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Assay Detail

CHEMBL1047417

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

Binding
Inhibition of recombinant Braf V600E mutant
12
Total Activities
12
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

Selective inhibitors of the mutant B-Raf pathway: discovery of a potent and orally bioavailable aminoisoquinoline.
Smith AL, DeMorin FF, Paras NA, Huang Q, Petkus JK, Doherty EM, Nixey T, Kim JL, Whittington DA, Epstein LF, Lee MR, Rose MJ, Babij C, Fernando M, Hess K, Le Q, Beltran P, Carnahan J.
J Med Chem (2009) 52 : 6189 -6192
PubMed 19764794 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.97 9.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL385956 1 9.34
CHEMBL3215582 1 8.80
CHEMBL212964 1 8.77
CHEMBL565884 1 8.47
CHEMBL576787 1 8.27
CHEMBL571703 1 7.77
CHEMBL571278 1 7.75
CHEMBL576985 1 7.68
CHEMBL570567 1 7.41
CHEMBL565885 1 7.25
CHEMBL569882 1 7.16
CHEMBL570573 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL385956 IC50 = 0.46 nM 9.34
CHEMBL3215582 IC50 = 1.6 nM 8.80
CHEMBL212964 IC50 = 1.7 nM 8.77
CHEMBL565884 IC50 = 3.4 nM 8.47
CHEMBL576787 IC50 = 5.4 nM 8.27
CHEMBL571703 IC50 = 17.0 nM 7.77
CHEMBL571278 IC50 = 18.0 nM 7.75
CHEMBL576985 IC50 = 21.0 nM 7.68
CHEMBL570567 IC50 = 39.0 nM 7.41
CHEMBL565885 IC50 = 56.0 nM 7.25
CHEMBL569882 IC50 = 70.0 nM 7.16
CHEMBL570573 IC50 = 110.0 nM 6.96