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Assay Detail

CHEMBL5581709

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

Binding
Inhibition of B-RAF V600E mutant (unknown origin)
11
Total Activities
11
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 11 7.84 10.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5591799 1 10.18
CHEMBL2028663 DABRAFENIB 4.0 1 9.19
CHEMBL5583891 1 8.89
CHEMBL5591160 1 8.23
CHEMBL3977543 BELVARAFENIB 2.0 1 8.05
CHEMBL1336 SORAFENIB 4.0 1 7.42
CHEMBL4583691 NAPORAFENIB 3.0 1 7.31
CHEMBL5518141 1 7.20
CHEMBL5557132 1 7.05
CHEMBL3348923 TOVORAFENIB 4.0 1 7.03
CHEMBL5590473 1 5.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5591799 IC50 = 0.066 nM 10.18
CHEMBL2028663 DABRAFENIB IC50 = 0.65 nM 9.19
CHEMBL5583891 IC50 = 1.3 nM 8.89
CHEMBL5591160 IC50 = 5.89 nM 8.23
CHEMBL3977543 BELVARAFENIB IC50 = 9.0 nM 8.05
CHEMBL1336 SORAFENIB IC50 = 38.0 nM 7.42
CHEMBL4583691 NAPORAFENIB IC50 = 49.2 nM 7.31
CHEMBL5518141 IC50 = 63.0 nM 7.20
CHEMBL5557132 IC50 = 89.0 nM 7.05
CHEMBL3348923 TOVORAFENIB IC50 = 94.2 nM 7.03
CHEMBL5590473 IC50 = 1840.0 nM 5.74