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Assay Detail

CHEMBL5581708

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Binding
Inhibition of wild-type B-RAF (unknown origin)
8
Total Activities
8
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

An overview of RAF kinases and their inhibitors (2019-2023).
Hashem O, Shahin AI, Al Hindawi MA, Fageeri MF, Al-Sbbagh SA, Tarazi H, El-Gamal MI.
Eur J Med Chem (2024) 275 : 116631 -116631
PubMed 38954961 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.64 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2028663 DABRAFENIB 4.0 1 8.49
CHEMBL4583691 NAPORAFENIB 3.0 1 8.43
CHEMBL5591160 1 8.23
CHEMBL1336 SORAFENIB 4.0 1 7.66
CHEMBL5518141 1 7.30
CHEMBL5557132 1 7.15
CHEMBL3348923 TOVORAFENIB 4.0 1 6.20
CHEMBL5591799 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2028663 DABRAFENIB IC50 = 3.2 nM 8.49
CHEMBL4583691 NAPORAFENIB IC50 = 3.7 nM 8.43
CHEMBL5591160 IC50 = 5.9 nM 8.23
CHEMBL1336 SORAFENIB IC50 = 22.0 nM 7.66
CHEMBL5518141 IC50 = 50.0 nM 7.30
CHEMBL5557132 IC50 = 71.0 nM 7.15
CHEMBL3348923 TOVORAFENIB IC50 = 633.0 nM 6.20
CHEMBL5591799 IC50 = 1.1 nM -