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Assay Detail

CHEMBL869911

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Binding
Inhibition bRaf kinase activity
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

The identification of potent and selective imidazole-based inhibitors of B-Raf kinase.
Takle AK, Brown MJ, Davies S, Dean DK, Francis G, Gaiba A, Hird AW, King FD, Lovell PJ, Naylor A, Reith AD, Steadman JG, Wilson DM.
Bioorg Med Chem Lett (2006) 16 : 378 -381
PubMed 16260133 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.48 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200889 1 8.22
CHEMBL381250 1 8.22
CHEMBL200320 1 8.10
CHEMBL373011 1 8.00
CHEMBL200172 1 7.92
CHEMBL200863 1 7.89
CHEMBL371952 1 7.89
CHEMBL381447 1 7.85
CHEMBL200118 1 7.48
CHEMBL426476 1 7.40
CHEMBL68215 1 6.47
CHEMBL371694 1 6.05
CHEMBL200259 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200889 IC50 = 6.0 nM 8.22
CHEMBL381250 IC50 = 6.0 nM 8.22
CHEMBL200320 IC50 = 8.0 nM 8.10
CHEMBL373011 IC50 = 10.0 nM 8.00
CHEMBL200172 IC50 = 12.0 nM 7.92
CHEMBL200863 IC50 = 13.0 nM 7.89
CHEMBL371952 IC50 = 13.0 nM 7.89
CHEMBL381447 IC50 = 14.0 nM 7.85
CHEMBL200118 IC50 = 33.0 nM 7.48
CHEMBL426476 IC50 = 40.0 nM 7.40
CHEMBL68215 IC50 = 339.0 nM 6.47
CHEMBL371694 IC50 = 900.0 nM 6.05
CHEMBL200259 IC50 = 1585.0 nM 5.80