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Assay Detail

CHEMBL1811533

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

Binding
Inhibition of B-Raf V600E mutant
19
Total Activities
19
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

Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.
Stellwagen JC, Adjabeng GM, Arnone MR, Dickerson SH, Han C, Hornberger KR, King AJ, Mook RA, Petrov KG, Rheault TR, Rominger CM, Rossanese OW, Smitheman KN, Waterson AG, Uehling DE.
Bioorg Med Chem Lett (2011) 21 : 4436 -4440
PubMed 21733693 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 8.16 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1808262 1 9.30
CHEMBL1808255 1 9.22
CHEMBL1808259 1 9.22
CHEMBL1808256 1 9.10
CHEMBL1808263 1 9.05
CHEMBL1808261 1 8.92
CHEMBL1808260 1 8.89
CHEMBL1807711 1 8.44
CHEMBL1808264 1 8.42
CHEMBL1807709 1 8.40
CHEMBL1807706 1 8.30
CHEMBL1807707 1 8.05
CHEMBL1808257 1 8.02
CHEMBL1807710 1 7.92
CHEMBL1807705 1 7.92
CHEMBL1808258 1 7.47
CHEMBL1807708 1 6.88
CHEMBL1808254 1 5.87
CHEMBL1807712 1 5.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1808262 IC50 = 0.5 nM 9.30
CHEMBL1808255 IC50 = 0.6 nM 9.22
CHEMBL1808259 IC50 = 0.6 nM 9.22
CHEMBL1808256 IC50 = 0.8 nM 9.10
CHEMBL1808263 IC50 = 0.9 nM 9.05
CHEMBL1808261 IC50 = 1.2 nM 8.92
CHEMBL1808260 IC50 = 1.3 nM 8.89
CHEMBL1807711 IC50 = 3.6 nM 8.44
CHEMBL1808264 IC50 = 3.8 nM 8.42
CHEMBL1807709 IC50 = 4.0 nM 8.40
CHEMBL1807706 IC50 = 5.0 nM 8.30
CHEMBL1807707 IC50 = 9.0 nM 8.05
CHEMBL1808257 IC50 = 9.5 nM 8.02
CHEMBL1807710 IC50 = 12.0 nM 7.92
CHEMBL1807705 IC50 = 12.0 nM 7.92
CHEMBL1808258 IC50 = 34.0 nM 7.47
CHEMBL1807708 IC50 = 132.0 nM 6.88
CHEMBL1808254 IC50 = 1358.0 nM 5.87
CHEMBL1807712 IC50 = 1970.0 nM 5.71