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Assay Detail

CHEMBL958804

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

Binding
Inhibition of human recombinant B-Raf-V600E mutant
3
Total Activities
3
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

Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors.
Peifer C, Selig R, Kinkel K, Ott D, Totzke F, Schächtele C, Heidenreich R, Röcken M, Schollmeyer D, Laufer S.
J Med Chem (2008) 51 : 3814 -3824
PubMed 18529047 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.37 4.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL488646 1 4.42
CHEMBL201511 MALEIMIDE 1 4.40
CHEMBL509435 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL488646 IC50 = 38000.0 nM 4.42
CHEMBL201511 MALEIMIDE IC50 = 40000.0 nM 4.40
CHEMBL509435 IC50 = 50000.0 nM 4.30