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Assay Detail

CHEMBL1948264

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

Binding
Inhibition of wild-type B-Raf
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase B-raf (CHEMBL5145)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Small molecule inhibitors of BRAF in clinical trials.
Zambon A, Niculescu-Duvaz I, Niculescu-Duvaz D, Marais R, Springer CJ.
Bioorg Med Chem Lett (2012) 22 : 789 -792
PubMed 22222036 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.99 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1946171 1 8.52
CHEMBL1230020 PLX-4720 1 7.89
CHEMBL1946170 REGORAFENIB 4.0 1 7.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1946171 IC50 = 3.0 nM 8.52
CHEMBL1230020 PLX-4720 IC50 = 13.0 nM 7.89
CHEMBL1946170 REGORAFENIB IC50 = 28.0 nM 7.55