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Assay Detail

CHEMBL2090789

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

Binding
Inhibition of human 6x-His tagged BRAF V600E mutant expressed in Sf9 cells by ELISA based kinase assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Identification of a novel family of BRAF(V600E) inhibitors.
Qin J, Xie P, Ventocilla C, Zhou G, Vultur A, Chen Q, Liu Q, Herlyn M, Winkler J, Marmorstein R.
J Med Chem (2012) 55 : 5220 -5230
PubMed 22537109 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.40 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2030274 1 7.10
CHEMBL2030272 1 7.00
CHEMBL2087793 1 6.92
CHEMBL2088028 1 6.85
CHEMBL2088021 1 6.85
CHEMBL2030281 1 6.82
CHEMBL2087792 1 6.72
CHEMBL2088018 1 6.72
CHEMBL2088022 1 6.68
CHEMBL2030271 1 6.60
CHEMBL2088019 1 6.55
CHEMBL2087788 1 6.52
CHEMBL2030469 1 6.50
CHEMBL2030468 1 6.42
CHEMBL581146 1 6.40
CHEMBL2088026 1 6.28
CHEMBL2087789 1 6.22
CHEMBL2088027 1 6.17
CHEMBL2087787 1 6.16
CHEMBL2088020 1 6.14
CHEMBL2088024 1 6.14
CHEMBL2087791 1 6.10
CHEMBL2087790 1 6.05
CHEMBL2088023 1 5.80
CHEMBL2088025 1 5.44
CHEMBL1342041 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2030274 IC50 = 80.0 nM 7.10
CHEMBL2030272 IC50 = 100.0 nM 7.00
CHEMBL2087793 IC50 = 120.0 nM 6.92
CHEMBL2088028 IC50 = 140.0 nM 6.85
CHEMBL2088021 IC50 = 140.0 nM 6.85
CHEMBL2030281 IC50 = 150.0 nM 6.82
CHEMBL2087792 IC50 = 190.0 nM 6.72
CHEMBL2088018 IC50 = 190.0 nM 6.72
CHEMBL2088022 IC50 = 210.0 nM 6.68
CHEMBL2030271 IC50 = 250.0 nM 6.60
CHEMBL2088019 IC50 = 280.0 nM 6.55
CHEMBL2087788 IC50 = 300.0 nM 6.52
CHEMBL2030469 IC50 = 320.0 nM 6.50
CHEMBL2030468 IC50 = 380.0 nM 6.42
CHEMBL581146 IC50 = 400.0 nM 6.40
CHEMBL2088026 IC50 = 520.0 nM 6.28
CHEMBL2087789 IC50 = 600.0 nM 6.22
CHEMBL2088027 IC50 = 670.0 nM 6.17
CHEMBL2087787 IC50 = 700.0 nM 6.16
CHEMBL2088020 IC50 = 720.0 nM 6.14
CHEMBL2088024 IC50 = 720.0 nM 6.14
CHEMBL2087791 IC50 = 800.0 nM 6.10
CHEMBL2087790 IC50 = 900.0 nM 6.05
CHEMBL2088023 IC50 = 1600.0 nM 5.80
CHEMBL2088025 IC50 = 3600.0 nM 5.44
CHEMBL1342041 IC50 = 6100.0 nM 5.21