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Assay Detail

CHEMBL4329882

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

Binding
Inhibition of recombinant human full length GST-tagged BRAF expressed in baculovirus expression system
11
Total Activities
11
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

Privileged Structures and Polypharmacology within and between Protein Families.
Meyers J, Chessum NEA, Ali S, Mok NY, Wilding B, Pasqua AE, Rowlands M, Tucker MJ, Evans LE, Rye CS, O'Fee L, Le Bihan YV, Burke R, Carter M, Workman P, Blagg J, Brown N, van Montfort RLM, Jones K, Cheeseman MD.
ACS Med Chem Lett (2018) 9 : 1199 -1204
PubMed 30613326 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.02 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2028663 DABRAFENIB 4.0 1 8.30
CHEMBL3125890 1 8.10
CHEMBL1229517 VEMURAFENIB 4.0 1 7.00
CHEMBL1230020 PLX-4720 1 6.80
CHEMBL4070633 1 6.38
CHEMBL4087666 1 5.54
CHEMBL4091953 1 -
CHEMBL525191 1 -
CHEMBL558752 RAF-265 2.0 1 -
CHEMBL2144069 1 -
CHEMBL4473676 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2028663 DABRAFENIB IC50 = 5.0 nM 8.30
CHEMBL3125890 IC50 = 8.0 nM 8.10
CHEMBL1229517 VEMURAFENIB IC50 = 100.0 nM 7.00
CHEMBL1230020 PLX-4720 IC50 = 160.0 nM 6.80
CHEMBL4070633 IC50 = 420.0 nM 6.38
CHEMBL4087666 IC50 = 2900.0 nM 5.54
CHEMBL4091953 IC50 - -
CHEMBL525191 IC50 - -
CHEMBL558752 RAF-265 IC50 - -
CHEMBL2144069 IC50 - -
CHEMBL4473676 IC50 > 10000.0 nM -