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Assay Detail

CHEMBL3636911

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

Binding
Inhibition of B-RAF V600E mutant in human Malme-3M cells assessed as phosphorylation of ERK
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Malme-3M
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 RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.
Williams TE, Subramanian S, Verhagen J, McBride CM, Costales A, Sung L, Antonios-McCrea W, McKenna M, Louie AK, Ramurthy S, Levine B, Shafer CM, Machajewski T, Renhowe PA, Appleton BA, Amiri P, Chou J, Stuart D, Aardalen K, Poon D.
ACS Med Chem Lett (2015) 6 : 961 -965
PubMed 26396681 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.40 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL558752 RAF-265 2.0 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL558752 RAF-265 IC50 = 40.0 nM 7.40