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Assay Detail

CHEMBL3636900

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Functional
Antiproliferative activity against human SK-MEL-28 cells harboring B-RAF V600E mutant
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type SK-MEL-28
Confidence 1 — Organism
Curated By Autocuration

Target

SK-MEL-28 (CHEMBL614919)
Type CELL-LINE
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 10 6.46 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3632721 1 7.30
CHEMBL3632719 1 6.92
CHEMBL558752 RAF-265 2.0 1 6.80
CHEMBL3335371 1 6.75
CHEMBL3632720 1 6.64
CHEMBL3632723 1 6.22
CHEMBL3632724 1 6.13
CHEMBL470808 1 6.05
CHEMBL3632718 1 5.96
CHEMBL3632722 1 5.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3632721 IC50 = 50.0 nM 7.30
CHEMBL3632719 IC50 = 120.0 nM 6.92
CHEMBL558752 RAF-265 IC50 = 160.0 nM 6.80
CHEMBL3335371 IC50 = 180.0 nM 6.75
CHEMBL3632720 IC50 = 230.0 nM 6.64
CHEMBL3632723 IC50 = 600.0 nM 6.22
CHEMBL3632724 IC50 = 740.0 nM 6.13
CHEMBL470808 IC50 = 900.0 nM 6.05
CHEMBL3632718 IC50 = 1100.0 nM 5.96
CHEMBL3632722 IC50 = 1620.0 nM 5.79