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Assay Detail

CHEMBL4273764

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

Binding
Inhibition of mouse full length GST-tagged BRAF V600E mutant using recombinant human His6-tagged MEK1 as substrate preincubated for 1 hr followed by substrate addition measured after 25 mins by ELISA
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Serine/threonine-protein kinase B-raf (CHEMBL2331061)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis, anticancer activity and molecular modeling studies of 1,2,4-triazole derivatives as EGFR inhibitors.
El-Sherief HAM, Youssif BGM, Abbas Bukhari SN, Abdelazeem AH, Abdel-Aziz M, Abdel-Rahman HM.
Eur J Med Chem (2018) 156 : 774 -789
PubMed 30055463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.37 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1079742 ERLOTINIB HYDROCHLORIDE 4.0 1 7.40
CHEMBL4279008 1 5.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1079742 ERLOTINIB HYDROCHLORIDE IC50 = 40.0 nM 7.40
CHEMBL4279008 IC50 = 4700.0 nM 5.33