 = 45.0 nM 7.35
CHEMBL2335897 — IC50 = 45.0 nM 7.35
CHEMBL2335891 — IC50 = 49.0 nM 7.31
CHEMBL2335895 — IC50 = 57.0 nM 7.24
CHEMBL2335893 — IC50 = 60.0 nM 7.22
CHEMBL2335906 — IC50 = 63.0 nM 7.20
CHEMBL2335888 — IC50 = 63.0 nM 7.20
CHEMBL2335892 — IC50 = 71.0 nM 7.15
CHEMBL2335902 — IC50 = 74.0 nM 7.13
CHEMBL2335871 — IC50 = 89.0 nM 7.05
CHEMBL2335900 — IC50 = 140.0 nM 6.85
CHEMBL2335894 — IC50 = 160.0 nM 6.80
CHEMBL2335879 — IC50 = 170.0 nM 6.77
CHEMBL2335864 — IC50 = 190.0 nM 6.72
CHEMBL2335504 — IC50 = 190.0 nM 6.72
CHEMBL2335882 — IC50 = 230.0 nM 6.64
CHEMBL2335878 — IC50 = 230.0 nM 6.64
CHEMBL2335877 — IC50 = 280.0 nM 6.55
CHEMBL2335880 — IC50 = 330.0 nM 6.48
CHEMBL2335881 — IC50 = 350.0 nM 6.46
CHEMBL2335876 — IC50 = 350.0 nM 6.46
CHEMBL2335889 — IC50 = 400.0 nM 6.40
CHEMBL2335884 — IC50 = 410.0 nM 6.39
CHEMBL2335909 — IC50 = 430.0 nM 6.37
CHEMBL2335911 — IC50 = 573.0 nM 6.24
CHEMBL2335887 — IC50 = 660.0 nM 6.18
CHEMBL2335901 — IC50 = 688.0 nM 6.16
CHEMBL2335890 — IC50 = 855.0 nM 6.07
CHEMBL2335867 — IC50 = 960.0 nM 6.02
CHEMBL2335886 — IC50 = 970.0 nM 6.01
CHEMBL2335883 — IC50 = 1600.0 nM 5.80
CHEMBL2335866 — IC50 = 1800.0 nM 5.75
CHEMBL2335868 — IC50 = 2000.0 nM 5.70
CHEMBL2335869 — IC50 = 3800.0 nM 5.42
CHEMBL2335874 — IC50 = 6400.0 nM 5.19
CHEMBL2335870 — IC50 = 7040.0 nM 5.15
CHEMBL2335872 — IC50 > 32000.0 nM -
CHEMBL2335865 — IC50 > 17000.0 nM -