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Assay Detail

CHEMBL3129554

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

Binding
Inhibition of N-terminal FLAG-tagged wild type BRAF (unknown origin) expressed in baculovirus system using GST-MEK1(K96R) as substrate after 20 mins
1
Total Activities
1
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

Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives.
Okaniwa M, Hirose M, Arita T, Yabuki M, Nakamura A, Takagi T, Kawamoto T, Uchiyama N, Sumita A, Tsutsumi S, Tottori T, Inui Y, Sang BC, Yano J, Aertgeerts K, Yoshida S, Ishikawa T.
J Med Chem (2013) 56 : 6478 -6494
PubMed 23906342 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.08 8.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3125890 1 8.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3125890 IC50 = 8.3 nM 8.08